ntcp

战天斗hbv

Sodium taurocholate cotransporting polypeptide (NTCP) is a multiple transmembrane transporter predominantly expressed in the liver, functioning as a functional receptor for HBV. Through our continuous efforts to identify NTCP as a novel HBV target, we designed and synthesized a series of new compounds based on the structure of our previous compound NT-5. Molecular docking and MD simulation validated that a new compound named NTI-007 can tightly bind to NTCP, whose efficacy was also measured in vitro virological examination and cytotoxicity studies. Furthermore, autophagy was observed in NTI-007 incubated HepG2.2.15 cells, and results of q-PCR and Western blotting revealed that NTI-007 induced autophagy through NTCP–APOA1–HBx–Beclin1-mediated pathway. Taken together, considering crucial role of NTCP in HBV infection, NTCP-mediated autophagic pathway may provide a promising strategy of HBV therapy and given efficacy of NTI-007 triggering autophagy. Our study suggests pre-clinical potential of this compound as a novel anti-HBV drug candidate.

战天斗hbv

牛磺胆酸钠cotransporting多肽（NTCP）是一个多跨膜转运主要在肝中表达，用作功能性受体的HBV。通过我们的不断努力，以确定NTCP作为一种新型的HBV目标，我们设计并合成了一系列基于我们以前的复合NT-5结构的新化合物。分子对接和MD模拟验证了一个名为NTI-007的新化合物裹紧NTCP，其疗效还测定体外病毒学检查和细胞毒性研究。此外，自噬观察NTI-007培养HepG2.2.15细胞，并导致Q-PCR和Western印迹显示，通过NTCP，APOA1-HBx蛋白-Beclin1基因介导途径NTI-007诱导自噬。综合来看，考虑到NTCP在HBV感染至关重要的作用，NTCP介导的自噬途径可以提供NTI-007触发自噬的前途HBV治疗策略和疗效给出。我们的研究表明，这种化合物的临床前势作为一种新的抗HBV药物候选

战天斗hbv

NTCP抑制剂、最强的盾、虽然还有很多问题要解决、SW提到过这个NTCP受体的原本功能是很重要的、竞争性的占据NTCP受体是否对肝功能有负面影响、有待研究、而且德国人的第一个受体抑制剂、现在有点那啥、当然、第一个候选药物有点缺陷可以理解、现在看日本人做出的抑制剂效果怎么样了、现在还需要一把最强的矛（现在我认为、咱们一个矛都没有、核苷不配）、看好birinapant、单药one shoot、搞不定HBV、还有一点、以前那些争论NTCP是否是骗事的、是否真实的争论可以休矣、NTCP目前得到了业界广泛认可、怎么利用NTCP、就看各路好汉了

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