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Title: Michael acceptors as cysteine protease inhibitors
Author: Santos, Maria M. M.
Moreira, Rui
Keywords: Cysteine protease inhibitors
Vinyl sulfone
Alfa,beta-unsaturated carbonyl derivative
Aza-peptide Michael acceptor
Issue Date: 2007
Publisher: Bentham Science Publishers
Citation: Santos, Maria M. M.; Moreira, Rui. Michael acceptors as cysteine protease inhibitors, Mini Reviews Medicinal Chemistry, 7, 1040-1050, 2007.
Abstract: Cysteine proteases selectively catalyze the hydrolysis of peptide bonds. Uncontrolled, unregulated, or undesired proteolysis can lead to many disease states including emphysema, stroke, viral infections, cancer, Alzheimer’s disease, inflammation, and arthritis. Cysteine proteases inhibitors thus have considerable potential utility for therapeutic intervention in a variety of disease states. This review emphasizes on the new developments from literature reports on Michael acceptors as potential cysteine protease inhibitors, namely vinyl sulfones, alfa,beta-unsaturated carbonyl derivatives and aza-peptides. These compounds irreversibly alkylate the active site cysteine residue via conjugate addition. Examples of Michael acceptors inhibitors that have already progressed to clinical testing are also presented.
Peer review: yes
ISSN: 1389-5575
Publisher Version:
Appears in Collections:FF - Artigos em Revistas Internacionais

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