IR415是有效的抗HBV试剂(anti-HBVagent)，可通过阻断HBx的活性来抑制HBV复制。IR415选择性地与HBx相互作用(Kd=2nM)并阻断HBV介导的RNAi抑制，逆转HBx蛋白对Dicer核糖核酸内切酶活性的抑制作用。
IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease[1]. HBx: hepatitis B virus X protein.
Hepatitis B virus X protein (HBx) as a suppressor of host defenses consisting of RNAi-based silencing of viral genes[1].IR415 (50-200 μM) has a dose-dependent inhibitory effect on HBx, with a minimal effective concentration of 50 μM in HepG2/GFP-shRNA line transfected with HBx[1].
[1]. Ghosh S, et al. An RNAi-based high-throughput screening assay to identify small molecule inhibitors of hepatitis B virus replication.J Biol Chem. 2017 Jul 28;292(30):12577-12588.
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