| Literature DB >> 19195886 |
Rainer Machauer1, Siem Veenstra, Jean-Michel Rondeau, Marina Tintelnot-Blomley, Claudia Betschart, Ulf Neumann, Paolo Paganetti.
Abstract
The hydroxyethylene octapeptide inhibitor OM99-2 served as starting point to create the tripeptide inhibitor 1 and its analogues 2a and b. An X-ray co-crystal structure of 1 with BACE-1 allowed the design and syntheses of a series of macrocyclic analogues 3a-h covalently linking the P1 and P3 side-chains. These inhibitors show improved enzymatic potency over their open-chain analogue. Inhibitor 3h also shows activity in a cellular system.Entities:
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Year: 2009 PMID： 19195886 DOI： 10.1016/j.bmcl.2009.01.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823