期刊
CHEMISTRY & BIOLOGY
卷 11, 期 3, 页码 389-395出版社
CELL PRESS
DOI: 10.1016/j.chembiol.2004.02.020
关键词
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资金
- NCI NIH HHS [CA 30991] Funding Source: Medline
- PHS HHS [A 78040] Funding Source: Medline
Antiapoptotic Bcl-2-family proteins Bcl-2 and Bcl-1X(L) have been recently validated as drug discovery targets for cancer. Here, by using a combination of molecular modeling, NMR-based structural analysis, fluorescence polarization assays, and cell-based assays, we have designed and characterized a novel proapoptotic compound targeting these proteins. Our compound, Apogossypol, is capable of binding and inhibiting Bcl-2 and Bcl-X-L with high affinity and induces apoptosis of tumor cell lines. Mechanistic studies on the action of our compound were also performed via confocal microscopy that provided real-time detection of the interaction with Bcl-X-L in intact cells. Finally, preliminary data on cells freshly isolated from patients affected by chronic lymphocytic leukemia strongly suggest potential applications of Bcl-2 antagonists as chemosensitizers in cancer therapy.
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