Browse views: by Year, by Function, by GLF, by Subfunction, by Conference, by Journal

Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.

Imbach, Patricia and Lang, Marc and Garcia-Echeverria, Carlos and Guagnano, Vito and Noorani, Maria and Roesel, Johannes and Bitsch, Francis and Rihs, Grety and Furet, Pascal (2007) Novel beta-lactam derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome. Bioorganic & Medicinal Chemistry Letters, 17 (2). pp. 358-362. ISSN 0960-894X

Abstract

A series of beta-lactam derivatives has been designed and synthesized to inhibit the chymotrypsin-like activity of the human 20S proteasome. The most potent compounds of this new structural class of beta-subunit selective 20S proteasome inhibitors exhibit IC50 values in the low-nanomolar range and show good selectivity over the trypsin-like and post-glutamyl-peptide hydrolytic activities of the enzyme.

Item Type: Article
Related URLs:
Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Proteasome inhibitors; β-Lactams; Covalent inhibitors; Antiproliferative agents
Related URLs:
Date Deposited: 14 Dec 2009 13:57
Last Modified: 31 Jan 2013 01:13
URI: https://oak.novartis.com/id/eprint/572

Search

Email Alerts

Register with OAK to receive email alerts for saved searches.