Profiling small molecule inhibitors against helix-receptor interactions: The Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2
We validate a practical methodology for the rapid profiling of small molecule inhibitors of protein-protein interactions. We find that a well known BH3 family inhibitor can potently inhibit the p53/hDM2 interaction.
Porter, Jason R.,Helmers, Mark R.,Wang, Ping,Furman, Jennifer L.,Joy, Stephen T.,Arora, Paramjit S.,Ghosh, Indraneel
supporting information; experimental part
p. 8020 - 8022
(2011/01/03)
Processes To Make Apoptosis Promoters
Processes to make compounds, including N-acylsulfonamide apoptosis promoters are disclosed.
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Page/Page column 33
(2009/12/28)
An efficient synthesis of ABT-263, a novel inhibitor of antiapoptotic Bcl-2 proteins
ABT-263, a newly developed Bcl-2 inhibitor, was efficiently synthesized. The key intermediates 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl] methyl}piperazin-1-yl)benzoic acid and 4-fluoro-3-[(trifluoromethyl)sulfonyl] benzenesulfonamide were eff
Wang, Guangjun,Zhang, Hushan,Zhou, Jing,Ha, Chengyong,Pei, Duanqing,Ding, Ke
experimental part
p. 2398 - 2404
(2009/04/07)
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins
Overexpression of prosurvival proteins such as Bcl-2 and Bcl-XL has been correlated with tumorigenesis and resistance to chemotherapy, and thus, the development of antagonists of these proteins may provide a novel means for the treatment of can
Park, Cheol-Min,Bruncko, Milan,Adickes, Jessica,Bauch, Joy,Ding, Hong,Kunzer, Aaron,Marsh, Kennan C.,Nimmer, Paul,Shoemaker, Alexander R.,Song, Xiaohong,Tahir, Stephen K.,Tse, Christin,Wang, Xilu,Wendt, Michael D.,Yang, Xiufen,Zhang, Haichao,Fesik, Stephen W.,Rosenberg, Saul H.,Elmore, Steven W.
experimental part
p. 6902 - 6915
(2009/11/30)
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