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Structure–Activity relationships within a series of caspase inhibitors: effect of leaving group modifications

✍ Scribed by Brett R. Ullman; Teresa Aja; Thomas L. Deckwerth; Jose-Luis Diaz; Julia Herrmann; Vincent J. Kalish; Donald S. Karanewsky; Steven P. Meduna; Kip Nalley; Edward D. Robinson; Silvio P. Roggo; Robert O. Sayers; Albert Schmitz; Robert J. Ternansky; Kevin J. Tomaselli; Joe C. Wu

Publisher: Elsevier Science
Year: 2003
Tongue: English
Weight: 178 KB
Volume: 13
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(03)00755-8

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✦ Synopsis

Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum caspase inhibitors have been identified. Their efficacy in cellular models of cell death and inflammation are also discussed.

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