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Peter Blumberg

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Noemi Kedei; Nancy E Lewin; Langston Lim; Poonam Mannan; Yam B Poudel; Arnab Rudra; Julia Selezneva; Peter M Blumberg; Derek C Braun; Jinqiu Chen; Thomas J Cummins; Susan H Garfield; Tamás Géczy; Madeleine R Heldman; Michelle A Herrmann; Gary E Keck
Biological profile of the less lipophilic and synthetically more accessible bryostatin 7 closely resembles that of bryostatin 1.
Noemi Kedei; M B Kraft; W Li; A M Michalowski; M E Petersen; Y B Poudel; A Rudra; A Telek; Gary E Keck; Peter M Blumberg
Comparison of transcriptional response to phorbol ester, bryostatin 1, and bryostatin analogs in LNCaP and U937 cancer cell lines provides insight into their differential mechanism of action.
Robert L Kortum; Wenmei Li; Evan Markegard; Robert K Merrill; Michihiko Miyaji; Nandan N Nath; John M Pinski; Jeroen P Roose; Alexandre K Rouquette-Jazdanian; Lawrence E Samelson; Clayton P Alexander; Peter M Blumberg; Noemi Kedei; Amelia Wesselink; Connie L Sommers
A phospholipase C-γ1-independent, RasGRP1-ERK-dependent pathway drives lymphoproliferative disease in linker for activation of T cells-Y136F mutant mice.

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All Publications

2013: Noemi Kedei; Nancy E Lewin; Langston Lim; Poonam Mannan; Yam B Poudel; Arnab Rudra; Julia Selezneva; Peter M Blumberg; Derek C Braun; Jinqiu Chen; Thomas J Cummins; Susan H Garfield; Tamás Géczy; Madeleine R Heldman; Michelle A Herrmann; Gary E Keck
Biological profile of the less lipophilic and synthetically more accessible bryostatin 7 closely resembles that of bryostatin 1.
ACS chemical biology 2013;8(4):767-77.
2013: Noemi Kedei; M B Kraft; W Li; A M Michalowski; M E Petersen; Y B Poudel; A Rudra; A Telek; Gary E Keck; Peter M Blumberg
Comparison of transcriptional response to phorbol ester, bryostatin 1, and bryostatin analogs in LNCaP and U937 cancer cell lines provides insight into their differential mechanism of action.
Biochemical pharmacology 2013;85(3):313-24.
2013: Robert L Kortum; Wenmei Li; Evan Markegard; Robert K Merrill; Michihiko Miyaji; Nandan N Nath; John M Pinski; Jeroen P Roose; Alexandre K Rouquette-Jazdanian; Lawrence E Samelson; Clayton P Alexander; Peter M Blumberg; Noemi Kedei; Amelia Wesselink; Connie L Sommers
A phospholipase C-γ1-independent, RasGRP1-ERK-dependent pathway drives lymphoproliferative disease in linker for activation of T cells-Y136F mutant mice.
Journal of immunology (Baltimore, Md. : 1950) 2013;190(1):147-58.
2012: Myeong Seop Kim; Mi-Yeon Kim; Yong Soo Kim; Babette Y Kögel; Eun Joo Kwak; Gregor Bahrenberg; Rahul S Bhondwe; Peter M Blumberg; Seong-Hee Cho; Sun Choi; Thomas Christoph; Ian A DeAndrea-Lazarus; Robert Frank; Dong Wook Kang; Ho Shin Kim; Seul-gi Park; Young Soo Park; Larry V Pearce; Hyungchul Ryu; Klaus Schiene; Sejin Seo; Karam Son; Hannelore Stockhausen; Jeewoo Lee
2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.
Journal of medicinal chemistry 2012;55(19):8392-408.
2012: Yongsung Cho; Ho Shin Kim; Myeong Seop Kim; Jiyoun Lee; Matthew A Morgan; Vladimir A Pavlyukovets; Larry V Pearce; Jihyae Ann; Peter M Blumberg; Jeewoo Lee
The SAR analysis of TRPV1 agonists with the α-methylated B-region.
Bioorganic & medicinal chemistry letters 2012;22(16):5227-31.
2012: Gary E Keck; Noemi Kedei; Nancy E Lewin; Yam B Poudel; Arnab Rudra; Jeffrey C Stephens; Peter M Blumberg
Role of the C8 gem-dimethyl group of bryostatin 1 on its unique pattern of biological activity.
Bioorganic & medicinal chemistry letters 2012;22(12):4084-8.
2012: Rahul S Bhondwe; Peter M Blumberg; Sun Choi; Dong Wook Kang; Ho Shin Kim; Myeong Seop Kim; Seul-gi Park; Vladimir A Pavlyukovets; Larry V Pearce; Karam Son; Krystle A Lang Kuhs; Jeewoo Lee
Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism.
Bioorganic & medicinal chemistry letters 2012;22(11):3656-60.
2012: Wei Sun; Shivaji A Thorat; Attila Toth; Richard Tran; Keliang Liu; Matthew A Morgan; Vladimir A Pavlyukovets; Larry V Pearce; Christopher B Ryder; Hyungchul Ryu; Rahul S Bhondwe; Peter M Blumberg; Yongsung Cho; Dong Wook Kang; Ho Shin Kim; Myeong Seop Kim; Yong Soo Kim; Jozsef Lazar; Jeewoo Lee
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions.
Bioorganic & medicinal chemistry 2012;20(3):1310-8.
2011: Noga Gal; Susan H Garfield; Peter M Blumberg; Saïd El Kazzouli; Noemi Kedei; Sofiya Kolusheva; Nancy E Lewin; Langston Lim; Poonam Mannan; Victor E Marquez; Taiyabah A Naeem; Dina M Sigano; Andrea Telek; Raz Jelinek
N-methyl-substituted fluorescent DAG-indololactone isomers exhibit dramatic differences in membrane interactions and biological activity.
Chembiochem : a European journal of chemical biology 2011;12(15):2331-40.
2011: Noemi Kedei; Andrea Telek; Alexandra Czap; Emanuel S Lubart; Gabriella Czifra; Dazhi Yang; Jinqiu Chen; Tyler Morrison; Paul K Goldsmith; Langston Lim; Poonam Mannan; Susan H Garfield; Matthew B Kraft; Wei Li; Gary E Keck; Peter M Blumberg
The synthetic bryostatin analog Merle 23 dissects distinct mechanisms of bryostatin activity in the LNCaP human prostate cancer cell line.
Biochemical pharmacology 2011;81(11):1296-308.
2011: Noemi Kedei; Emanuel Lubart; Nancy E Lewin; Andrea Telek; Langston Lim; Poonam Mannan; Susan H Garfield; Matthew B Kraft; Gary E Keck; Sofiya Kolusheva; Raz Jelinek; Peter M Blumberg
Some phorbol esters might partially resemble bryostatin 1 in their actions on LNCaP prostate cancer cells and U937 leukemia cells.
Chembiochem : a European journal of chemical biology 2011;12(8):1242-51.
2011: Jin Hee Lee; Yoonji Lee; Hyungchul Ryu; Dong Wook Kang; Jeewoo Lee; Jozsef Lazar; Larry V Pearce; Vladimir A Pavlyukovets; Peter M Blumberg; Sun Choi
Structural insights into transient receptor potential vanilloid type 1 (TRPV1) from homology modeling, flexible docking, and mutational studies.
Journal of computer-aided molecular design 2011;25(4):317-27.
2011: Peter M Blumberg; Larry V Pearce; Jeewoo Lee
TRPV1 activation is not an all-or-none event: TRPV1 partial agonism/antagonism and its regulatory modulation.
Current topics in medicinal chemistry 2011;11(17):2151-8.
2011: Kwang Su Lim; Dong Wook Kang; Yong Soo Kim; Myeong Seop Kim; Seul-Gi Park; Sun Choi; Larry V Pearce; Peter M Blumberg; Jeewoo Lee
Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands.
Bioorganic & medicinal chemistry letters 2011;21(1):299-302.
2010: Dong Wook Kang; Yong Soo Kim; Kwang Su Lim; Myeong Seop Kim; Larry V Pearce; Vladimir A Pavlyukovets; Andy K Tao; Krystle A Lang-Kuhs; Peter M Blumberg; Jeewoo Lee
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorganic & medicinal chemistry 2010;18(22):8092-105.
2010: Dazhi Yang; Noemi Kedei; Luowei Li; Juan Tao; Julia F Velasquez; Aleksandra M Michalowski; Balázs Istvan Tóth; Rita Marincsák; Attila Varga; Tamás Bíró; Stuart H Yuspa; Peter M Blumberg
RasGRP3 contributes to formation and maintenance of the prostate cancer phenotype.
Cancer research 2010;70(20):7905-17.
2010: Or Raifman; Sofiya Kolusheva; Said El Kazzouli; Dina M Sigano; Noemi Kedei; Nancy E Lewin; Ruben Lopez-Nicolas; Ana Ortiz-Espin; Juan C Gomez-Fernandez; Peter M Blumberg; Victor E Marquez; Senena Corbalan-Garcia; Raz Jelinek
Membrane-surface anchoring of charged diacylglycerol-lactones correlates with biological activities.
Chembiochem : a European journal of chemical biology 2010;11(14):2003-9.
2010: Gary E Keck; Yam B Poudel; Arnab Rudra; Jeffrey C Stephens; Noemi Kedei; Nancy E Lewin; Megan L Peach; Peter M Blumberg
Molecular modeling, total synthesis, and biological evaluations of C9-deoxy bryostatin 1.
Angewandte Chemie (International ed. in English) 2010;49(27):4580-4.
2010: Ji-Hye Kang; Yerim Kim; Shin-Hye Won; Song-Kyu Park; Chang Woo Lee; Hwan Mook Kim; Nancy E Lewin; Nicholas A Perry; Larry V Pearce; Daniel J Lundberg; Robert J Surawski; Peter M Blumberg; Jeewoo Lee
Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents.
Bioorganic & medicinal chemistry letters 2010;20(3):1008-12.
2010: Or Raifman; Sofiya Kolusheva; Maria J Comin; Noemi Kedei; Nancy E Lewin; Peter M Blumberg; Victor E Marquez; Raz Jelinek
Membrane anchoring of diacylglycerol lactones substituted with rigid hydrophobic acyl domains correlates with biological activities.
The FEBS journal 2010;277(1):233-43.
2009: Maria Soledad Sosa; Nancy E Lewin; Sung-Hee Choi; Peter M Blumberg; Marcelo G Kazanietz
Biochemical characterization of hyperactive beta2-chimaerin mutants revealed an enhanced exposure of C1 and Rac-GAP domains.
Biochemistry 2009;48(34):8171-8.
2009: Gary E Keck; Wei Li; Matthew B Kraft; Noemi Kedei; Nancy E Lewin; Peter M Blumberg
The bryostatin 1 A-ring acetate is not the critical determinant for antagonism of phorbol ester-induced biological responses.
Organic letters 2009;11(11):2277-80.
2009: Maria J Comin; Gabriella Czifra; Noemi Kedei; Andrea Telek; Nancy E Lewin; Sofiya Kolusheva; Julia F Velasquez; Ryan Kobylarz; Raz Jelinek; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.
Journal of medicinal chemistry 2009;52(10):3274-83.
2009: Gary E Keck; Yam B Poudel; Dennie S Welch; Matthew B Kraft; Anh P Truong; Jeffrey C Stephens; Noemi Kedei; Nancy E Lewin; Peter M Blumberg
Substitution on the A-ring confers to bryopyran analogues the unique biological activity characteristic of bryostatins and distinct from that of the phorbol esters.
Organic letters 2009;11(3):593-6.
2009: József Lázár; Peter M Blumberg; Laxmikant Gharat; Neelima Khairathkar-Joshi; Arpad Szallasi
Screening TRPV1 antagonists for the treatment of pain: lessons learned over a decade.
Expert opinion on drug discovery 2009;4(2):159-80.
2009: Andrea Szegedi; Edit Páyer; Gabriella Czifra; Balázs Istvan Tóth; Emese Schmidt; László Kovács; Peter M Blumberg; Tamás Bíró
Protein kinase C isoenzymes differentially regulate the differentiation-dependent expression of adhesion molecules in human epidermal keratinocytes.
Experimental dermatology 2009;18(2):122-9.
2009: Hyun-Kyung Choi; Sun Choi; Yoonji Lee; Dong Wook Kang; Hyungchul Ryu; Han-Joo Maeng; Suk-Jae Chung; Vladimir A Pavlyukovets; Larry V Pearce; Attila Toth; Richard Tran; Yun Wang; Matthew A Morgan; Peter M Blumberg; Jeewoo Lee
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Bioorganic & medicinal chemistry 2009;17(2):690-8.
2009: Yongmei Pu; Susan H Garfield; Noemi Kedei; Peter M Blumberg
Characterization of the differential roles of the twin C1a and C1b domains of protein kinase C-delta.
The Journal of biological chemistry 2009;284(2):1302-12.
2009: Attila Tóth; Peter M Blumberg; Judit Boczán
Anandamide and the vanilloid receptor (TRPV1).
Vitamins and hormones 2009;81():389-419.
2009: Ju-Ok Lim; Mi-Kyoung Jin; Hyungchul Ryu; Dong Wook Kang; Jeewoo Lee; Larry V Pearce; Richard Tran; Attila Toth; Peter M Blumberg
Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.
European journal of medicinal chemistry 2009;44(1):322-31.
2008: Liron Philosof-Mazor; Roman Volinsky; Maria J Comin; Nancy E Lewin; Noemi Kedei; Peter M Blumberg; Victor E Marquez; Raz Jelinek
Self-assembly and lipid interactions of diacylglycerol lactone derivatives studied at the air/water interface.
Langmuir : the ACS journal of surfaces and colloids 2008;24(19):11043-52.
2008: Dehui Duan; Dina M Sigano; James A Kelley; Christopher C Lai; Nancy E Lewin; Noemi Kedei; Megan L Peach; Jeewoo Lee; Thushara P Abeyweera; Susan A Rotenberg; Hee Kim; Young Ho Kim; Saïd El Kazzouli; Jae-Uk Chung; Howard A Young; Matthew R Young; Alyson Baker; Nancy H Colburn; Adriana Haimovitz-Friedman; Jean-Philip Truman; Damon Parrish; Jeffrey Deschamps; Nicholas A Perry; Robert J Surawski; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities.
Journal of medicinal chemistry 2008;51(17):5198-220.
2008: Peter M Blumberg; Noemi Kedei; N E Lewin; D Yang; Gabriella Czifra; Yongmei Pu; M L Peach; Victor E Marquez
Wealth of opportunity - the C1 domain as a target for drug development.
Current drug targets 2008;9(8):641-52.
2008: Mónika Gönczi; Andrea Telek; Gabriella Czifra; Attila Balogh; Peter M Blumberg; Tamás Bíró; Laszlo Csernoch
Altered calcium handling following the recombinant overexpression of protein kinase C isoforms in HaCaT cells.
Experimental dermatology 2008;17(7):584-91.
2008: Stephanie Lomonaco; Sarit Kahana; Michal Blass; Yehuda Brody; Hana Okhrimenko; Cunli Xiang; Susan Finniss; Peter M Blumberg; Hae-Kyung Lee; Chaya Brodie
Phosphorylation of protein kinase Cdelta on distinct tyrosine residues induces sustained activation of Erk1/2 via down-regulation of MKP-1: role in the apoptotic effect of etoposide.
The Journal of biological chemistry 2008;283(25):17731-9.
2008: Gary E Keck; Matthew B Kraft; Anh P Truong; Wei Li; Carina C Sanchez; Noemi Kedei; Nancy E Lewin; Peter M Blumberg
Convergent assembly of highly potent analogues of bryostatin 1 via pyran annulation: bryostatin look-alikes that mimic phorbol ester function.
Journal of the American Chemical Society 2008;130(21):6660-1.
2008: Sung Hee Choi; Gabriella Czifra; Noemi Kedei; Nancy E Lewin; Jozsef Lazar; Yongmei Pu; Victor E Marquez; Peter M Blumberg
Characterization of the interaction of phorbol esters with the C1 domain of MRCK (myotonic dystrophy kinase-related Cdc42 binding kinase) alpha/beta.
The Journal of biological chemistry 2008;283(16):10543-9.
2008: Larry V Pearce; Attila Toth; HyungChul Ryu; Dong Wook Kang; Hyun-Kyung Choi; Mi-Kyung Jin; Jeewoo Lee; Peter M Blumberg
Differential modulation of agonist and antagonist structure activity relations for rat TRPV1 by cyclosporin A and other protein phosphatase inhibitors.
Naunyn-Schmiedeberg's archives of pharmacology 2008;377(2):149-57.
2008: Hyungchul Ryu; Mi-Kyung Jin; Su Yeon Kim; Hyun-Kyung Choi; Sang-Uk Kang; Dong Wook Kang; Jeewoo Lee; Larry V Pearce; Vladimir A Pavlyukovets; Matthew A Morgan; Richard Tran; Attila Toth; Daniel J Lundberg; Peter M Blumberg
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
Journal of medicinal chemistry 2008;51(1):57-67.
2007: Peter M Blumberg
Lighting a backfire to quench the blaze: a combined drug approach targeting the vanilloid receptor TRPV1.
Molecular interventions 2007;7(6):310-2.
2007: Jae-Uk Chung; Su Yeon Kim; Ju-Ok Lim; Hyun-Kyung Choi; Sang-Uk Kang; Hae-Seok Yoon; Hyungchul Ryu; Dong Wook Kang; Jeewoo Lee; Bomi Kang; Sun Choi; Attila Toth; Larry V Pearce; Vladimir A Pavlyukovets; Daniel J Lundberg; Peter M Blumberg
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Bioorganic & medicinal chemistry 2007;15(18):6043-53.
2007: Yongseok Choi; Yongmei Pu; Megan L Peach; Ji-Hye Kang; Nancy E Lewin; Dina M Sigano; Susan H Garfield; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 28. DAG-dioxolanones reveal a new additional interaction site in the C1b domain of PKC delta.
Journal of medicinal chemistry 2007;50(15):3465-81.
2007: Krishnan Malolanarasimhan; Noemi Kedei; Dina M Sigano; James A Kelley; Christopher C Lai; Nancy E Lewin; Robert J Surawski; Vladimir A Pavlyukovets; Susan H Garfield; Stephen Wincovitch; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 27. Modulation of membrane translocation of protein kinase C (PKC) isozymes alpha and delta by diacylglycerol lactones (DAG-lactones) containing rigid-rod acyl groups.
Journal of medicinal chemistry 2007;50(5):962-78.
2007: Dong Wook Kang; Hyungchul Ryu; Jeewoo Lee; Krystle A Lang; Vladimir A Pavlyukovets; Larry V Pearce; Tetsurou Ikeda; Jozsef Lazar; Peter M Blumberg
Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin.
Bioorganic & medicinal chemistry letters 2007;17(1):214-9.
2006: Yongmei Pu; Megan L Peach; Susan H Garfield; Stephen Wincovitch; Victor E Marquez; Peter M Blumberg
Effects on ligand interaction and membrane translocation of the positively charged arginine residues situated along the C1 domain binding cleft in the atypical protein kinase C isoforms.
The Journal of biological chemistry 2006;281(44):33773-88.
2006: Gabriella Czifra; Balázs Istvan Tóth; Rita Marincsák; István Juhász; Ildikó Kovács; Peter Acs; László Kovács; Peter M Blumberg; Tamás Bíró
Insulin-like growth factor-I-coupled mitogenic signaling in primary cultured human skeletal muscle cells and in C2C12 myoblasts. A central role of protein kinase Cdelta.
Cellular signalling 2006;18(9):1461-72.
2006: Sung Hee Choi; Tehila Hyman; Peter M Blumberg
Differential effect of bryostatin 1 and phorbol 12-myristate 13-acetate on HOP-92 cell proliferation is mediated by down-regulation of protein kinase Cdelta.
Cancer research 2006;66(14):7261-9.
2006: Ji-Hye Kang; Samira Benzaria; Dina M Sigano; Nancy E Lewin; Yongmei Pu; Megan L Peach; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 26. Exploring the chemical space surrounding the C1 domain of protein kinase C with DAG-lactones containing aryl groups at the sn-1 and sn-2 positions.
Journal of medicinal chemistry 2006;49(11):3185-203.
2006: Jozsef Lazar; Derek C Braun; Attila Tóth; Yun Wang; Larry V Pearce; Vladimir A Pavlyukovets; Peter M Blumberg; Susan H Garfield; Stephen Wincovitch; Hyun-Kyung Choi; Jeewoo Lee
Kinetics of penetration influence the apparent potency of vanilloids on TRPV1.
Molecular pharmacology 2006;69(4):1166-73.
2006: Jeewoo Lee; Ji-Hye Kang; Kee-Chung Han; Yerim Kim; Su Yeon Kim; Hae-Suk Youn; Inhee Mook-Jung; Hee Kim; Jee Hye Lo Han; Hee-Jin Ha; Young Ho Kim; Victor E Marquez; Nancy E Lewin; Larry V Pearce; Daniel J Lundberg; Peter M Blumberg
Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.
Journal of medicinal chemistry 2006;49(6):2028-36.
2006: Jeewoo Lee; Ju-Hyun Lee; Su Yeon Kim; Nicholas A Perry; Nancy E Lewin; Jolene A Ayres; Peter M Blumberg
2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands.
Bioorganic & medicinal chemistry 2006;14(6):2022-31.
2006: Erzsébet Lizanecz; Zsolt Bagi; Eniko T Pásztor; Zoltán Papp; István Ferenc Édes; Noemi Kedei; Peter M Blumberg; Attila Tóth
Phosphorylation-dependent desensitization by anandamide of vanilloid receptor-1 (TRPV1) function in rat skeletal muscle arterioles and in Chinese hamster ovary cells expressing TRPV1.
Molecular pharmacology 2006;69(3):1015-23.
2005: Jeewoo Lee; Sang-Uk Kang; Min-Jung Kil; Myoungyoup Shin; Ju-Ok Lim; Hyun-Kyung Choi; Mi-Kyung Jin; Su Yeon Kim; Sung-Eun Kim; Yong-Sil Lee; Kyung-Hoon Min; Young-Ho Kim; Hee-Jin Ha; Richard Tran; Jacqueline D Welter; Yun Wang; Tamas Szabo; Larry V Pearce; Daniel J Lundberg; Attila Toth; Vladimir A Pavlyukovets; Matthew A Morgan; Peter M Blumberg
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Bioorganic & medicinal chemistry letters 2005;15(18):4136-42.
2005: Jeewoo Lee; Mi-Kyung Jin; Sang-Uk Kang; Su Yeon Kim; Jiyoun Lee; Myoungyoup Shin; Jaemin Hwang; Sookhyun Cho; Yeon-Sil Choi; Hyun-Kyung Choi; Sung-Eun Kim; Young-Ger Suh; Yong-Sil Lee; Young-Ho Kim; Hee-Jin Ha; Attila Toth; Larry V Pearce; Richard Tran; Tamas Szabo; Jacqueline D Welter; Daniel J Lundberg; Yun Wang; Jozsef Lazar; Vladimir A Pavlyukovets; Matthew A Morgan; Peter M Blumberg
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Bioorganic & medicinal chemistry letters 2005;15(18):4143-50.
2005: Ji-Hye Kang; Megan L Peach; Yongmei Pu; Nancy E Lewin; Marc C Nicklaus; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
Journal of medicinal chemistry 2005;48(18):5738-48.
2005: Ya-Wei Qiang; Katie Walsh; Lei Yao; Noemi Kedei; Peter M Blumberg; Jeffrey S Rubin; John Shaughnessy; Stuart Rudikoff
Wnts induce migration and invasion of myeloma plasma cells.
Blood 2005;106(5):1786-93.
2005: Yongmei Pu; Nicholas A Perry; Dazhi Yang; Nancy E Lewin; Noemi Kedei; Derek C Braun; Sung Hee Choi; Peter M Blumberg; Susan H Garfield; James C Stone; Dehui Duan; Victor E Marquez
A novel diacylglycerol-lactone shows marked selectivity in vitro among C1 domains of protein kinase C (PKC) isoforms alpha and delta as well as selectivity for RasGRP compared with PKCalpha.
The Journal of biological chemistry 2005;280(29):27329-38.
2005: Hana Okhrimenko; Wei Lu; Cunli Xiang; Donghong Ju; Peter M Blumberg; Ruth Gomel; Gila Kazimirsky; Chaya Brodie
Roles of tyrosine phosphorylation and cleavage of protein kinase Cdelta in its protective effect against tumor necrosis factor-related apoptosis inducing ligand-induced apoptosis.
The Journal of biological chemistry 2005;280(25):23643-52.
2005: Attila Tóth; Yun Wang; Noemi Kedei; Richard Tran; Larry V Pearce; Sang-Uk Kang; Mi-Kyung Jin; Hyun-Kyung Choi; Jeewoo Lee; Peter M Blumberg
Different vanilloid agonists cause different patterns of calcium response in CHO cells heterologously expressing rat TRPV1.
Life sciences 2005;76(25):2921-32.
2005: Attila Tóth; Judit Boczán; Noemi Kedei; Erzsébet Lizanecz; Zsolt Bagi; Zoltán Papp; István Ferenc Édes; László Csiba; Peter M Blumberg
Expression and distribution of vanilloid receptor 1 (TRPV1) in the adult rat brain.
Brain research. Molecular brain research 2005;135(1-2):162-8.
2005: Derek C Braun; Susan H Garfield; Peter M Blumberg
Analysis by fluorescence resonance energy transfer of the interaction between ligands and protein kinase Cdelta in the intact cell.
The Journal of biological chemistry 2005;280(9):8164-71.
2005: Derek C Braun; Yeyu Cao; Shaomeng Wang; Susan H Garfield; Gang Min Hur; Peter M Blumberg
Role of phorbol ester localization in determining protein kinase C or RasGRP3 translocation: real-time analysis using fluorescent ligands and proteins.
Molecular cancer therapeutics 2005;4(1):141-50.
2004: Yun Wang; Noemi Kedei; Min Wang; Qiming J Wang; Anna R Huppler; Attila Toth; Richard Tran; Peter M Blumberg
Interaction between protein kinase Cmu and the vanilloid receptor type 1.
The Journal of biological chemistry 2004;279(51):53674-82.
2004: Hirokazu Tamamura; Dina M Sigano; Nancy E Lewin; Megan L Peach; Marc C Nicklaus; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C).
Journal of medicinal chemistry 2004;47(20):4858-64.
2004: Larry V Pearce; Pavel A Petukhov; Tamas Szabo; Noemi Kedei; Fero Bizik; Alan P Kozikowski; Peter M Blumberg
Evodiamine functions as an agonist for the vanilloid receptor TRPV1.
Organic & biomolecular chemistry 2004;2(16):2281-6.
2004: Ji-Hye Kang; Su Yeon Kim; Jeewoo Lee; Victor E Marquez; Nancy E Lewin; Larry V Pearce; Peter M Blumberg
Macrocyclic diacylglycerol-bis-lactones as conformationally constrained analogues of diacylglycerol-lactones. Interactions with protein kinase C.
Journal of medicinal chemistry 2004;47(16):4000-7.
2004: Ji-Hye Kang; Maqbool A Siddiqui; Dina M Sigano; Krzysztof Krajewski; Nancy E Lewin; Yongmei Pu; Peter M Blumberg; Jeewoo Lee; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 24. Asymmetric synthesis of a chiral (R)-DAG-lactone template as a versatile precursor for highly functionalized DAG-lactones.
Organic letters 2004;6(14):2413-6.
2004: Chaya Brodie; Rivka Steinhart; Gila Kazimirsky; Hadara Rubinfeld; Tehila Hyman; Jolene N Ayres; Gang Min Hur; Attila Toth; Dazhi Yang; Susan H Garfield; James C Stone; Peter M Blumberg
PKCdelta associates with and is involved in the phosphorylation of RasGRP3 in response to phorbol esters.
Molecular pharmacology 2004;66(1):76-84.
2004: Jeewoo Lee; Su Yeon Kim; Jiyoun Lee; Myungshim Kang; Min-Jung Kil; Hyun-Kyung Choi; Mi-Kyung Jin; Yun Wang; Attila Toth; Larry V Pearce; Daniel J Lundberg; Richard Tran; Peter M Blumberg
Analysis of structure-activity relationships with the N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea template for vanilloid receptor 1 antagonism.
Bioorganic & medicinal chemistry 2004;12(13):3411-20.
2004: Dehui Duan; Nancy E Lewin; Dina M Sigano; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.
Journal of medicinal chemistry 2004;47(12):3248-54.
2004: József Lázár; Tamás Szabó; Rita Marincsák; László Kovács; Peter M Blumberg; Tamás Bíró
Sensitization of recombinant vanilloid receptor-1 by various neurotrophic factors.
Life sciences 2004;75(2):153-63.
2004: Narender R Gavva; Lana Klionsky; Yusheng Qu; Licheng Shi; Rami Tamir; Steve Edenson; Tie J Zhang; Vellarkad Viswanadhan; Attila Toth; Larry V Pearce; Todd W Vanderah; Frank Porreca; Peter M Blumberg; Jack Lile; Yax Sun; Kenneth D Wild; Jean-Claude Louis; James J S Treanor
Molecular determinants of vanilloid sensitivity in TRPV1.
The Journal of biological chemistry 2004;279(19):20283-95.
2004: Jeewoo Lee; Sang-Uk Kang; Hyun-Kyung Choi; Jiyoun Lee; Ju-Ok Lim; Min-Jung Kil; Mi-Kyung Jin; Kang-Pil Kim; Jong-Hyuk Sung; Suk-Jae Chung; Hee-Jin Ha; Young-Ho Kim; Larry V Pearce; Richard Tran; Daniel J Lundberg; Yun Wang; Attila Toth; Peter M Blumberg
Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.
Bioorganic & medicinal chemistry letters 2004;14(9):2291-7.
2004: Noemi Kedei; Daniel J Lundberg; Attila Toth; Peter Welburn; Susan H Garfield; Peter M Blumberg
Characterization of the interaction of ingenol 3-angelate with protein kinase C.
Cancer research 2004;64(9):3243-55.
2004: Helga Papp; Gabriella Czifra; Eniko Bodó; József Lázár; Ildikó Kovács; Magdolna Aleksza; István Juhász; Peter Acs; Sándor Sipka; László Kovács; Peter M Blumberg; Tamás Bíró
Opposite roles of protein kinase C isoforms in proliferation, differentiation, apoptosis, and tumorigenicity of human HaCaT keratinocytes.
Cellular and molecular life sciences : CMLS 2004;61(9):1095-105.
2004: George R Pettit; Holger Hoffmann; Delbert L Herald; James McNulty; Alison Murphy; Kerianne C Higgs; Ernest Hamel; Nancy E Lewin; Larry V Pearce; Peter M Blumberg; Robin K Pettit; John C Knight
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine.
The Journal of organic chemistry 2004;69(7):2251-6.
2004: George R Pettit; Holger Hoffmann; Delbert L Herald; Peter M Blumberg; Ernest Hamel; Jean M Schmidt; Yung Chang; Robin K Pettit; Nancy E Lewin; Larry V Pearce
Antineoplastic agents. 499. Synthesis of hystatin 2 and related 1H-benzo[de][1,6]-naphthyridinium salts from aaptamine.
Journal of medicinal chemistry 2004;47(7):1775-82.
2004: Jeewoo Lee; Su Yeon Kim; Soyoung Park; Ju-Ok Lim; Ji-Min Kim; Myungshim Kang; Jiyoun Lee; Sang-Uk Kang; Hyun-Kyung Choi; Mi-Kyung Jin; Jacqueline D Welter; Tamas Szabo; Richard Tran; Larry V Pearce; Attila Toth; Peter M Blumberg
Structure-activity relationships of simplified resiniferatoxin analogues with potent VR1 agonism elucidates an active conformation of RTX for VR1 binding.
Bioorganic & medicinal chemistry 2004;12(5):1055-69.
2004: Qiming J Wang; Ganwei Lu; Walter A Schlapkohl; Axel Goerke; Christer Larsson; Mischak Harald; Peter M Blumberg; J Frederic Mushinski
The V5 domain of protein kinase C plays a critical role in determining the isoform-specific localization, translocation, and biological function of protein kinase C-delta and -epsilon.
Molecular cancer research : MCR 2004;2(2):129-40.
2004: Attila Tóth; Peter M Blumberg; Zili Chen; Alan P Kozikowski
Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population.
Molecular pharmacology 2004;65(2):282-91.
2004: Hirokazu Tamamura; Dina M Sigano; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones.
Journal of medicinal chemistry 2004;47(3):644-55.
2004: Jeewoo Lee; Sang-Uk Kang; Ju-Ok Lim; Hyun-Kyung Choi; Mi-Kyung Jin; Attila Toth; Larry V Pearce; Richard Tran; Yun Wang; Tamas Szabo; Peter M Blumberg
N-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: analysis of structure-activity relationships for the "C-Region".
Bioorganic & medicinal chemistry 2004;12(2):371-85.
2004: Jeewoo Lee; Su Yeon Kim; Ji-Hye Kang; Geza Acs; Peter Acs; Peter M Blumberg; Victor E Marquez
Conformationally constrained diacylglycerol (DAG) analogs: 4-C-hydroxyethyl-5-O-acyl-2,3-dideoxy-D-glyceropentono-1,4-lactone analogs as protein kinase C (PKC) ligands.
European journal of medicinal chemistry 2004;39(1):69-77.
2003: Reshmi A Rambaratsingh; James C Stone; Peter M Blumberg; Patricia S Lorenzo
RasGRP1 represents a novel non-protein kinase C phorbol ester signaling pathway in mouse epidermal keratinocytes.
The Journal of biological chemistry 2003;278(52):52792-801.
2003: Qiming J Wang; Tzan-Wei Fang; Dazhi Yang; Nancy E Lewin; Johan Van Lint; Victor E Marquez; Peter M Blumberg
Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase D.
Molecular pharmacology 2003;64(6):1342-8.
2003: József Lázár; Tamás Szabó; László Kovács; Peter M Blumberg; Tamás Bíró
Distinct features of recombinant rat vanilloid receptor-1 expressed in various expression systems.
Cellular and molecular life sciences : CMLS 2003;60(10):2228-40.
2003: Dean H Hamer; Sven Bocklandt; Louise McHugh; Tae-Wook Chun; Peter M Blumberg; Dina M Sigano; Victor E Marquez
Rational design of drugs that induce human immunodeficiency virus replication.
Journal of virology 2003;77(19):10227-36.
2003: Jayalakshmi Sridhar; Zhi-Liang Wei; Ireneusz Nowak; Nancy E Lewin; Jolene A Ayres; Larry V Pearce; Peter M Blumberg; Alan P Kozikowski
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Journal of medicinal chemistry 2003;46(19):4196-204.
2003: Yun Wang; Attila Toth; Richard Tran; Tamas Szabo; Jacqueline D Welter; Peter M Blumberg; Jiyoun Lee; Sang-Uk Kang; Ju-Ok Lim; Jeewoo Lee
High-affinity partial agonists of the vanilloid receptor.
Molecular pharmacology 2003;64(2):325-33.
2003: Jeewoo Lee; Jiyoun Lee; Myungshim Kang; Myoungyoup Shin; Ji-Min Kim; Sang-Uk Kang; Ju-Ok Lim; Hyun-Kyung Choi; Young-Ger Suh; Hyeung-geun Park; Uhtaek Oh; Hee-Doo Kim; Young-Ho Park; Hee-Jin Ha; Young-Ho Kim; Attila Toth; Yun Wang; Richard Tran; Larry V Pearce; Daniel J Lundberg; Peter M Blumberg
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.
Journal of medicinal chemistry 2003;46(14):3116-26.
2003: Sven Bocklandt; Peter M Blumberg; Dean H Hamer
Activation of latent HIV-1 expression by the potent anti-tumor promoter 12-deoxyphorbol 13-phenylacetate.
Antiviral research 2003;59(2):89-98.
2003: Tehila Hyman; Marjan Huizing; Peter M Blumberg; Tzipora C Falik-Zaccai; Yair Anikster; William A Gahl
Use of a cDNA microarray to determine molecular mechanisms involved in grey platelet syndrome.
British journal of haematology 2003;122(1):142-9.
2003: Yongseok Choi; Ji-Hye Kang; Nancy E Lewin; Peter M Blumberg; Jeewoo Lee; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 19. Synthesis and protein kinase C binding affinity of diacylglycerol lactones bearing an N-hydroxylamide side chain.
Journal of medicinal chemistry 2003;46(13):2790-3.
2003: Attila Tóth; Noemi Kedei; Yun Wang; Peter M Blumberg
Arachidonyl dopamine as a ligand for the vanilloid receptor VR1 of the rat.
Life sciences 2003;73(4):487-98.
2003: Ji-Hye Kang; Hye-Eun Chung; Su Yeon Kim; Yerim Kim; Jeewoo Lee; Nancy E Lewin; Larry V Pearce; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). Effect on protein kinase C (PK-C) binding by the isosteric replacement of sn-1 and sn-2 esters in DAG-lactones.
Bioorganic & medicinal chemistry 2003;11(12):2529-39.
2003: Victor E Marquez; Peter M Blumberg
Synthetic diacylglycerols (DAG) and DAG-lactones as activators of protein kinase C (PK-C).
Accounts of chemical research 2003;36(6):434-43.
2003: Dina M Sigano; Megan L Peach; Kassoum Nacro; Yongseok Choi; Nancy E Lewin; Marc C Nicklaus; Peter M Blumberg; Victor E Marquez
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).
Journal of medicinal chemistry 2003;46(9):1571-9.
2003: Amy S Clark; Kip A West; Peter M Blumberg; Phillip A Dennis
Altered protein kinase C (PKC) isoforms in non-small cell lung cancer cells: PKCdelta promotes cellular survival and chemotherapeutic resistance.
Cancer research 2003;63(4):780-6.
2003: Alan P Kozikowski; Ireneusz Nowak; Pavel A Petukhov; René Etcheberrigaray; Ali Mohamed; Mathew Tan; Nancy E Lewin; Henry Hennings; Larry L Pearce; Peter M Blumberg
New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha.
Journal of medicinal chemistry 2003;46(3):364-73.
2003: Nancy E Lewin; Peter M Blumberg
[3H]Phorbol 12,13-dibutyrate binding assay for protein kinase C and related proteins.
Methods in molecular biology (Clifton, N.J.) 2003;233():129-56.
2003: Chaya Brodie; Peter M Blumberg
Regulation of cell apoptosis by protein kinase c delta.
Apoptosis : an international journal on programmed cell death 2003;8(1):19-27.
2002: Yun Wang; Tamas Szabo; Jacqueline D Welter; Attila Toth; Richard Tran; Jiyoun Lee; Sang-Uk Kang; Young-Ger Suh; Peter M Blumberg; Jeewoo Lee
High affinity antagonists of the vanilloid receptor.
Molecular pharmacology 2002;62(4):947-56.
2002: George R Pettit; Sylvie Ducki; Rui Tan; Roberta S Gardella; James B McMahon; Michael R Boyd; George R Pettit; Peter M Blumberg; Nancy E Lewin; Dennis L Doubek; Larry P Tackett; Michael D Williams
Isolation and structure of pedilstatin from a republic of maldives Pedilanthus sp.
Journal of natural products 2002;65(9):1262-5.
2002: Vincenzo Di Marzo; Peter M Blumberg; Arpad Szallasi
Endovanilloid signaling in pain.
Current opinion in neurobiology 2002;12(4):372-9.
2002: Avi Zrachya; Melamed Dobroslav; Michal Blass; Gila Kazimirsky; Ilana Kronfeld; Peter M Blumberg; David Kobiler; Shlomo Lustig; Chaya Brodie
Infection of glioma cells with Sindbis virus induces selective activation and tyrosine phosphorylation of protein kinase C delta. Implications for Sindbis virus-induced apoptosis.
The Journal of biological chemistry 2002;277(26):23693-701.
2002: Zhi-Liang Wei; Sukumar Sakamuri; Pavel A Petukhov; Clifford George; Nancy E Lewin; Peter M Blumberg; Alan P Kozikowski
Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators.
Organic letters 2002;4(13):2169-72.
2002: Attila Tóth; Noemi Kedei; Tamás Szabó; Yun Wang; Peter M Blumberg
Thapsigargin binds to and inhibits the cloned vanilloid receptor-1.
Biochemical and biophysical research communications 2002;293(2):777-82.
2002: Elizabeth Joseloff; Christophe Cataisson; Heather Aamodt; Henrietta Ocheni; Peter M Blumberg; Alan J Kraker; Stuart H Yuspa
Src family kinases phosphorylate protein kinase C delta on tyrosine residues and modify the neoplastic phenotype of skin keratinocytes.
The Journal of biological chemistry 2002;277(14):12318-23.
2002: Jeewoo Lee; Jiyoun Lee; Myung-Sim Kang; Kang-Pil Kim; Suk-Jae Chung; Peter M Blumberg; Jung-Bum Yi; Young Ho Park
Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics.
Bioorganic & medicinal chemistry 2002;10(4):1171-9.
2002: Suo-Bao Rong; Istvan J Enyedy; Lixin Qiao; Lianyun Zhao; Dawei Ma; Larry L Pearce; Patricia S Lorenzo; James C Stone; Peter M Blumberg; Shaomeng Wang; Alan P Kozikowski
Structural basis of RasGRP binding to high-affinity PKC ligands.
Journal of medicinal chemistry 2002;45(4):853-60.
2002: Tamas Szabo; Tamas Biro; Adamar F Gonzalez; Miklós Palkovits; Peter M Blumberg
Pharmacological characterization of vanilloid receptor located in the brain.
Brain research. Molecular brain research 2002;98(1-2):51-7.
2002: Maria Laura Garcia-Bermejo; Federico Coluccio Leskow; Teruhiko Fujii; Qiming Wang; Peter M Blumberg; Motoi Ohba; Toshio Kuroki; Kee-Chung Han; Jeewoo Lee; Victor E Marquez; Marcelo G Kazanietz
Diacylglycerol (DAG)-lactones, a new class of protein kinase C (PKC) agonists, induce apoptosis in LNCaP prostate cancer cells by selective activation of PKCalpha.
The Journal of biological chemistry 2002;277(1):645-55.
2002: Michal Blass; Ilana Kronfeld; Gila Kazimirsky; Peter M Blumberg; Chaya Brodie
Tyrosine phosphorylation of protein kinase Cdelta is essential for its apoptotic effect in response to etoposide.
Molecular and cellular biology 2002;22(1):182-95.
2001: Jeewoo Lee; Kee-Chung Han; Ji-Hye Kang; L L Pearce; Nancy E Lewin; S Yan; Samira Benzaria; Marc C Nicklaus; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity.
Journal of medicinal chemistry 2001;44(25):4309-12.
2001: Lei Shao; Nancy E Lewin; Patricia S Lorenzo; Zengjian Hu; Istvan J Enyedy; Susan H Garfield; James C Stone; F J Marner; Peter M Blumberg; Shaomeng Wang
Iridals are a novel class of ligands for phorbol ester receptors with modest selectivity for the RasGRP receptor subfamily.
Journal of medicinal chemistry 2001;44(23):3872-80.
2001: Noemi Kedei; Tamas Szabo; Jack Lile; James J S Treanor; Zoltan Olah; Michael Iadarola; Peter M Blumberg
Analysis of the native quaternary structure of vanilloid receptor 1.
The Journal of biological chemistry 2001;276(30):28613-9.
2001: Jeewoo Lee; J Lee; Tamas Szabo; A F Gonzalez; Jacqueline D Welter; Peter M Blumberg
N-(3-acyloxy-2-benzylpropyl)-N'-dihydroxytetrahydrobenzazepine and tetrahydroisoquinoline thiourea analogues as vanilloid receptor ligands.
Bioorganic & medicinal chemistry 2001;9(7):1713-20.
2001: Kassoum Nacro; Dina M Sigano; S Yan; Marc C Nicklaus; L L Pearce; Nancy E Lewin; Susan H Garfield; Peter M Blumberg; Victor E Marquez
An optimized protein kinase C activating diacylglycerol combining high binding affinity (Ki) with reduced lipophilicity (log P).
Journal of medicinal chemistry 2001;44(12):1892-904.
2001: R Mandil; E Ashkenazi; Michal Blass; Ilana Kronfeld; Gila Kazimirsky; Guy Rosenthal; Felix Umansky; Patricia S Lorenzo; Peter M Blumberg; Chaya Brodie
Protein kinase Calpha and protein kinase Cdelta play opposite roles in the proliferation and apoptosis of glioma cells.
Cancer research 2001;61(11):4612-9.
2001: Qiming J Wang; Tzan-Wei Fang; Kassoum Nacro; Victor E Marquez; Shulin Wang; Peter M Blumberg
Role of hydrophobic residues in the C1b domain of protein kinase C delta on ligand and phospholipid interactions.
The Journal of biological chemistry 2001;276(22):19580-7.
2001: Y Pak; Istvan J Enyedy; Judith Varady; J W Kung; Patricia S Lorenzo; Peter M Blumberg; Shaomeng Wang
Structural basis of binding of high-affinity ligands to protein kinase C: prediction of the binding modes through a new molecular dynamics method and evaluation by site-directed mutagenesis.
Journal of medicinal chemistry 2001;44(11):1690-701.
2001: Zoltan Olah; Tamas Szabo; Laszlo Karai; C Hough; R D Fields; Robert M Caudle; Peter M Blumberg; Michael Iadarola
Ligand-induced dynamic membrane changes and cell deletion conferred by vanilloid receptor 1.
The Journal of biological chemistry 2001;276(14):11021-30.
2001: Jeewoo Lee; Kee-Chung Han; S Y Lee; Su Yeon Kim; Ji-Hye Kang; Nancy E Lewin; L S Best; Peter M Blumberg; Victor E Marquez
5-acyloxy-5-hydroxymethyltetrahydro-2-furancarboxylate as a novel template for protein kinase C (PKC) binding.
Farmaco (Società chimica italiana : 1989) 2001;56(3):203-10.
2001: Patricia S Lorenzo; J W Kung; Drell A Bottorff; Susan H Garfield; James C Stone; Peter M Blumberg
Phorbol esters modulate the Ras exchange factor RasGRP3.
Cancer research 2001;61(3):943-9.
2001: Jeewoo Lee; J Lee; Jeongmin Kim; Su Yeon Kim; Moon Woo Chun; H Cho; S W Hwang; U Oh; Y H Park; Victor E Marquez; M Beheshti; Tamas Szabo; Peter M Blumberg
N-(3-Acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesics.
Bioorganic & medicinal chemistry 2001;9(1):19-32.
2000: Ilana Kronfeld; Gila Kazimirsky; Patricia S Lorenzo; Susan H Garfield; Peter M Blumberg; Chaya Brodie
Phosphorylation of protein kinase Cdelta on distinct tyrosine residues regulates specific cellular functions.
The Journal of biological chemistry 2000;275(45):35491-8.
2000: H Tamamura; B Bienfait; Kassoum Nacro; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.
Journal of medicinal chemistry 2000;43(17):3209-17.
2000: JO Ebinu; Stacey L Stang; Christine Teixeira; Drell A Bottorff; Jonathan W Hooton; Peter M Blumberg; M Barry; R C Bleakley; Hanne L Ostergaard; James C Stone
RasGRP links T-cell receptor signaling to Ras.
Blood 2000;95(10):3199-203.
2000: Peter Acs; M Beheshti; Z Szállási; Luowei Li; Stuart H Yuspa; Peter M Blumberg
Effect of a tyrosine 155 to phenylalanine mutation of protein kinase cdelta on the proliferative and tumorigenic properties of NIH 3T3 fibroblasts.
Carcinogenesis 2000;21(5):887-91.
2000: Patricia S Lorenzo; M Beheshti; George R Pettit; James C Stone; Peter M Blumberg
The guanine nucleotide exchange factor RasGRP is a high -affinity target for diacylglycerol and phorbol esters.
Molecular pharmacology 2000;57(5):840-6.
2000: Qiming J Wang; Tzan-Wei Fang; D Fenick; Susan H Garfield; B Bienfait; Victor E Marquez; Peter M Blumberg
The lipophilicity of phorbol esters as a critical factor in determining the pattern of translocation of protein kinase C delta fused to green fluorescent protein.
The Journal of biological chemistry 2000;275(16):12136-46.
2000: Kassoum Nacro; B Bienfait; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones.
Bioorganic & medicinal chemistry letters 2000;10(7):653-5.
2000: Eva Mezey; Z E Tóth; Daniel N Cortright; M K Arzubi; James E Krause; R Elde; A Guo; Peter M Blumberg; Arpad Szallasi
Distribution of mRNA for vanilloid receptor subtype 1 (VR1), and VR1-like immunoreactivity, in the central nervous system of the rat and human.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(7):3655-60.
2000: Kassoum Nacro; B Bienfait; Jeewoo Lee; Kee-Chung Han; Ji-Hye Kang; Samira Benzaria; Nancy E Lewin; Dipak Bhattacharyya; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?
Journal of medicinal chemistry 2000;43(5):921-44.
1999: Qiming J Wang; Dipak Bhattacharyya; Susan H Garfield; Kassoum Nacro; Victor E Marquez; Peter M Blumberg
Differential localization of protein kinase C delta by phorbol esters and related compounds using a fusion protein with green fluorescent protein.
The Journal of biological chemistry 1999;274(52):37233-9.
1999: Patricia S Lorenzo; K Bögi; K M Hughes; M Beheshti; Dipak Bhattacharyya; Susan H Garfield; George R Pettit; Peter M Blumberg
Differential roles of the tandem C1 domains of protein kinase C delta in the biphasic down-regulation induced by bryostatin 1.
Cancer research 1999;59(24):6137-44.
1999: Luowei Li; Patricia S Lorenzo; K Bogi; Peter M Blumberg; Stuart H Yuspa
Protein kinase Cdelta targets mitochondria, alters mitochondrial membrane potential, and induces apoptosis in normal and neoplastic keratinocytes when overexpressed by an adenoviral vector.
Molecular and cellular biology 1999;19(12):8547-58.
1999: Jeewoo Lee; S U Park; J Y Kim; J K Kim; J Lee; U Oh; Victor E Marquez; M Beheshti; Q J Wang; S Modarres; Peter M Blumberg
3-Acyloxy-2-phenalkylpropyl amides and esters of homovanillic acid as novel vanilloid receptor agonists.
Bioorganic & medicinal chemistry letters 1999;9(20):2909-14.
1999: Maria Jose Caloca; M L Garcia-Bermejo; Peter M Blumberg; Nancy E Lewin; Elisabeth Kremmer; H Mischak; Shulin Wang; Kassoum Nacro; B Bienfait; Victor E Marquez; Marcelo G Kazanietz
beta2-chimaerin is a novel target for diacylglycerol: binding properties and changes in subcellular localization mediated by ligand binding to its C1 domain.
Proceedings of the National Academy of Sciences of the United States of America 1999;96(21):11854-9.
1999: Jeewoo Lee; Ji-Hye Kang; S Y Lee; Kee-Chung Han; C M Torres; Dipak Bhattacharyya; Peter M Blumberg; Victor E Marquez
Protein kinase C ligands based on tetrahydrofuran templates containing a new set of phorbol ester pharmacophores.
Journal of medicinal chemistry 1999;42(20):4129-39.
1999: Shaomeng Wang; M Liu; Nancy E Lewin; Patricia S Lorenzo; D Bhattacharrya; Lixin Qiao; Alan P Kozikowski; Peter M Blumberg
Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations.
Journal of medicinal chemistry 1999;42(18):3436-46.
1999: Tamas Szabo; Zoltan Olah; Michael Iadarola; Peter M Blumberg
Epidural resiniferatoxin induced prolonged regional analgesia to pain.
Brain research 1999;840(1-2):92-8.
1999: Arpad Szallasi; Tamás Szabó; Tamás Bíró; S Modarres; Peter M Blumberg; James E Krause; Daniel N Cortright; Giovanni Appendino
Resiniferatoxin-type phorboid vanilloids display capsaicin-like selectivity at native vanilloid receptors on rat DRG neurons and at the cloned vanilloid receptor VR1.
British journal of pharmacology 1999;128(2):428-34.
1999: Arpad Szallasi; Peter M Blumberg; L L Annicelli; James E Krause; Daniel N Cortright
The cloned rat vanilloid receptor VR1 mediates both R-type binding and C-type calcium response in dorsal root ganglion neurons.
Molecular pharmacology 1999;56(3):581-7.
1999: K Bögi; Patricia S Lorenzo; Peter Acs; Z Szállási; G S Wagner; Peter M Blumberg
Comparison of the roles of the C1a and C1b domains of protein kinase C alpha in ligand induced translocation in NIH 3T3 cells.
FEBS letters 1999;456(1):27-30.
1999: Arpad Szallasi; Peter M Blumberg
Vanilloid (Capsaicin) receptors and mechanisms.
Pharmacological reviews 1999;51(2):159-212.
1999: Victor E Marquez; Kassoum Nacro; Samira Benzaria; Jeewoo Lee; R Sharma; K Teng; GW Milne; B Bienfait; Shulin Wang; Nancy E Lewin; Peter M Blumberg
The transition from a pharmacophore-guided approach to a receptor-guided approach in the design of potent protein kinase C ligands.
Pharmacology & therapeutics 1999;82(2-3):251-61.
1999: Larisa Y Romanova; I A Alexandrov; Mikhail V Blagosklonny; R P Nordan; Susan H Garfield; Peter Acs; P Nguyen; Jane Trepel; Peter M Blumberg; J Frederic Mushinski
Regulation of actin cytoskeleton in lymphocytes: PKC-delta disrupts IL-3-induced membrane ruffles downstream of Rac1.
Journal of cellular physiology 1999;179(2):157-69.
1999: Arpad Szallasi; Tamás Bíró; Tamás Szabó; S Modarres; M Petersen; A Klusch; Peter M Blumberg; James E Krause; Olov Sterner
A non-pungent triprenyl phenol of fungal origin, scutigeral, stimulates rat dorsal root ganglion neurons via interaction at vanilloid receptors.
British journal of pharmacology 1999;126(6):1351-8.
1999: Chaya Brodie; K Bogi; Peter Acs; Philip Lazarovici; Gyorgy Petrovics; Wayne B Anderson; Peter M Blumberg
Protein kinase C-epsilon plays a role in neurite outgrowth in response to epidermal growth factor and nerve growth factor in PC12 cells.
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research 1999;10(3):183-91.
1998: Samira Benzaria; B Bienfait; Kassoum Nacro; Shulin Wang; Nancy E Lewin; M Beheshti; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol (DAG). 15. The indispensable role of the sn-1 and sn-2 carbonyls in the binding of DAG-lactones to protein kinase C (PK-C).
Bioorganic & medicinal chemistry letters 1998;8(23):3403-8.
1998: Chaya Brodie; K Bogi; Peter Acs; Patricia S Lorenzo; L Baskin; Peter M Blumberg
Protein kinase C delta (PKCdelta) inhibits the expression of glutamine synthetase in glial cells via the PKCdelta regulatory domain and its tyrosine phosphorylation.
The Journal of biological chemistry 1998;273(46):30713-8.
1998: Arpad Szallasi; Tamás Bíró; S Modarres; L Garlaschelli; M Petersen; A Klusch; G Vidari; M Jonassohn; S De Rosa; Olov Sterner; Peter M Blumberg; James E Krause
Dialdehyde sesquiterpenes and other terpenoids as vanilloids.
European journal of pharmacology 1998;356(1):81-9.
1998: Victor E Marquez; R Sharma; Shulin Wang; Nancy E Lewin; Peter M Blumberg; I S Kim; Jeewoo Lee
Conformationally constrained analogues of diacylglycerol (DAG). 14. Dissection of the roles of the sn-1 and sn-2 carbonyls in DAG mimetics by isopharmacophore replacement.
Bioorganic & medicinal chemistry letters 1998;8(13):1757-62.
1998: Chaya Brodie; Peter M Blumberg; Kenneth Alan Jacobson
Activation of the A2A adenosine receptor inhibits nitric oxide production in glial cells.
FEBS letters 1998;429(2):139-42.
1998: Chaya Brodie; I Kuperstein; Peter Acs; Peter M Blumberg
Differential role of specific PKC isoforms in the proliferation of glial cells and the expression of the astrocytic markers GFAP and glutamine synthetase.
Brain research. Molecular brain research 1998;56(1-2):108-17.
1998: Tamás Bíró; Chaya Brodie; S Modarres; Nancy E Lewin; Peter Acs; Peter M Blumberg
Specific vanilloid responses in C6 rat glioma cells.
Brain research. Molecular brain research 1998;56(1-2):89-98.
1998: K Bögi; Patricia S Lorenzo; Z Szállási; Peter Acs; G S Wagner; Peter M Blumberg
Differential selectivity of ligands for the C1a and C1b phorbol ester binding domains of protein kinase Cdelta: possible correlation with tumor-promoting activity.
Cancer research 1998;58(7):1423-8.
1998: Tamás Bíró; Marcus Maurer; S Modarres; Nancy E Lewin; Chaya Brodie; Geza Acs; Peter Acs; R Paus; Peter M Blumberg
Characterization of functional vanilloid receptors expressed by mast cells.
Blood 1998;91(4):1332-40.
1998: Qiming J Wang; Peter Acs; JoAnne Goodnight; Peter M Blumberg; Mischak Harald; J Frederic Mushinski
The catalytic domain of PKC-epsilon, in reciprocal PKC-delta and -epsilon chimeras, is responsible for conferring tumorgenicity to NIH3T3 cells, whereas both regulatory and catalytic domains of PKC-epsilon contribute to in vitro transformation.
Oncogene 1998;16(1):53-60.
1997: Patricia S Lorenzo; K Bögi; Peter Acs; George R Pettit; Peter M Blumberg
The catalytic domain of protein kinase Cdelta confers protection from down-regulation induced by bryostatin 1.
The Journal of biological chemistry 1997;272(52):33338-43.
1997: Peter Acs; Qiming J Wang; K Bögi; A M Marquez; Patricia S Lorenzo; Tamás Bíró; Z Szállási; J Frederic Mushinski; Peter M Blumberg
Both the catalytic and regulatory domains of protein kinase C chimeras modulate the proliferative properties of NIH 3T3 cells.
The Journal of biological chemistry 1997;272(45):28793-9.
1997: Elana Appel; O Kolman; Gila Kazimirsky; Peter M Blumberg; Chaya Brodie
Regulation of GDNF expression in cultured astrocytes by inflammatory stimuli.
Neuroreport 1997;8(15):3309-12.
1997: Maria Jose Caloca; N Fernandez; Nancy E Lewin; D Ching; rama modali; Peter M Blumberg; Marcelo G Kazanietz
Beta2-chimaerin is a high affinity receptor for the phorbol ester tumor promoters.
The Journal of biological chemistry 1997;272(42):26488-96.
1997: Peter Acs; K Bögi; Patricia S Lorenzo; A M Marquez; Tamás Bíró; Z Szállási; Peter M Blumberg
The catalytic domain of protein kinase C chimeras modulates the affinity and targeting of phorbol ester-induced translocation.
The Journal of biological chemistry 1997;272(35):22148-53.
1997: Tamas Biro; Geza Acs; Peter Acs; S Modarres; Peter M Blumberg
Recent advances in understanding of vanilloid receptors: a therapeutic target for treatment of pain and inflammation in skin.
The journal of investigative dermatology. Symposium proceedings / the Society for Investigative Dermatology, Inc. [and] European Society for Dermatological Research 1997;2(1):56-60.
1997: Geza Acs; Tamas Biro; Peter Acs; S Modarres; Peter M Blumberg
Differential activation and desensitization of sensory neurons by resiniferatoxin.
The Journal of neuroscience : the official journal of the Society for Neuroscience 1997;17(14):5622-8.
1997: Alan P Kozikowski; Shaomeng Wang; Dawei Ma; J Yao; S Ahmad; R I Glazer; K Bogi; Peter Acs; S Modarres; Nancy E Lewin; Peter M Blumberg
Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity.
Journal of medicinal chemistry 1997;40(9):1316-26.
1997: Qiming J Wang; Peter Acs; JoAnne Goodnight; Thomas Giese; Peter M Blumberg; Mischak Harald; J Frederic Mushinski
The catalytic domain of protein kinase C-delta in reciprocal delta and epsilon chimeras mediates phorbol ester-induced macrophage differentiation of mouse promyelocytes.
The Journal of biological chemistry 1997;272(1):76-82.
1996: J Lee; Nancy E Lewin; Peter Acs; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 13. Protein kinase C ligands based on templates derived from 2,3-dideoxy-L-erythro(threo)-hexono-1,4-lactone and 2-deoxyapiolactone.
Journal of medicinal chemistry 1996;39(25):4912-9.
1996: Arpad Szallasi; M Jonassohn; G Acs; Tamás Bíró; Peter Acs; Peter M Blumberg; Olov Sterner
The stimulation of capsaicin-sensitive neurones in a vanilloid receptor-mediated fashion by pungent terpenoids possessing an unsaturated 1,4-dialdehyde moiety.
British journal of pharmacology 1996;119(2):283-90.
1996: Z Szallasi; K Bogi; S Gohari; T Biro; Peter Acs; Peter M Blumberg
Non-equivalent roles for the first and second zinc fingers of protein kinase Cdelta. Effect of their mutation on phorbol ester-induced translocation in NIH 3T3 cells.
The Journal of biological chemistry 1996;271(31):18299-301.
1996: J Lee; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Synthesis of bis-gamma-butyrolactones containing conformationally constrained (S)- and (R)-diacylglycerol structures.
Bioorganic & medicinal chemistry 1996;4(8):1299-305.
1996: Shulin Wang; Marcelo G Kazanietz; Peter M Blumberg; Victor E Marquez; GW Milne
Molecular modeling and site-directed mutagenesis studies of a phorbol ester-binding site in protein kinase C.
Journal of medicinal chemistry 1996;39(13):2541-53.
1996: T Farkas-Szallasi; G J Bennett; Peter M Blumberg; Tomas Hökfelt; Jan M Lundberg; Arpad Szallasi
Vanilloid receptor loss is independent of the messenger plasticity that follows systemic resiniferatoxin administration.
Brain research 1996;719(1-2):213-8.
1996: Z Szallasi; L Du; R Levine; Nancy E Lewin; P N Nguyen; M D Williams; George R Pettit; Peter M Blumberg
The bryostatins inhibit growth of B16/F10 melanoma cells in vitro through a protein kinase C-independent mechanism: dissociation of activities using 26-epi-bryostatin 1.
Cancer research 1996;56(9):2105-11.
1996: Arpad Szallasi; G Acs; G Cravotto; Peter M Blumberg; Jan M Lundberg; Giovanni Appendino
A novel agonist, phorbol 12-phenylacetate 13-acetate 20-homovanillate, abolishes positive cooperativity of binding by the vanilloid receptor.
European journal of pharmacology 1996;299(1-3):221-8.
1996: Arpad Szallasi; S Nilsson; Peter M Blumberg; Tomas Hökfelt; Jan M Lundberg
Binding of neuroleptic drugs (trifluoperazine and rimcazole) to vanilloid receptors in porcine dorsal horn.
European journal of pharmacology 1996;298(3):321-7.
1996: J Lee; R Sharma; Shulin Wang; GW Milne; Nancy E Lewin; Z Szallasi; Peter M Blumberg; C George; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 12. Ultrapotent protein kinase C ligands based on a chiral 4,4-disubstituted heptono-1,4-lactone template.
Journal of medicinal chemistry 1996;39(1):36-45.
1996: J Lee; Shulin Wang; GW Milne; R Sharma; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 11. Ultrapotent protein kinase C ligands based on a chiral 5-disubstituted tetrahydro-2-furanone template.
Journal of medicinal chemistry 1996;39(1):29-35.
1996: R Sharma; J Lee; Shulin Wang; GW Milne; Nancy E Lewin; Peter M Blumberg; Victor E Marquez
Conformationally constrained analogues of diacylglycerol. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template.
Journal of medicinal chemistry 1996;39(1):19-28.
1996: G Acs; Miklós Palkovits; Peter M Blumberg
Specific binding of [3H]resiniferatoxin by human and rat preoptic area, locus ceruleus, medial hypothalamus, reticular formation and ventral thalamus membrane preparations.
Life sciences 1996;59(22):1899-908.
1996: G Acs; J Lee; V E Marquez; Peter M Blumberg
Distinct structure-activity relations for stimulation of 45Ca uptake and for high affinity binding in cultured rat dorsal root ganglion neurons and dorsal root ganglion membranes.
Brain research. Molecular brain research 1996;35(1-2):173-82.
1995: Arpad Szallasi; S Nilsson; T Farkas-Szallasi; Peter M Blumberg; Tomas Hökfelt; Jan M Lundberg
Vanilloid (capsaicin) receptors in the rat: distribution in the brain, regional differences in the spinal cord, axonal transport to the periphery, and depletion by systemic vanilloid treatment.
Brain research 1995;703(1-2):175-83.
1995: Mitchell F Denning; Marcelo G Kazanietz; Peter M Blumberg; Stuart H Yuspa
Cholesterol sulfate activates multiple protein kinase C isoenzymes and induces granular cell differentiation in cultured murine keratinocytes.
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research 1995;6(12):1619-26.
1995: Peter Acs; Z Szallasi; Marcelo G Kazanietz; Peter M Blumberg
Differential activation of PKC isozymes by 14-3-3 zeta protein.
Biochemical and biophysical research communications 1995;216(1):103-9.
1995: Hana Haleem-Smith; E Y Chang; Z Szallasi; Peter M Blumberg; Juan Rivera
Tyrosine phosphorylation of protein kinase C-delta in response to the activation of the high-affinity receptor for immunoglobulin E modifies its substrate recognition.
Proceedings of the National Academy of Sciences of the United States of America 1995;92(20):9112-6.
1995: Z Szallasi; Mitchell F Denning; E Y Chang; Juan Rivera; Stuart H Yuspa; C Lehel; Zoltan Olah; Wayne B Anderson; Peter M Blumberg
Development of a rapid approach to identification of tyrosine phosphorylation sites: application to PKC delta phosphorylated upon activation of the high affinity receptor for IgE in rat basophilic leukemia cells.
Biochemical and biophysical research communications 1995;214(3):888-94.
1995: Marcelo G Kazanietz; Shulin Wang; GW Milne; Nancy E Lewin; H L Liu; Peter M Blumberg
Residues in the second cysteine-rich region of protein kinase C delta relevant to phorbol ester binding as revealed by site-directed mutagenesis.
The Journal of biological chemistry 1995;270(37):21852-9.
1995: G Acs; Miklós Palkovits; Peter M Blumberg
Trifluoperazine modulates [3H]resiniferatoxin binding by human and rat vanilloid (capsaicin) receptors and affects 45Ca uptake by adult rat dorsal root ganglion neurones.
The Journal of pharmacology and experimental therapeutics 1995;274(3):1090-8.
1995: C Lehel; Z Oláh; G Jakab; Z Szállási; Gyorgy Petrovics; G Harta; Peter M Blumberg; Wayne B Anderson
Protein kinase C epsilon subcellular localization domains and proteolytic degradation sites. A model for protein kinase C conformational changes.
The Journal of biological chemistry 1995;270(33):19651-8.
1995: Geza Acs; J Lee; Victor E Marquez; Shulin Wang; GW Milne; L Du; Nancy E Lewin; Peter M Blumberg
Resiniferatoxin-amide and analogues as ligands for protein kinase C and vanilloid receptors and determination of their biological activities as vanilloids.
Journal of neurochemistry 1995;65(1):301-18.
1995: Marcelo G Kazanietz; Joseph J Barchi; James G. Omichinski; Peter M Blumberg
Low affinity binding of phorbol esters to protein kinase C and its recombinant cysteine-rich region in the absence of phospholipids.
The Journal of biological chemistry 1995;270(24):14679-84.
1995: Marcelo G Kazanietz; Nancy E Lewin; J D Bruns; Peter M Blumberg
Characterization of the cysteine-rich region of the Caenorhabditis elegans protein Unc-13 as a high affinity phorbol ester receptor. Analysis of ligand-binding interactions, lipid cofactor requirements, and inhibitor sensitivity.
The Journal of biological chemistry 1995;270(18):10777-83.
1995: Arpad Szallasi; Peter M Blumberg; Jan M Lundberg
Proton inhibition of [3H]resiniferatoxin binding to vanilloid (capsaicin) receptors in rat spinal cord.
European journal of pharmacology 1995;289(2):181-7.
1995: Z Szallasi; K Kosa; C B Smith; Andrzej Dlugosz; E K Williams; Stuart H Yuspa; Peter M Blumberg
Differential regulation by anti-tumor-promoting 12-deoxyphorbol-13-phenylacetate reveals distinct roles of the classical and novel protein kinase C isozymes in biological responses of primary mouse keratinocytes.
Molecular pharmacology 1995;47(2):258-65.
1995: Mitchell F Denning; Andrzej Dlugosz; E K Williams; Z Szallasi; Peter M Blumberg; Stuart H Yuspa
Specific protein kinase C isozymes mediate the induction of keratinocyte differentiation markers by calcium.
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research 1995;6(2):149-57.
1995: Peter M Blumberg; Geza Acs; Peter Acs; L B Areces; Marcelo G Kazanietz; Nancy E Lewin; Z Szallasi
Protein kinase C in cell signaling: strategies for the development of selective inhibitors.
Agents and actions. Supplements 1995;47():87-100.
1994: Shulin Wang; Daniel W Zaharevitz; R Sharma; Victor E Marquez; Nancy E Lewin; L Du; Peter M Blumberg; GW Milne
The discovery of novel, structurally diverse protein kinase C agonists through computer 3D-database pharmacophore search. Molecular modeling studies.
Journal of medicinal chemistry 1994;37(26):4479-89.
1994: Z Szallasi; C B Smith; Peter M Blumberg
Dissociation of phorbol esters leads to immediate redistribution to the cytosol of protein kinases C alpha and C delta in mouse keratinocytes.
The Journal of biological chemistry 1994;269(44):27159-62.
1994: Z Szallasi; Mitchell F Denning; C B Smith; Andrzej Dlugosz; Stuart H Yuspa; George R Pettit; Peter M Blumberg
Bryostatin 1 protects protein kinase C-delta from down-regulation in mouse keratinocytes in parallel with its inhibition of phorbol ester-induced differentiation.
Molecular pharmacology 1994;46(5):840-50.
1994: Arpad Szallasi; Peter M Blumberg; S Nilsson; Tomas Hökfelt; Jan M Lundberg
Visualization by [3H]resiniferatoxin autoradiography of capsaicin-sensitive neurons in the rat, pig and man.
European journal of pharmacology 1994;264(2):217-21.
1994: Marcelo G Kazanietz; Nancy E Lewin; F Gao; George R Pettit; Peter M Blumberg
Binding of [26-3H]bryostatin 1 and analogs to calcium-dependent and calcium-independent protein kinase C isozymes.
Molecular pharmacology 1994;46(2):374-9.
1994: L B Areces; Marcelo G Kazanietz; Peter M Blumberg
Close similarity of baculovirus-expressed n-chimaerin and protein kinase C alpha as phorbol ester receptors.
The Journal of biological chemistry 1994;269(30):19553-8.
1994: C M Seynaeve; Marcelo G Kazanietz; Peter M Blumberg; Edward A Sausville; P J Worland
Differential inhibition of protein kinase C isozymes by UCN-01, a staurosporine analogue.
Molecular pharmacology 1994;45(6):1207-14.
1994: G Acs; Miklós Palkovits; Peter M Blumberg
[3H]resiniferatoxin binding by the human vanilloid (capsaicin) receptor.
Brain research. Molecular brain research 1994;23(3):185-90.
1994: Shulin Wang; GW Milne; Marc C Nicklaus; Victor E Marquez; J Lee; Peter M Blumberg
Protein kinase C. Modeling of the binding site and prediction of binding constants.
Journal of medicinal chemistry 1994;37(9):1326-38.
1994: Marcelo G Kazanietz; X R Bustelo; M Barbacid; Walter Kolch; Mischak Harald; G Wong; George R Pettit; J D Bruns; Peter M Blumberg
Zinc finger domains and phorbol ester pharmacophore. Analysis of binding to mutated form of protein kinase C zeta and the vav and c-raf proto-oncogene products.
The Journal of biological chemistry 1994;269(15):11590-4.
1994: Z Szallasi; C B Smith; George R Pettit; Peter M Blumberg
Differential regulation of protein kinase C isozymes by bryostatin 1 and phorbol 12-myristate 13-acetate in NIH 3T3 fibroblasts.
The Journal of biological chemistry 1994;269(3):2118-24.
1994: G Acs; Peter M Blumberg
Comparison of [3H]resiniferatoxin binding to spinal cord and dorsal root ganglia of newborn and adult rats.
Life sciences 1994;54(24):1875-82.
1994: G Acs; Miklós Palkovits; Peter M Blumberg
Comparison of [3H]resiniferatoxin binding by the vanilloid (capsaicin) receptor in dorsal root ganglia, spinal cord, dorsal vagal complex, sciatic and vagal nerve and urinary bladder of the rat.
Life sciences 1994;55(13):1017-26.
1994: G Acs; Peter M Blumberg
[3H]resiniferatoxin binding to pig dorsal horn membranes displays positive cooperativity.
Life sciences 1994;55(5):337-46.
1994: Peter M Blumberg; Geza Acs; L B Areces; Marcelo G Kazanietz; Nancy E Lewin; Z Szallasi
Protein kinase C in signal transduction and carcinogenesis.
Progress in clinical and biological research 1994;387():3-19.
1993: Mischak Harald; JH Pierce; JoAnne Goodnight; Marcelo G Kazanietz; Peter M Blumberg; J Frederic Mushinski
Phorbol ester-induced myeloid differentiation is mediated by protein kinase C-alpha and -delta and not by protein kinase C-beta II, -epsilon, -zeta, and -eta.
The Journal of biological chemistry 1993;268(27):20110-5.
1993: Marcelo G Kazanietz; L B Areces; A Bahador; Mischak Harald; JoAnne Goodnight; J Frederic Mushinski; Peter M Blumberg
Characterization of ligand and substrate specificity for the calcium-dependent and calcium-independent protein kinase C isozymes.
Molecular pharmacology 1993;44(2):298-307.
1993: A Szallasi; N A Lewin; Peter M Blumberg
Vanilloid (capsaicin) receptor in the rat: positive cooperativity of resiniferatoxin binding and its modulation by reduction and oxidation.
The Journal of pharmacology and experimental therapeutics 1993;266(2):678-83.
1993: J Lee; Victor E Marquez; Peter M Blumberg; Kristopher W Krausz; Marcelo G Kazanietz
Conformationally constrained analogues of diacylglycerol (DAG)--II. Differential interaction of delta-lactones and gamma-lactones with protein kinase C (PK-C).
Bioorganic & medicinal chemistry 1993;1(2):119-23.
1993: Z Szallasi; L Krsmanovic; Peter M Blumberg
Nonpromoting 12-deoxyphorbol 13-esters inhibit phorbol 12-myristate 13-acetate induced tumor promotion in CD-1 mouse skin.
Cancer research 1993;53(11):2507-12.
1993: Georg Martiny-Baron; Marcelo G Kazanietz; Mischak Harald; Peter M Blumberg; Georg Kochs; H Hug; Dieter Marmé; C Schächtele
Selective inhibition of protein kinase C isozymes by the indolocarbazole Gö 6976.
The Journal of biological chemistry 1993;268(13):9194-7.
1993: Mischak Harald; JoAnne Goodnight; Walter Kolch; Georg Martiny-Baron; C Schaechtle; Marcelo G Kazanietz; Peter M Blumberg; JH Pierce; J Frederic Mushinski
Overexpression of protein kinase C-delta and -epsilon in NIH 3T3 cells induces opposite effects on growth, morphology, anchorage dependence, and tumorigenicity.
The Journal of biological chemistry 1993;268(9):6090-6.
1993: Arpad Szallasi; Peter M Blumberg
[3H]resiniferatoxin binding by the vanilloid receptor: species-related differences, effects of temperature and sulfhydryl reagents.
Naunyn-Schmiedeberg's archives of pharmacology 1993;347(1):84-91.
1992: JoAnne Goodnight; Marcelo G Kazanietz; Peter M Blumberg; J Frederic Mushinski; Mischak Harald
The cDNA sequence, expression pattern and protein characteristics of mouse protein kinase C-zeta.
Gene 1992;122(2):305-11.
1992: Z Szallasi; Kristopher W Krausz; Peter M Blumberg
Non-promoting 12-deoxyphorbol 13-esters as potent inhibitors of phorbol 12-myristate 13-acetate-induced acute and chronic biological responses in CD-1 mouse skin.
Carcinogenesis 1992;13(11):2161-7.
1992: Marcelo G Kazanietz; Kristopher W Krausz; Peter M Blumberg
Differential irreversible insertion of protein kinase C into phospholipid vesicles by phorbol esters and related activators.
The Journal of biological chemistry 1992;267(29):20878-86.
1992: A Szallasi; N E Lewin; Peter M Blumberg
Identification of alpha-1-acid glycoprotein (orosomucoid) as a major vanilloid binding protein in serum.
The Journal of pharmacology and experimental therapeutics 1992;262(3):883-8.
1992: Nancy E Lewin; M L Dell'Aquila; George R Pettit; Peter M Blumberg; B S Warren
Binding of [3H]bryostatin 4 to protein kinase C.
Biochemical pharmacology 1992;43(9):2007-14.
1992: C M Hasler; Geza Acs; Peter M Blumberg
Specific binding to protein kinase C by ingenol and its induction of biological responses.
Cancer research 1992;52(1):202-8.
1991: Arpad Szallasi; Janos Szolcsanyi; Z Szallasi; Peter M Blumberg
Inhibition of [3H]resiniferatoxin binding to rat dorsal root ganglion membranes as a novel approach in evaluating compounds with capsaicin-like activity.
Naunyn-Schmiedeberg's archives of pharmacology 1991;344(5):551-6.
1991: Z Szallasi; Peter M Blumberg
Prostratin, a nonpromoting phorbol ester, inhibits induction by phorbol 12-myristate 13-acetate of ornithine decarboxylase, edema, and hyperplasia in CD-1 mouse skin.
Cancer research 1991;51(19):5355-60.
1991: Arpad Szallasi; Peter M Blumberg
Characterization of vanilloid receptors in the dorsal horn of pig spinal cord.
Brain research 1991;547(2):335-8.
1991: N E Lewin; George R Pettit; Y Kamano; Peter M Blumberg
Binding of [26-3H]-epi-bryostatin 4 to protein kinase C.
Cancer communications 1991;3(3):67-70.
1991: Janos Szolcsanyi; A Szallasi; Z Szallasi; F Joo; Peter M Blumberg
Resiniferatoxin. An ultrapotent neurotoxin of capsaicin-sensitive primary afferent neurons.
Annals of the New York Academy of Sciences 1991;632():473-5.
1991: Peter M Blumberg
Complexities of the protein kinase C pathway.
Molecular carcinogenesis 1991;4(5):339-44.
1991: A Szallasi; Peter M Blumberg
Molecular target size of the vanilloid (capsaicin) receptor in pig dorsal root ganglia.
Life sciences 1991;48(19):1863-9.
1990: Arpad Szallasi; Z Szallasi; Peter M Blumberg
Permanent effects of neonatally administered resiniferatoxin in the rat.
Brain research 1990;537(1-2):182-6.
1990: Janos Szolcsanyi; A Szallasi; Z Szallasi; F Joo; Peter M Blumberg
Resiniferatoxin: an ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons.
The Journal of pharmacology and experimental therapeutics 1990;255(2):923-8.
1990: Arpad Szallasi; Peter M Blumberg
Specific binding of resiniferatoxin, an ultrapotent capsaicin analog, by dorsal root ganglion membranes.
Brain research 1990;524(1):106-11.
1990: A Szallasi; Peter M Blumberg
Effect of resiniferatoxin pretreatment on the inflammatory response to phorbol-12-myristate-13-acetate in mouse strains with different susceptibilities to phorbol ester tumor promotion.
Carcinogenesis 1990;11(4):583-7.
1990: A Szallasi; Peter M Blumberg
Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor.
Life sciences 1990;47(16):1399-408.
1989: Arpad Szallasi; F Joo; Peter M Blumberg
Duration of desensitization and ultrastructural changes in dorsal root ganglia in rats treated with resiniferatoxin, an ultrapotent capsaicin analog.
Brain research 1989;503(1):68-72.
1989: Arpad Szallasi; Peter M Blumberg
Neurogenic component of phorbol ester-induced mouse skin inflammation.
Cancer research 1989;49(21):6052-7.
1989: N A Sharkey; Henry Hennings; Stuart H Yuspa; Peter M Blumberg
Comparison of octahydromezerein and mezerein as protein kinase C activators and as mouse skin tumor promoters.
Carcinogenesis 1989;10(10):1937-41.
1989: D J de Vries; Peter M Blumberg
Thermoregulatory effects of resiniferatoxin in the mouse: comparison with capsaicin.
Life sciences 1989;44(11):711-5.
1989: Peter M Blumberg; George R Pettit; B S Warren; Arpad Szallasi; L D Schuman; N A Sharkey; H Nakakuma; M L Dell'Aquila; D J de Vries
The protein kinase C pathway in tumor promotion.
Progress in clinical and biological research 1989;298():201-12.
1989: Arpad Szallasi; Peter M Blumberg
Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper.
Neuroscience 1989;30(2):515-20.
1989: H Nakakuma; M C Willingham; Peter M Blumberg
Effect of microinjected catalytic fragment of protein kinase C on morphological change in Swiss 3T3 cells.
Cancer communications 1989;1(2):127-32.
1988: D J de Vries; C L Herald; George R Pettit; Peter M Blumberg
Demonstration of sub-nanomolar affinity of bryostatin 1 for the phorbol ester receptor in rat brain.
Biochemical pharmacology 1988;37(21):4069-73.
1988: B S Warren; Y Kamano; George R Pettit; Peter M Blumberg
Mimicry of bryostatin 1 induced phosphorylation patterns in HL-60 cells by high-phorbol ester concentrations.
Cancer research 1988;48(21):5984-8.
1988: Paul A Wender; C M Cribbs; Koehler F Konrad; N A Sharkey; C L Herald; Y Kamano; George R Pettit; Peter M Blumberg
Modeling of the bryostatins to the phorbol ester pharmacophore on protein kinase C.
Proceedings of the National Academy of Sciences of the United States of America 1988;85(19):7197-201.
1988: T Sako; A I Tauber; A Y Jeng; Stuart H Yuspa; Peter M Blumberg
Contrasting actions of staurosporine, a protein kinase C inhibitor, on human neutrophils and primary mouse epidermal cells.
Cancer research 1988;48(16):4646-50.
1988: M L Dell'Aquila; C L Herald; Y Kamano; George R Pettit; Peter M Blumberg
Differential effects of bryostatins and phorbol esters on arachidonic acid metabolite release and epidermal growth factor binding in C3H 10T1/2 cells.
Cancer research 1988;48(13):3702-8.
1988: T Nakadate; A Y Jeng; Peter M Blumberg
Comparison of protein kinase C functional assays to clarify mechanisms of inhibitor action.
Biochemical pharmacology 1988;37(8):1541-5.
1988: G Pasti; E Rivedal; Stuart H Yuspa; C L Herald; George R Pettit; Peter M Blumberg
Contrasting duration of inhibition of cell-cell communication in primary mouse epidermal cells by phorbol 12,13-dibutyrate and by bryostatin 1.
Cancer research 1988;48(2):447-51.
1988: Peter M Blumberg
Protein kinase C as the receptor for the phorbol ester tumor promoters: sixth Rhoads memorial award lecture.
Cancer research 1988;48(1):1-8.
1987: T Nakadate; Peter M Blumberg
Modulation by palmitoylcarnitine of protein kinase C activation.
Cancer research 1987;47(24 Pt 1):6537-42.
1987: M L Dell'Aquila; H T Nguyen; C L Herald; George R Pettit; Peter M Blumberg
Inhibition by bryostatin 1 of the phorbol ester-induced blockage of differentiation in hexamethylene bisacetamide-treated Friend erythroleukemia cells.
Cancer research 1987;47(22):6006-9.
1987: J C Lacal; T P Fleming; B S Warren; Peter M Blumberg; Stuart A Aaronson
Involvement of functional protein kinase C in the mitogenic response to the H-ras oncogene product.
Molecular and cellular biology 1987;7(11):4146-9.
1987: T Sako; Stuart H Yuspa; C L Herald; George R Pettit; Peter M Blumberg
Partial parallelism and partial blockade by bryostatin 1 of effects of phorbol ester tumor promoters on primary mouse epidermal cells.
Cancer research 1987;47(20):5445-50.
1986: G Pasti; J C Lacal; B S Warren; Stuart A Aaronson; Peter M Blumberg
Loss of mouse fibroblast cell response to phorbol esters restored by microinjected protein kinase C.
Nature 1986;324(6095):375-7.
1986: Paul A Wender; Koehler F Konrad; N A Sharkey; M L Dell'Aquila; Peter M Blumberg
Analysis of the phorbol ester pharmacophore on protein kinase C as a guide to the rational design of new classes of analogs.
Proceedings of the National Academy of Sciences of the United States of America 1986;83(12):4214-8.