2. Academic Validation
  3. Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors

  • Bioorg Med Chem Lett. 2004 Feb 9;14(3):805-8. doi: 10.1016/j.bmcl.2003.10.064.
Yongxin Han 1,  André Giroux,  Erich L Grimm,  Renée Aspiotis,  Sébastien Francoeur,  Christopher I Bayly,  Daniel J Mckay,  Sophie Roy,  Steve Xanthoudakis,  John P Vaillancourt,  Dita M Rasper,  John Tam,  Paul Tawa,  Nancy A Thornberry,  Erin P Paterson,  Margarita Garcia-Calvo,  Joseph W Becker,  Jennifer Rotonda,  Donald W Nicholson,  Robert J Zamboni
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co, PO Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8. [email protected]
PMID: 14741294 DOI: 10.1016/j.bmcl.2003.10.064
Abstract

The discovery of a series of potent, selective and reversible dipeptidyl Caspase-3 inhibitors are reported. The iterative discovery process of using combinatorial chemistry, parallel synthesis, moleculare modelling and structural biology will be discussed.

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