Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor
Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT<sub>2B</sub>R) in 1992, significant progress has been made in 5-HT<sub>2B</sub>R research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5...
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| Format: | Article |
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MDPI AG
2021-01-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/2/76 |
| _version_ | 1797409190265749504 |
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| author | Qing Wang Yu Zhou Jianhui Huang Niu Huang |
| author_facet | Qing Wang Yu Zhou Jianhui Huang Niu Huang |
| author_sort | Qing Wang |
| collection | DOAJ |
| description | Since the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT<sub>2B</sub>R) in 1992, significant progress has been made in 5-HT<sub>2B</sub>R research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT<sub>2B</sub>R. Emerging evidence has suggested that the 5-HT<sub>2B</sub>R 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<sub>2B</sub>R bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT<sub>2B</sub>R antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT<sub>2B</sub>R antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas. |
| first_indexed | 2024-03-09T04:10:46Z |
| format | Article |
| id | doaj.art-851db81cf5394b7198069ef9e1e76d17 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T04:10:46Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-851db81cf5394b7198069ef9e1e76d172023-12-03T14:01:04ZengMDPI AGPharmaceuticals1424-82472021-01-011427610.3390/ph14020076Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B ReceptorQing Wang0Yu Zhou1Jianhui Huang2Niu Huang3School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, ChinaNational Institute of Biological Sciences, No. 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, ChinaSchool of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, ChinaNational Institute of Biological Sciences, No. 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, ChinaSince the first characterization of the 5-hydroxytryptamine 2B receptor (5-HT<sub>2B</sub>R) in 1992, significant progress has been made in 5-HT<sub>2B</sub>R research. Herein, we summarize the biological function, structure, and small-molecule pharmaceutical ligands of the 5-HT<sub>2B</sub>R. Emerging evidence has suggested that the 5-HT<sub>2B</sub>R 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<sub>2B</sub>R bound with different ligands provided great insights into ligand recognition, activation mechanism, and biased signaling. Numerous 5-HT<sub>2B</sub>R antagonists have been discovered and developed, and several of them have advanced to clinical trials. It is expected that the novel 5-HT<sub>2B</sub>R antagonists with high potency and selectivity will lead to the development of first-in-class drugs in various therapeutic areas.https://www.mdpi.com/1424-8247/14/2/76GPCR5-HT<sub>2B</sub>Rbiased signalingagonistantagonist |
| spellingShingle | Qing Wang Yu Zhou Jianhui Huang Niu Huang Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor Pharmaceuticals GPCR 5-HT<sub>2B</sub>R biased signaling agonist antagonist |
| title | Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor |
| title_full | Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor |
| title_fullStr | Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor |
| title_full_unstemmed | Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor |
| title_short | Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor |
| title_sort | structure function and pharmaceutical ligands of 5 hydroxytryptamine 2b receptor |
| topic | GPCR 5-HT<sub>2B</sub>R biased signaling agonist antagonist |
| url | https://www.mdpi.com/1424-8247/14/2/76 |
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