Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

Qing Wang; Yu Zhou; Jianhui Huang; Niu Huang

doi:10.3390/ph14020076

Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor

Pharmaceuticals (Basel). 2021 Jan 20;14(2):76. doi: 10.3390/ph14020076.

Authors

Qing Wang^{1

2}, Yu Zhou², Jianhui Huang¹, Niu Huang^{2

3}

Affiliations

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.

Abstract

Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT_2BR) in 1992, significant progress has been made in 5-HT_2BR research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT_2BR. Emerging evidence has suggested that the 5-HT_2BR 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-HT_2BR bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT_2BR antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT_2BR antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas.

Keywords: 5-HT2BR; GPCR; agonist; antagonist; biased signaling.

Publication types

Review

Abstract

Publication types

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