一种在活细胞中效力增强的β3肽HIV融合抑制剂的鉴定。
Identification of a beta3-peptide HIV fusion inhibitor with improved potency in live cells.
作者信息
Bautista Arjel D, Stephens Olen M, Wang Ligong, Domaoal Robert A, Anderson Karen S, Schepartz Alanna
机构信息
Department of Chemistry, Yale University, New Haven, CT 06520, USA.
出版信息
Bioorg Med Chem Lett. 2009 Jul 15;19(14):3736-8. doi: 10.1016/j.bmcl.2009.05.032. Epub 2009 May 15.
Abstract
We recently reported a beta(3)-decapeptide, betaWWI-1, that binds a validated gp41 model in vitro and inhibits gp41-mediated fusion in cell culture. Here we report six analogs of betaWWI-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, betaWXI-a, offers a significantly improved CC(50)/EC(50) ratio in the live cell assay.
摘要
我们最近报道了一种β(3)-十肽βWWI-1，它在体外能结合经过验证的gp41模型，并在细胞培养中抑制gp41介导的融合。在此我们报道βWWI-1的六种类似物，它们含有多种非天然侧链，取代了WWI表位的中心色氨酸。基于体外gp41亲和力和在活的HIV感染细胞中的融合抑制作用对这些类似物进行了比较。一种新的β(3)-肽βWXI-a在活细胞试验中提供了显著改善的CC(50)/EC(50)比值。
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