Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins
G Wang, Z Nikolovska-Coleska, CY Yang… - Journal of medicinal …, 2006 - ACS Publications
G Wang, Z Nikolovska-Coleska, CY Yang, R Wang, G Tang, J Guo, S Shangary, S Qiu…
Journal of medicinal chemistry, 2006•ACS PublicationsA 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 IC50 value of 200 nM and effectively induces
apoptosis in a dose-dependent manner.
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 IC50 value of 200 nM and effectively induces
apoptosis in a dose-dependent manner.
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 Ki 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 IC50 value of 200 nM and effectively induces apoptosis in a dose-dependent manner.
ACS Publications