Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 14, Pages 3736-3738Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.032
Keywords
Foldamer; Peptidomimetic; Anti-viral; Drug design
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Funding
- NIH [GM 74756, GM 49551]
- National Foundation for Cancer Research
- Bristol-Myers Squibb
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We recently reported a beta(3)-decapeptide, beta WWI-1, that binds a validated gp41 model in vitro and inhibits gp41-mediated fusion in cell culture. Here we report six analogs of beta WWI-1 containing a variety of non-natural side chains in place of the central tryptophan of the WWI-epitope. These analogs were compared on the basis of both gp41 affinity in vitro and fusion inibition in live, HIV-infected cells. One new beta(3)-peptide, beta WXI-a, offers a significantly improved CC50/EC50 ratio in the live cell assay. (C) 2009 Elsevier Ltd. All rights reserved.
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