Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Research Abstract Details 

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Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Abstract Text:

Guoping Wang,Zaneta Nikolovska-Coleska,Chao-Yie Yang,Renxiao Wang,Guozhi Tang,Jie Guo,Sanjeev Shangary,Su Qiu,Wei Gao,Dajun Yang,Jennifer Meagher,Jeanne Stuckey,Krzysztof Krajewski,Sheng Jiang,Peter P Roller,Hatice Ozel Abaan,York Tomita,Shaomeng Wang,

A structure-based approach was employed to design a new class of small-molecule inhibitors of Bcl-2. The most potent compound 5 (TW-37) binds to Bcl-2 with a K(i) value of 290 nM and also to Bcl-xL and Mcl-1 with high affinities. Compound 5 potently inhibits cell growth in PC-3 prostate cancer cells with an IC(50) value of 200 nM and effectively induces apoptosis in a dose-dependent manner.

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Publishing Authors By Initials

G Wang,Z Nikolovska-Coleska,CY Yang,R Wang,G Tang,J Guo,S Shangary,S Qiu,W Gao,D Yang,J Meagher,J Stuckey,K Krajewski,S Jiang,PP Roller,HO Abaan,Y Tomita,S Wang,

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Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Journal Published:

PUBLICATION TYPE: Research Support, U.S. Gov't,

Journal: Journal of medicinal chemistry

VOLUME: 49

Page Numbers: 6139-42

Journal Abbreviation: J. Med. Chem.

ISSN: 0022-2623

DAY: 19

MONTH: Oct

YEAR: 2006

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Information

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LANGUAGE: eng

NlmUniqueID: 9716531

Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Keywords Mesh Terms:

KEYWORDS: Sulfones

MESH TERMS: pharmacology

Chemical & Substance for Abstract: Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins. Information

Substance Name: Gossypol

Registry Number: 303-45-7

Grant and Affiliation Information for Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.

AFFILIATION: Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, USA.

Country: United States

AGENCY: United States NCI

GRANT: U19CA113317

ACRONYM: CA

MEDLINETA: J Med Chem

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