First Mariner Mos1 transposase inhibitors

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...

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Bibliographic Details
Published inMini reviews in medicinal chemistry Vol. 9; no. 4; p. 431
Main Authors Bouchet, N, Bischerour, J, Germon, S, Guillard, J, Dubernet, M, Viaud-Massuard, M C, Delelis, O, Ryabinin, V, Bigot, Y, Augé-Gouillou, C
Format Journal Article
LanguageEnglish
Published Netherlands 01.04.2009
Subjects
Cross Reactions
DNA-Binding Proteins - antagonists & inhibitors
Drug Discovery
HIV Integrase - drug effects
In Vitro Techniques
Maleimides - chemistry
Maleimides - pharmacology
Transposases - antagonists & inhibitors
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Summary: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.
ISSN:1389-5575
DOI:10.2174/138955709787847912