(_plusmn_)-BI-D是HIV整合酶（integrase）变构抑制剂，作用于整合酶与LEDGF/p75结合部位。
(±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.IC50 value: 2.4-2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1]Target: integrase inhibitorin vitro: Approximately 2.4-2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160-200 nM, in Psip1 and double-KO cells [1].
[1]. Wang H, et al. HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor. Nucleic Acids Res. 2012 Dec;40(22):115 [2]. Fader LD, et al. Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6.
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