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Larry Pearce

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TOP 3
Daisy van Veghel; Alfons Verbruggen; Peter M Blumberg; Jan Cleynhens; Ian A Deandrea-Lazarus; Larry V Pearce; Koen Van Laere; Guy Bormans
New transient receptor potential vanilloid subfamily member 1 positron emission tomography radioligands: synthesis, radiolabeling, and preclinical evaluation.
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.
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.

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All Publications

2013: Daisy van Veghel; Alfons Verbruggen; Peter M Blumberg; Jan Cleynhens; Ian A Deandrea-Lazarus; Larry V Pearce; Koen Van Laere; Guy Bormans
New transient receptor potential vanilloid subfamily member 1 positron emission tomography radioligands: synthesis, radiolabeling, and preclinical evaluation.
ACS chemical neuroscience 2013;4(4):624-34.
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: 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: 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: 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.
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: 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: 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: 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: 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: 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.
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: 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.
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: 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: 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: 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: 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.
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: 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: 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.