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Preparation and Delivery of Protein Microcrystals in Lipidic Cubic Phase for Serial Femtosecond Crystallography
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Structure, Function, and Pharmaceutical Ligands of 5-Hydroxytryptamine 2B Receptor.
Qing Wang1,2, Yu Zhou2, Jianhui Huang1
1School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
Pharmaceuticals (Basel, Switzerland)
|January 27, 2021
Summary
Research on the 5-hydroxytryptamine 2B receptor (5-HT2BR) has advanced significantly. New antagonists show promise for developing first-in-class drugs targeting various diseases.
Area of Science:
- Pharmacology and Molecular Biology
- G protein-coupled receptor (GPCR) research
- Drug discovery and development
Background:
- The 5-hydroxytryptamine 2B receptor (5-HT2BR) was first characterized in 1992.
- The 5-HT2BR plays a role in cardiovascular regulation, fibrosis, cancer, gastrointestinal function, and the nervous system.
Purpose of the Study:
- To summarize the current understanding of the 5-HT2BR.
- To review its biological functions, structural characteristics, and pharmaceutical ligands.
- To highlight the therapeutic potential of 5-HT2BR antagonists.
Main Methods:
- Review of existing scientific literature on 5-HT2BR.
- Analysis of eight crystal complex structures of 5-HT2BR with ligands.
- Summary of preclinical and clinical development of 5-HT2BR antagonists.
Main Results:
- The 5-HT2BR is involved in diverse physiological and pathological processes.
- Structural studies provide insights into ligand binding, receptor activation, and biased signaling.
- Several potent and selective 5-HT2BR antagonists have been developed, with some in clinical trials.
Conclusions:
- The 5-HT2BR is a promising drug target for multiple therapeutic areas.
- Development of novel, highly selective 5-HT2BR antagonists is expected to yield first-in-class therapeutics.
- Continued research into 5-HT2BR biology and pharmacology is crucial for advancing drug development.
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