Article
Potent inhibitors of HIV-1 integrase display a two-step, slow-binding inhibition mechanism which is absent in a drug-resistant T66I/M154I mutant.
Biochemistry - 24 Feb 2009
Garvey Edward P, Schwartz Benjamin, Gartland Margaret J, Lang Scott, Halsey Wendy, Sathe Ganesh, Carter H Luke, Weaver Kurt L
Abstract excerpt
Two-metal binding HIV-1 integrase inhibitors (INIs) are potent inhibitors of HIV-1 in vitro and in patients. We report here for the first time the kinetics of inhibition of integrase-catalyzed strand transfer. First, the IC(50) values for each of six structurally distinct INIs decreased when a preincubation was included: S-1360 (1.3 microM vs 0.12 microM), L-731,988 (130 nM vs 9 nM), L-870,810 (130 nM vs 4 nM),...
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