First Mariner Mos1 Transposase Inhibitors
| Autor: | Bouchet, Nicolas, Bischerour, Julien, Germon, Stephanie, Guillard, Jerome, Dubernet, Mathieu, Viaud-Massuard, Maire-Claude, Delelis, Olivier, Ryabinin, Vladimir, Bigot, Yves, Auge-Gouillou, Corinne |
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| Přispěvatelé: | Génétique, immunothérapie, chimie et cancer (GICC), UMR 6239 CNRS [2008-2011] (GICC UMR 6239 CNRS), Université de Tours-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Biologie et de Pharmacologie Appliquée (LBPA), École normale supérieure - Cachan (ENS Cachan)-Centre National de la Recherche Scientifique (CNRS), Institute of Chemical Biology and Fundamental Medicine [Novosibirsk, Russia] (ICBFM SB RAS), Siberian Branch of the Russian Academy of Sciences (SB RAS), Université de Tours (UT)-Centre National de la Recherche Scientifique (CNRS), Cambefort, Jeanne |
| Jazyk: | angličtina |
| Rok vydání: | 2009 |
| Předmět: | |
| Zdroj: | Mini-Reviews in Medicinal Chemistry Mini-Reviews in Medicinal Chemistry, Bentham Science Publishers, 2009, 9 (4), pp.431-439 |
| ISSN: | 1389-5575 |
| Popis: | International audience; 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. |
| Databáze: | OpenAIRE |
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