Ontology highlight
ABSTRACT:
SUBMITTER: Wei J
PROVIDER: S-EPMC2750823 | biostudies-literature | 2009 Apr
REPOSITORIES: biostudies-literature
Wei Jun J Kitada Shinichi S Rega Michele F MF Emdadi Aras A Yuan Hongbin H Cellitti Jason J Stebbins John L JL Zhai Dayong D Sun Jiazhi J Yang Li L Dahl Russell R Zhang Ziming Z Wu Bainan B Wang Si S Reed Tyler A TA Wang Hong-Gang HG Lawrence Nicholas N Sebti Said S Reed John C JC Pellecchia Maurizio M
Molecular cancer therapeutics 20090401 4
Guided by a combination of nuclear magnetic resonance binding assays and computational docking studies, we synthesized a library of 5,5' substituted Apogossypol derivatives as potent Bcl-XL antagonists. Each compound was subsequently tested for its ability to inhibit Bcl-XL in an in vitro fluorescence polarization competition assay and exert single-agent proapoptotic activity in human cancer cell lines. The most potent compound BI79D10 binds to Bcl-XL, Bcl-2, and Mcl-1 with IC50 values of 190, 3 ...[more]