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

@article{Petros2010DiscoveryOA,
  title={Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.},
  author={Andrew M. Petros and Jeffrey R. Huth and Thorsten Oost and Cheol-Min Park and Hong Ding and Xilu Wang and Haichao Zhang and Paul M. Nimmer and Renaldo Mendoza and Chaohong C Sun and Jamey Mack and Karl Walter and Sarah A Dorwin and Emily Gramling and Uri S. Ladror and Saul H. Rosenberg and Steven W. Elmore and Stephen W. Fesik and Philip J. Hajduk},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 22},
  pages={
          6587-91
        }
}
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-x(L), 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… CONTINUE READING
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Cell Death Differ

  • H. Zhang, P. M. Nimmer, +13 authors C. Tse
  • 2007
Highly Influential
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