1258270-22-2Relevant academic research and scientific papers
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
Petros, Andrew M.,Huth, Jeffrey R.,Oost, Thorsten,Park, Cheol-Min,Ding, Hong,Wang, Xilu,Zhang, Haichao,Nimmer, Paul,Mendoza, Renaldo,Sun, Chaohong,MacK, Jamey,Walter, Karl,Dorwin, Sarah,Gramling, Emily,Ladror, Uri,Rosenberg, Saul H.,Elmore, Steven W.,Fesik, Stephen W.,Hajduk, Philip J.
scheme or table, p. 6587 - 6591 (2010/12/20)
The Bcl-2 family of proteins plays a major role in the regulation of apoptosis, or programmed cell death. Overexpression of the anti-apoptotic members of this family (Bcl-2, Bcl-xL, and Mcl-1) can render cancer cells resistant to chemotherapeutic agents and therefore these proteins are important targets for the development of new anti-cancer agents. Here we describe the discovery of a potent, highly selective, Bcl-2 inhibitor using SAR by NMR and structure-based drug design which could serve as a starting point for the development of a Bcl-2 selective anti-cancer agent. Such an agent would potentially overcome the Bcl-xL mediated thrombocytopenia observed with ABT-263.
