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Nancy Lewin
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58
Blumberg, Peter
34
Marquez, Victor
12
Lee, Jeewoo
10
Sigano, Dina
10
Kang, Ji-Hye
10
Wang, Shulin
8
Kazanietz, Marcelo
8
Nacro, Kassoum
7
Pettit, George
7
Milne, GW
7
Kedei, Noemi
6
Bienfait, B
6
Peach, Megan
6
Pearce, Larry
6
Pu, Yongmei
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All Publications
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2009: Sosa Maria Soledad; Lewin Nancy E; Choi Sung-Hee; Blumberg Peter M; Kazanietz Marcelo G
Biochemical characterization of hyperactive beta2-chimaerin mutants revealed an enhanced exposure of C1 and Rac-GAP domains.
Biochemistry 2009;48(34):8171-8.
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2009: Keck Gary E; Li Wei; Kraft Matthew B; Kedei Noemi; Lewin Nancy E; Blumberg Peter M
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.
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2009: Comin Maria J; Czifra Gabriella; Kedei Noemi; Telek Andrea; Lewin Nancy E; Kolusheva Sofiya; Velasquez Julia F; Kobylarz Ryan; Jelinek Raz; Blumberg Peter M; Marquez Victor E
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.
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2009: Keck Gary E; Poudel Yam B; Welch Dennie S; Kraft Matthew B; Truong Anh P; Stephens Jeffrey C; Kedei Noemi; Lewin Nancy E; Blumberg Peter M
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.
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2008: Duan Dehui; Sigano Dina M; Kelley James A; Lai Christopher C; Lewin Nancy E; Kedei Noemi; Peach Megan L; Lee Jeewoo; Abeyweera Thushara P; Rotenberg Susan A; Kim Hee; Kim Young Ho; El Kazzouli Saïd; Chung Jae-Uk; Young Howard A; Young Matthew R; Baker Alyson; Colburn Nancy H; Haimovitz-Friedman Adriana; Truman Jean-Philip; Parrish Damon A; Deschamps Jeffrey R; Perry Nicholas A; Surawski Robert J; Blumberg Peter M; Marquez Victor E
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.
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2008: Choi Sung Hee; Czifra Gabriella; Kedei Noemi; Lewin Nancy E; Lazar Jozsef; Pu Yongmei; Marquez Victor E; Blumberg Peter M
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.
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2007: Choi Yongseok; Pu Yongmei; Peach Megan L; Kang Ji-Hye; Lewin Nancy E; Sigano Dina M; Garfield Susan H; Blumberg Peter M; Marquez Victor E
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.
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2007: Malolanarasimhan Krishnan; Kedei Noemi; Sigano Dina M; Kelley James A; Lai Christopher C; Lewin Nancy E; Surawski Robert J; Pavlyukovets Vladimir A; Garfield Susan H; Wincovitch Stephen; Blumberg Peter M; Marquez Victor E
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.
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2006: Kang Ji-Hye; Benzaria Samira; Sigano Dina M; Lewin Nancy E; Pu Yongmei; Peach Megan L; Blumberg Peter M; Marquez Victor E
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.
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2006: Lee Jeewoo; Kang Ji-Hye; Han Kee-Chung; Kim Yerim; Kim Su Yeon; Youn Hae-Suk; Mook-Jung Inhee; Kim Hee; Lo Han Jee Hye; Ha Hee Jin; Kim Young Ho; Marquez Victor E; Lewin Nancy E; Pearce Larry V; Lundberg Daniel J; Blumberg Peter M
Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators.
Journal of medicinal chemistry 2006;49(6):2028-36.
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2006: Lee Jeewoo; Lee Ju-Hyun; Kim Su Yeon; Perry Nicholas A; Lewin Nancy E; Ayres Jolene A; Blumberg Peter M
2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands.
Bioorganic & medicinal chemistry 2006;14(6):2022-31.
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2005: Kang Ji-Hye; Peach Megan L; Pu Yongmei; Lewin Nancy E; Nicklaus Marc C; Blumberg Peter M; Marquez Victor E
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.
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2005: Pu Yongmei; Perry Nicholas A; Yang Dazhi; Lewin Nancy E; Kedei Noemi; Braun Derek C; Choi Sung Hee; Blumberg Peter M; Garfield Susan H; Stone James C; Duan Dehui; Marquez Victor E
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.
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2004: Tamamura Hirokazu; Sigano Dina M; Lewin Nancy E; Peach Megan L; Nicklaus Marc C; Blumberg Peter M; Marquez Victor E
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.
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2004: Kang Ji-Hye; Kim Su Yeon; Lee Jeewoo; Marquez Victor E; Lewin Nancy E; Pearce Larry V; Blumberg Peter M
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.
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2004: Kang Ji-Hye; Siddiqui Maqbool A; Sigano Dina M; Krajewski Krzysztof; Lewin Nancy E; Pu Yongmei; Blumberg Peter M; Lee Jeewoo; Marquez Victor E
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.
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2004: Duan Dehui; Lewin Nancy E; Sigano Dina M; Blumberg Peter M; Marquez Victor E
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.
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2004: Pettit George R; Hoffmann Holger; Herald Delbert L; McNulty James; Murphy Alison; Higgs Kerianne C; Hamel Ernest; Lewin Nancy E; Pearce Larry V; Blumberg Peter M; Pettit Robin K; Knight John C
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine.
The Journal of organic chemistry 2004;69(7):2251-6.
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2004: Pettit George R; Hoffmann Holger; Herald Delbert L; Blumberg Peter M; Hamel Ernest; Schmidt Jean M; Chang Yung; Pettit Robin K; Lewin Nancy E; Pearce Larry V
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.
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2004: Tamamura Hirokazu; Sigano Dina M; Lewin Nancy E; Blumberg Peter M; Marquez Victor E
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.
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2003: Sridhar Jayalakshmi; Wei Zhi-Liang; Nowak Ireneusz; Lewin Nancy E; Ayres Jolene A; Pearce Larry V; Blumberg Peter M; Kozikowski Alan P
New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Journal of medicinal chemistry 2003;46(19):4196-204.
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2003: Choi Yongseok; Kang Ji-Hye; Lewin Nancy E; Blumberg Peter M; Lee Jeewoo; Marquez Victor E
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.
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2003: Kang Ji-Hye; Chung Hye-Eun; Kim Su Yeon; Kim Yerim; Lee Jeewoo; Lewin Nancy E; Pearce Larry V; Blumberg Peter M; Marquez Victor E
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.
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2003: Sigano Dina M; Peach Megan L; Nacro Kassoum; Choi Yongseok; Lewin Nancy E; Nicklaus Marc C; Blumberg Peter M; Marquez Victor E
Differential binding modes of diacylglycerol (DAG) and DAG lactones to protein kinase C (PK-C).
Journal of medicinal chemistry 2003;46(9):1571-9.
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2003: Kozikowski Alan P; Nowak Ireneusz; Petukhov Pavel A; Etcheberrigaray Rene; Mohamed Ali; Tan Mathew; Lewin Nancy; Hennings Henry; Pearce Larry L; Blumberg Peter M
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.
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2003: Lewin Nancy E; Blumberg Peter M
[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.
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2002: Pettit George R; Ducki Sylvie; Tan Rui; Gardella Roberta S; McMahon James B; Boyd Michael R; Pettit George R; Blumberg Peter M; Lewin Nancy E; Doubek Dennis L; Tackett Larry P; Williams Michael D
Isolation and structure of pedilstatin from a republic of maldives Pedilanthus sp.
Journal of natural products 2002;65(9):1262-5.
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2002: Wei Zhi-Liang; Sakamuri Sukumar; Petukhov Pavel A; George Clifford; Lewin Nancy E; Blumberg Peter M; Kozikowski Alan P
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.
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2001: Lee J; Han K C; Kang J H; Pearce L L; Lewin N E; Yan S; Benzaria S; Nicklaus M C; Blumberg P M; Marquez V E
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.
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2001: Shao L; Lewin N E; Lorenzo P S; Hu Z; Enyedy I J; Garfield S H; Stone J C; Marner F J; Blumberg P M; Wang S
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.
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2001: Nacro K; Sigano D M; Yan S; Nicklaus M C; Pearce L L; Lewin N E; Garfield S H; Blumberg P M; Marquez V E
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.
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2001: Lee J; Han K C; Lee S Y; Kim S Y; Kang J H; Lewin N E; Best L S; Blumberg P M; Marquez V E
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.
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2000: Tamamura H; Bienfait B; Nacro K; Lewin N E; Blumberg P M; Marquez V E
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.
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2000: Nacro K; Bienfait B; Lewin N E; Blumberg P M; Marquez V E
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.
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2000: Nacro K; Bienfait B; Lee J; Han K C; Kang J H; Benzaria S; Lewin N E; Bhattacharyya D K; Blumberg P M; Marquez V E
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.
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1999: Caloca M J; Garcia-Bermejo M L; Blumberg P M; Lewin N E; Kremmer E; Mischak H; Wang S; Nacro K; Bienfait B; Marquez V E; Kazanietz M G
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.
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1999: Wang S; Liu M; Lewin N E; Lorenzo P S; Bhattacharrya D; Qiao L; Kozikowski A P; Blumberg P M
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.
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1999: Marquez V E; Nacro K; Benzaria S; Lee J; Sharma R; Teng K; Milne G W; Bienfait B; Wang S; Lewin N E; Blumberg P M
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.
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1998: Benzaria S; Bienfait B; Nacro K; Wang S; Lewin N E; Beheshti M; Blumberg P M; Marquez V E
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.
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1998: Marquez V E; Sharma R; Wang S; Lewin N E; Blumberg P M; Kim I S; Lee J
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.
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1998: Bíró T; Brodie C; Modarres S; Lewin N E; Acs P; Blumberg P M
Specific vanilloid responses in C6 rat glioma cells.
Brain research. Molecular brain research 1998;56(1-2):89-98.
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1998: Bíró T; Maurer M; Modarres S; Lewin N E; Brodie C; Acs G; Acs P; Paus R; Blumberg P M
Characterization of functional vanilloid receptors expressed by mast cells.
Blood 1998;91(4):1332-40.
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1997: Caloca M J; Fernandez N; Lewin N E; Ching D; Modali R; Blumberg P M; Kazanietz M G
Beta2-chimaerin is a high affinity receptor for the phorbol ester tumor promoters.
The Journal of biological chemistry 1997;272(42):26488-96.
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1997: Kozikowski A P; Wang S; Ma D; Yao J; Ahmad S; Glazer R I; Bogi K; Acs P; Modarres S; Lewin N E; Blumberg P M
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.
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1996: Lee J; Lewin N E; Acs P; Blumberg P M; Marquez V E
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.
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1996: Lee J; Lewin N E; Blumberg P M; Marquez V E
Synthesis of bis-gamma-butyrolactones containing conformationally constrained (S)- and (R)-diacylglycerol structures.
Bioorganic & medicinal chemistry 1996;4(8):1299-305.
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1996: Szallasi Z; Du L; Levine R; Lewin N E; Nguyen P N; Williams M D; Pettit G R; Blumberg P M
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.
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1996: Lee J; Sharma R; Wang S; Milne G W; Lewin N E; Szallasi Z; Blumberg P M; George C; Marquez V E
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.
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1996: Lee J; Wang S; Milne G W; Sharma R; Lewin N E; Blumberg P M; Marquez V E
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.
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1996: Sharma R; Lee J; Wang S; Milne G W; Lewin N E; Blumberg P M; Marquez V E
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.
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1995: Kazanietz M G; Wang S; Milne G W; Lewin N E; Liu H L; Blumberg P M
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.
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1995: Acs G; Lee J; Marquez V E; Wang S; Milne G W; Du L; Lewin N E; Blumberg P M
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.
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1995: Kozikowski A P; Ma D; Du L; Lewin N E; Bumberg P M
Effect of alteration of the heterocyclic nucleus of ILV on its isoform selectivity for PKC. Palladium catalyzed route to benzofuran analogues of ILV.
Farmaco (Società chimica italiana : 1989) 1995;50(6):425-30.
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1995: Kazanietz M G; Lewin N E; Bruns J D; Blumberg P M
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.
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1995: Blumberg P M; Acs G; Acs P; Areces L B; Kazanietz M G; Lewin N E; Szallasi Z
Protein kinase C in cell signaling: strategies for the development of selective inhibitors.
Agents and actions. Supplements 1995;47():87-100.
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1994: Wang S; Zaharevitz D W; Sharma R; Marquez V E; Lewin N E; Du L; Blumberg P M; Milne G W
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.
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1994: Kazanietz M G; Lewin N E; Gao F; Pettit G R; Blumberg P M
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.
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1994: Blumberg P M; Acs G; Areces L B; Kazanietz M G; Lewin N E; Szallasi Z
Protein kinase C in signal transduction and carcinogenesis.
Progress in clinical and biological research 1994;387():3-19.
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1992: Gustafson K R; Cardellina J H; McMahon J B; Gulakowski R J; Ishitoya J; Szallasi Z; Lewin N E; Blumberg P M; Weislow O S; Beutler J A
A nonpromoting phorbol from the samoan medicinal plant Homalanthus nutans inhibits cell killing by HIV-1.
Journal of medicinal chemistry 1992;35(11):1978-86.
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1992: Lewin N E; Dell'Aquila M L; Pettit G R; Blumberg P M; Warren B S
Binding of [3H]bryostatin 4 to protein kinase C.
Biochemical pharmacology 1992;43(9):2007-14.
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