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HIV gp120-CD4相互作用潜在抑制剂的设计、合成与评估

Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions.

作者信息

Boussard Cyrille, Klimkait Thomas, Mahmood Naheed, Pritchard Martin, Gilbert Ian H

机构信息

Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, UK.

出版信息

Bioorg Med Chem Lett. 2004 May 17;14(10):2673-6. doi: 10.1016/j.bmcl.2004.02.091.

DOI:10.1016/j.bmcl.2004.02.091
PMID:15109676
Abstract

This paper describes an approach to prevent HIV-cell fusion by disrupting the interaction between HIV protein gp120 and CD4 receptor. The CD4 residues Phe43 and Arg59 make important interactions with gp120. Small molecule analogues were made to mimic the crucial features of these residues. The analogues were assayed using a cellular 'FIGS' assay to measure inhibition of cell fusion and caused some inhibition.

摘要

本文描述了一种通过破坏HIV蛋白gp120与CD4受体之间的相互作用来预防HIV-细胞融合的方法。CD4的苯丙氨酸43和精氨酸59残基与gp120形成重要的相互作用。制备了小分子类似物以模拟这些残基的关键特征。使用细胞“FIGS”试验对这些类似物进行检测，以测量细胞融合的抑制情况，结果显示有一定程度的抑制作用。

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