First Mariner Mos1 Transposase Inhibitors (Supplementary Data)

Author(s): N. Bouchet, J. Bischerour, S. Germon, J. Guillard, M. Dubernet, M. C. Viaud-Massuard, O. Delelis, V. Ryabinin, Y. Bigot, C. Auge-Gouillou

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 9 , Issue 4 , 2009


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Abstract:

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.

Keywords: Heterocyclic chemistry, maleimides, transposon inhibitor, HIV-1 integrase inhibitor, mariner inhibitor

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Article Details

VOLUME: 9
ISSUE: 4
Year: 2009
Page: [431 - 439]
Pages: 9
DOI: 10.2174/138955709787847912
Price: $65

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