Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential,Journal of Medicinal Chemistry

当前位置： X-MOL 学术 › J. Med. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2022-09-15 , DOI: 10.1021/acs.jmedchem.2c01097
Siwei Chen ₁ , Lan Zhang ₁ , Yi Chen ₂ , Leilei Fu ₁

Affiliation

Hepatitis B virus (HBV) infection is a worldwide health problem, and chronic infection can cause many diseases ranging from liver fibrosis to hepatocellular carcinoma (HCC) by complicated mechanisms. Currently, the treatment of HBV infection mainly depends on interferons (IFNs) and nucleotide analogues (NAs); however, both have some limitations. In 2012, sodium taurocholate cotransporting polypeptide (NTCP) was identified as the entry receptor of HBV. Based upon this groundbreaking discovery, a series of molecules have been gradually developed and evaluated to discover novel entry inhibitors targeting NTCP. However, only two macromolecules have been used for potential clinical applications so far. In this Perspective, we focus on summarizing the structural features that convey the biological functions of NTCP, as well as further discuss the anti-HBV activity and selectivity of inhibitors in HBV-related diseases, which should provide clues in the future for the discovery of drug candidates targeting NTCP.

中文翻译：

在 HBV 相关疾病中抑制牛磺胆酸钠协同转运多肽：从生物学功能到治疗潜力

乙型肝炎病毒（HBV）感染是一个世界性的健康问题，慢性感染可通过复杂的机制引起从肝纤维化到肝细胞癌（HCC）等多种疾病。目前，HBV感染的治疗主要依靠干扰素（IFNs）和核苷酸类似物（NAs）；但是，两者都有一些限制。2012年，牛磺胆酸钠协同转运多肽（NTCP）被确定为HBV的进入受体。基于这一突破性发现，一系列分子已逐渐开发和评估，以发现针对 NTCP 的新型进入抑制剂。然而，到目前为止，只有两种大分子被用于潜在的临床应用。在这个观点中，我们专注于总结传达 NTCP 生物学功能的结构特征，

更新日期：2022-09-15

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南