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
/
Revised: 18 January 2021
/
Accepted: 19 January 2021
/
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.
View Full-Text
Keywords:
GPCR; 5-HT2BR; biased signaling; agonist; antagonist
▼
Show Figures
Graphical abstract
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
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
Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.
