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Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors |
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| Authors: | Han Yongxin Giroux André Grimm Erich L Aspiotis Renée Francoeur Sébastien Bayly Christopher I Mckay Daniel J Roy Sophie Xanthoudakis Steve Vaillancourt John P Rasper Dita M Tam John Tawa Paul Thornberry Nancy A Paterson Erin P Garcia-Calvo Margarita Becker Joseph W Rotonda Jennifer Nicholson Donald W Zamboni Robert J |
| Affiliation: | Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co, PO Box 1005, Pointe-Claire-Dorval, Québec, Canada H9R 4P8. yongxin_han@merck.com |
| 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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