Article
Metal-dependent inhibition of HIV-1 integrase by beta-diketo acids and resistance of the soluble double-mutant (F185K/C280S).
Molecular pharmacology - 1 Sept 2003
Marchand Christophe, Johnson Allison A, Karki Rajeshri G, Pais Godwin C G, Zhang Xuechun, Cowansage Kiriana, Patel Tapan A, Nicklaus Marc C, Burke Terrence R, Pommier Yves
Abstract excerpt
The beta-diketo acids (DKAs) represent a major advance for anti-HIV-1 integrase drug development. We compared the inhibition of HIV-1 integrase by six DKA derivatives using the wild-type enzyme or the double-mutant F185K/C280S, which has been previously used for crystal structure determinations....
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