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Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
Wang, Guoping; Nikolovska-Coleska, Zaneta; Yang, Chao-Yie; Wang, Renxiao; Tang, Guozhi; Guo, Jie; Shangary, Sanjeev; Qiu, Su; Gao, Wei; Yang, Dajun; Meagher, Jennifer; Stuckey, Jeanne; Krajewski, Krzysztof; Jiang, Sheng; Roller, Peter P; Abaan, Hatice Ozel; Tomita, York; Wang, Shaomeng.
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  • Wang G; Comprehensive Cancer Center and Department of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, Michigan 48109, USA.
J Med Chem ; 49(21): 6139-42, 2006 Oct 19.
Article en En | MEDLINE | ID: mdl-17034116
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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Banco de datos: MEDLINE Asunto principal: Sulfonas / Benzamidas / Gosipol / Apoptosis / Proteínas Proto-Oncogénicas c-bcl-2 Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos
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PubMed Links

Banco de datos: MEDLINE Asunto principal: Sulfonas / Benzamidas / Gosipol / Apoptosis / Proteínas Proto-Oncogénicas c-bcl-2 Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2006 Tipo del documento: Article País de afiliación: Estados Unidos