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.
Bouchet
N
N
GICC UMR6239, Université de Tours, UFR Sciences & Techniques, Parc Grandmont, Bat L, 37200 Tours, France.
Bischerour
J
J
Germon
S
S
Guillard
J
J
Dubernet
M
M
Viaud-Massuard
M C
MC
Delelis
O
O
Ryabinin
V
V
Bigot
Y
Y
Augé-Gouillou
C
C
D003429:Cross Reactions; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors*; D055808:Drug Discovery; D019427:HIV Integrase / Q000187:drug effects*; D066298:In Vitro Techniques; D008301:Maleimides / Q000737:chemistry* / Q000494:pharmacology*; D019895:Transposases / Q000037:antagonists & inhibitors*
D004268:DNA-Binding Proteins; D008301:Maleimides; C111652:mariner transposases; D019427:HIV Integrase; D019895:Transposases; C514801:p31 integrase protein, Human immunodeficiency virus 1