Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor
1
School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China
2
National Institute of Biological Sciences, No. 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China
3
Tsinghua Institute of Multidisciplinary Biomedical Research, Tsinghua University, Beijing 102206, China
*
Author to whom correspondence should be addressed.
Academic Editor: Caroline Sevoz-Couche
Pharmaceuticals 2021, 14(2), 76; https://doi.org/10.3390/ph14020076
Received: 5 January 2021
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Revised: 18 January 2021
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Accepted: 19 January 2021
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Published: 20 January 2021
(This article belongs to the Special Issue Molecular Pharmacology of 5-HT Receptors)
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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Keywords:
GPCR; 5-HT2BR; biased signaling; agonist; antagonist
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MDPI and ACS Style
Wang, Q.; Zhou, Y.; Huang, J.; Huang, N. Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor. Pharmaceuticals 2021, 14, 76. https://doi.org/10.3390/ph14020076
AMA Style
Wang Q, Zhou Y, Huang J, Huang N. Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor. Pharmaceuticals. 2021; 14(2):76. https://doi.org/10.3390/ph14020076
Chicago/Turabian StyleWang, Qing, Yu Zhou, Jianhui Huang, and Niu Huang. 2021. "Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor" Pharmaceuticals 14, no. 2: 76. https://doi.org/10.3390/ph14020076
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