Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR

…, R Mendoza, C Sun, J Mack, K Walter, S Dorwin…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6587 - 6591

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Citation Number: 52

Abstract

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 ...