First Mariner Mos1 Transposase Inhibitors (Supplementary Data)

Title: First Mariner Mos1 Transposase Inhibitors (Supplementary Data)

Volume: 9 Issue: 4

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

Affiliation:

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

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.

Cite this article as:

Bouchet N., Bischerour J., Germon S., Guillard J., Dubernet M., Viaud-Massuard C. M., Delelis O., Ryabinin V., Bigot Y. and Auge-Gouillou C., First Mariner Mos1 Transposase Inhibitors (Supplementary Data), Mini-Reviews in Medicinal Chemistry 2009; 9 (4) . https://dx.doi.org/10.2174/138955709787847912