2. Academic Validation
  3. Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity

Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity

  • J Med Chem. 2015 Feb 12;58(3):1556-62. doi: 10.1021/jm501482t.
Heidi L Perez 1,  Charu Chaudhry,  Stuart L Emanuel,  Caroline Fanslau,  Joseph Fargnoli,  Jinping Gan,  Kyoung S Kim,  Ming Lei,  Joseph G Naglich,  Sarah C Traeger,  Ragini Vuppugalla,  Donna D Wei,  Gregory D Vite,  Randy L Talbott,  Robert M Borzilleri
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Research , P.O. Box 4000, Princeton, New Jersey 08543, United States.
PMID: 25584393 DOI: 10.1021/jm501482t
Abstract

The prominent role of IAPs in controlling cell death and their overexpression in a variety of cancers has prompted the development of IAP antagonists as potential antitumor therapies. We describe the identification of a series of heterodimeric antagonists with highly potent antiproliferative activities in cIAP- and XIAP-dependent cell lines. Compounds 15 and 17 further demonstrate curative efficacy in human melanoma and lung Cancer xenograft models and are promising candidates for advanced studies.

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