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

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.

SUBMITTER: Wang Q

PROVIDER: S-EPMC7909583 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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

Wang Qing Q Zhou Yu Y Huang Jianhui J Huang Niu N

Pharmaceuticals (Basel, Switzerland) 20210120 2

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 ...[more]

PMID: 33498477

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