Design, synthesis, and biological activity of a cyclic peptide: An inhibitor of HIV-1 Tat-TAR interactions in human cells

被引：32
|
作者：
Tamilarasu, N
Huq, I
Rana, TM
机构：
[1] Rutgers State Univ, Robert Wood Johnson Med Sch, Dept Pharmacol, Piscataway, NJ 08854 USA
[2] Rutgers State Univ, Mol Biosci Grad Program, Piscataway, NJ 08854 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期
关键词：
D O I：
10.1016/S0960-894X(00)00140-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of Tat protein with the transactivation responsive region (TAR) RNA, a 59-base stem-loop structure located at the 5'-end of all HIV mRNAs. A number of cyclic peptides are known to possess antibiotic activity and increased biological stability. Here we report the design, synthesis, and biological activity of a cyclic peptide (2), which inhibits transcriptional activation by Tat protein in human cells with an IC50 of approximate to 40 nM. Cyclic peptides that can target specific RNA structures provide a new class of small molecules that can be used to control cellular processes involving RNA-protein interactions in vivo. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：971 / 974
页数：4
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