First Mariner Mos1 Transposase Inhibitors

被引：5

作者：

Bouchet, N. ^{[2
]}

Bischerour, J. ^{[2
]}

Germon, S. ^{[2
]}

Guillard, J. ^{[2
]}

Dubernet, M. ^{[2
]}

Viaud-Massuard, M. C. ^{[2
]}

Delelis, O. ^{[4
]}

Ryabinin, V. ^{[5
]}

Bigot, Y. ^{[2
,3
]}

Auge-Gouillou, C. ^{[1
,2
]}

机构：

[1] Univ Tours, GICC, UMR6239, UFR Sci & Tech, F-37200 Tours, France

[2] CNRS, UMR6239, F-37200 Tours, France

[3] CHRU, F-37200 Tours, France

[4] Ecole Normale Super, CNRS, UMR8113, LBPA, F-94230 Cachan, France

[5] Russian Acad Sci, Siberian Div, Inst Chem Biol & Fundamental Med, Novosibirsk 630090, Russia

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2009年 / 9卷 / 04期

关键词：

Heterocyclic chemistry; maleimides; transposon inhibitor; HIV-1 integrase inhibitor; mariner inhibitor; HIV-1; INTEGRASE; BACTERIAL TRANSPOSITION; CATALYTIC DOMAIN; TN5; TRANSPOSASE; MOS1; MECHANISM; COMPLEX; BINDING; MU;

D O I：

10.2174/138955709787847912

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We described chemical inhibitors of Mos1 transposition. Some were already known to affect a related prokaryotic transposase (Tn5) or HIV-1 integrase, whereas the other were new compounds in this field. The new compounds were all organized around a bis-(heteroaryl) maleimides scaffold. Their mechanism of action depended on the chemical substitutions on the scaffold. The cross-activity, between HIV-1 integrase and Mos1 transposase, of the new group of inhibitors showed that Mos1 transposase could constitute an excellent surrogate HIV-1 inhibitor screen.

引用

页码：431 / 439

页数：9

共 29 条

[1] Targeting Tn5 transposase identifies human immunodeficiency virus type 1 inhibitors [J].