Interfacial peptide inhibitors of HIV-1 integrase activity and dimerization

被引：56
|
作者：
Zhao, L [1 ]
O'Reilly, MK [1 ]
Shultz, MD [1 ]
Chmielewski, J [1 ]
机构：
[1] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 06期
关键词：
D O I：
10.1016/S0960-894X(03)00040-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Peptides derived from the interfacial region of dimeric HIV-1 integrase were evaluated as inhibitors of integrase's 3'-endonuclease activity. Three peptides were found to be moderately potent inhibitors with IC50 values in the low micromolar range. The mode of inhibition was probed through protein crosslinking experiments. Active interfacial peptides were found to inhibit crosslinking of the dimeric form of integrase. Interfacial peptides that were poor inhibitors had no effect on integrase crosslinking. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1175 / 1177
页数：3
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