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Description: BMS-707035 is a novel, potent, specific, and reversible inhibitor of HIV-I integrase (IN) with IC50 of 15 nM. BMS-707035 is an investigational IN inhibitor. However, the IN mutations V75I, Q148R, V151I, and G163R are found to have resistance to BMS-707035. The inhibition of strand transfer activity by BMS-707035 is overcome when increasing amount of target DNA, so the binding of BMS-707035 to IN and target DNA to IN are mutually exclusive. The four terminal bases at the 5' end of LTR can affect the binding of BMS-707035 to IN.
References: J Biol Chem. 2007 Oct 26; 282(43):31186-96; Biochemistry. 2008 Dec 23; 47(51):13481-8.
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