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

Overview

Journal Pharmaceuticals (Basel)

Publisher MDPI

Specialty Chemistry

Date 2021 Jan 27

PMID 33498477

Citations 3

Authors

Qing Wang

Yu Zhou

Jianhui Huang

Niu Huang

Affiliations

Soon will be listed here.

Abstract

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

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