Literature DB >> 14741294

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

Yongxin Han1, 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.   

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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Year:  2004        PMID: 14741294     DOI: 10.1016/j.bmcl.2003.10.064

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Small Molecule Active Site Directed Tools for Studying Human Caspases.

Authors:  Marcin Poreba; Aleksandra Szalek; Paulina Kasperkiewicz; Wioletta Rut; Guy S Salvesen; Marcin Drag
Journal:  Chem Rev       Date:  2015-11-09       Impact factor: 60.622

Review 2.  The apoptosome: emerging insights and new potential targets for drug design.

Authors:  Marcello D'Amelio; Elisa Tino; Francesco Cecconi
Journal:  Pharm Res       Date:  2007-08-03       Impact factor: 4.200

3.  Structural and functional definition of the specificity of a novel caspase-3 inhibitor, Ac-DNLD-CHO.

Authors:  Atsushi Yoshimori; Junichi Sakai; Satoshi Sunaga; Takanobu Kobayashi; Satoshi Takahashi; Naoyuki Okita; Ryoko Takasawa; Sei-ichi Tanuma
Journal:  BMC Pharmacol       Date:  2007-06-27
  3 in total

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