2. Academic Validation
  3. 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

  • J Med Chem. 2006 Oct 19;49(21):6139-42. doi: 10.1021/jm060460o.
Guoping Wang 1,  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
Affiliations

Affiliation

  • 1 Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, USA.
PMID: 17034116 DOI: 10.1021/jm060460o
Abstract

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.

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