Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
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- 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.
- Issue Date
- PERGAMON-ELSEVIER SCIENCE LTD
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.22, pp.6587 - 6591
- 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.
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