A Template-Based Approach to Inhibitors of Calpain2, 20S Proteasome, and HIV-1 Protease

A Template-Based Approach to Inhibitors of Calpain2, 20S Proteasome, and HIV-1 Protease

Specificity counts: A template-based approach to protease inhibitors is presented using a core macrocycle that presents a generic [beta]-strand template for binding to protease active sites. This is then specifically functionalized at P2 , and the C and Ntermini to give inhibitors of calpain2, 20S p...

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Veröffentlicht in:ChemMedChem 2013-12, Vol.8 (12), p.1918
Hauptverfasser: Jones, Seth A, Neilsen, Paul M, Siew, Limei, Callen, David F, Goldfarb, Nathan E, Dunn, Ben M, Abell, Andrew D
Format: Artikel
Sprache:eng
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Zusammenfassung:Specificity counts: A template-based approach to protease inhibitors is presented using a core macrocycle that presents a generic [beta]-strand template for binding to protease active sites. This is then specifically functionalized at P2 , and the C and Ntermini to give inhibitors of calpain2, 20S proteasome, and HIV-1 protease.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201300387