Cyclic PNA hexamer-based compound: modelling, synthesis and inhibition of the HIV-1 RNA dimerization process

被引:41
作者
Schwergold, C
Depecker, G
Di Giorgio, C
Patino, N
Jossinet, F
Ehresmann, B
Terreux, R
Cabrol-Bass, D
Condom, R [1 ]
机构
[1] Univ Nice, Chim Bioorgan Lab, CNRS, UMR 6001,UNSA, F-06108 Nice 2, France
[2] CNRS, Inst Biol Mol & Cellulaire, UPR 9002, F-64084 Strasbourg, France
[3] Univ Nice, Lab ASI Equipe Chimiometrie & Modelisat, F-06108 Nice 2, France
关键词
PNA hexamer; HIV-1 dimerization process; synthesis;
D O I
10.1016/S0040-4020(02)00527-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A cyclic molecule constituted by (i) a hexameric PNA moiety complementary to six among the nine residues of the dimerization initiation site loop of HIV-1 and (ii) a spacer tethering the N- to the C-extremities of the PNA, has been elaborated to inhibit the dimerization process of HIV-1 genome. This compound has been synthesized following a liquid-phase procedure (fully protected backbone approach). Preliminary agarose gel electrophoresis analyses have shown that the cyclic PNA conjugate is able to inhibit the HIV-1 dimerization. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:5675 / 5687
页数:13
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