Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor.
Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor.
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5-羟色胺2B受体的结构、功能和药物配体
DOI：
10.3390/ph14020076
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发表时间：
2021-01-20
期刊：
影响因子：
--
通讯作者：
Huang N
中科院分区：
文献类型：
--
作者：
Wang Q;Zhou Y;Huang J;Huang N
自从1992年5-羟色胺2B受体(5-HT2BR)首次被鉴定以来，5-HT2BR的研究取得了重大进展。本文就5-HT2BR的生物学功能、结构和小分子药物配体作一综述。新的证据表明，5-HT2BR与心血管系统、纤维化疾病、癌症、胃肠道和神经系统的调节有关。与不同配体结合的5-HT2BR的8个晶体络合物结构为配体识别、激活机制和偏向信号转导提供了重要的信息。已经发现和开发了许多5-HT2BR拮抗剂，其中一些已经进入临床试验。具有高效、高选择性的新型5-HT2BR拮抗剂有望在不同的治疗领域开发出一流的药物。
Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT2BR) in 1992, significant progress has been made in 5-HT2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT2BR. Emerging evidence has suggested that the 5-HT2BR is implicated in the regulation of the cardiovascular system, fibrosis disorders, cancer, the gastrointestinal (GI) tract, and the nervous system. Eight crystal complex structures of the 5-HT2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT2BR antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT2BR antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas.
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DOI：
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影响因子：
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