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Description: (+/-)-BI-D is a novel and potent allosteric/noncatalytic site integrase inhibitor that binds integrase at the LEDGF/p75 binding site. It binds with higher affinity to a tetrameric form compared to a dimeric form of integrase. The binding of integrase (IN) to lens epithelium-derived growth factor (LEDGF)/p75 in large part determines the efficiency and specificity of HIV-1 integration. However, a significant residual preference for integration into active genes persists in Psip1 (the gene that encodes for LEDGF/p75) knockout (KO) cells.
References: Nucleic Acids Res. 2012 Dec; 40(22):11518-30; ACS Med Chem Lett. 2014 Apr 16; 5(6):711-6.
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