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Identification of a beta(3)-peptide HIV fusion inhibitor with improved potency in live cells

  作者 Bautista, AD; Stephens, OM; Wang, LG; Domaoal, RA; Anderson, KS; Schepartz, A  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-14;  页码  3736-3738  
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[摘要]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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