First Mariner Mos1 transposase inhibitors.
Copyright policy )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 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.
- Laboratoire de Biologie et Pharmacologie Appliquée France
- François Rabelais University France
- Siberian Branch of the Russian Academy of Sciences Russian Federation
- French National Centre for Scientific Research France
- Institute of Chemical Biology and Fundamental Medicine Russian Federation
maleimides, [CHIM.THER] Chemical Sciences/Medicinal Chemistry, transposon inhibitor, Transposases, mariner inhibitor, HIV Integrase, Cross Reactions, In Vitro Techniques, Heterocyclic chemistry, DNA-Binding Proteins, Maleimides, Drug Discovery, HIV-1 integrase inhibitor
maleimides, [CHIM.THER] Chemical Sciences/Medicinal Chemistry, transposon inhibitor, Transposases, mariner inhibitor, HIV Integrase, Cross Reactions, In Vitro Techniques, Heterocyclic chemistry, DNA-Binding Proteins, Maleimides, Drug Discovery, HIV-1 integrase inhibitor
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