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

页码：5700 / 5709

页数：10

共 41 条

[31] Cyclic PNA hexamer-based compound: modelling, synthesis and inhibition of the HIV-1 RNA dimerization process [J].