ANTI-HIV ACTIVITIES AND PHYSICOCHEMICAL PROPERTIES OF PHOSPHOROTHIOATE ANALOGS COMPLEMENTARY TO HIV SEQUENCES

被引：14

作者：

KIM, SG

KANBARA, K

NAKASHIMA, H

YAMAMOTO, N

MURAKAMI, K

TAKAKU, H

机构：

[1] CHIBA INST TECHNOL,DEPT IND CHEM,NARASHINO,CHIBA 275,JAPAN

[2] TOKYO MED & DENT UNIV,SCH MED,DEPT MICROBIOL,BUNKYO KU,TOKYO 113,JAPAN

[3] SANYO KOKUSAKU PULP CO LTD,BIORESOURCES RES LAB,YAMAGUCHI 740,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)80320-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The modifications of oligodeoxyribonucleotides include replacement of the other chain either the whole-PS (S-ODNs) group, or group end-capped with PS (SO-ODNs) at both 3'- and 5'-ends. The melting temperature of the duplexes for one normal chain with modified phosphorothioate oligomers indicates diminished hybridization capability of the whole phosphorothioate oligomers relative to both the unmodified phosphodiester oligomers and the partially phosphorothioate-diester oligomers. In the assays of HIV, oligomers (S-ODNs) with complete replacement of the phosphodiesters with phosphorothioate groups were found to be very active. Finally of particular interest are the oligomers complementary to the HIV sequences (S-ODNs-rev or tat, 15 and 20mers) which possessed higher anti-HIV activity than the homooligomers (S-dC28 or S-dC20) itself.

引用

收藏

页码：1223 / 1228

页数：6

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