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A cyclic PNA-based compound targeting domain IV of HCVIRES RNA inhibits in vitro IRES-dependent translation

被引：7
作者：
Caldarelli, SA
Mehiri, M
Di Giorgio, A
Martin, A
Hantz, O
Zoulim, F
Terreux, R
Condom, R
Patino, N
机构：
[1] Univ Nice, UMR CNRS 6001, Lab Chim Bioorgan, F-06108 Nice, France
[2] INSERM U271, F-69424 Lyon, France
[3] Univ Lyon 1, Fac Pharm, Lab LPCM2, F-69373 Lyon, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2005年 / 13卷 / 20期
基金：
澳大利亚研究理事会;
关键词：
cyclic PNA; HCVIRES; domain IV; Loop-Loop interaction;
D O I：
10.1016/j.bmc.2005.06.008
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A cyclic molecule I constituted by a hepta-peptide nucleic acid sequence complementary to the apical loop of domain IV of hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA has been prepared via a 'mixed' liquid-phase strategy, which relies on easily available protected PNA and poly(2-aminoethylglycinamide) building blocks. This compound 1 has been elaborated to mimic 'loop-loop' interactions. For comparison, its linear analog has also been investigated. Although preliminary biological assays have revealed the ability of I to inhibit in vitro the HCV IRES-dependent translation in a dose-dependent manner, the linear analog has shown a slightly higher activity. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5700 / 5709
页数：10
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