The DOI matches its Crossref record; 175 of the 175 references it cites were found in a registry or an index.
Structure and function of serotonin G protein-coupled receptors
Open accessAbstract
Serotonin receptors are prevalent throughout the nervous system and the periphery, and remain one of the most lucrative and promising drug discovery targets for disorders ranging from migraine headaches to neuropsychiatric disorders such as schizophrenia and depression. There are 14 distinct serotonin receptors, of which 13 are G protein coupled receptors (GPCRs), which are targets for approximately 40% of the approved medicines. Recent crystallographic and biochemical evidence has provided a converging understanding of the basic structure and functional mechanics of GPCR activation. Currently, two GPCR crystal structures exist for the serotonin family, the 5-HT1B and 5-HT2B receptor, with the antimigraine and valvulopathic drug ergotamine bound. The first serotonin crystal structures not only provide the first evidence of serotonin receptor topography but also provide mechanistic explanations into functional selectivity or biased agonism. This review will detail the findings of these crystal structures from a molecular and mutagenesis perspective for driving rational drug design for novel therapeutics incorporating biased signaling.
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Cites
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Jiang, S.-H., Li, J., Dong, F.-Y., Yang, J.-Y., Liu, D.-J., Yang, X.-M., Wang, Y.-H., Yang, M.-W., Fu, X.-L., Zhang, X.-X., et al. (2017) · Gastroenterology · doi:10.1053/j.gastro.2017.03.008 · Cited by 288
The serotonergic system and cognitive function
Švob Štrac, D., Pivac, N., & Mück-Šeler, D. (2016) · Translational Neuroscience · doi:10.1515/tnsci-2016-0007 · Cited by 285
Psychedelics as anti-inflammatory agents
Flanagan, T. W., & Nichols, C. D. (2018) · International Review of Psychiatry · doi:10.1080/09540261.2018.1481827 · Cited by 267
Fang, Y., Ding, X., Zhang, Y., Cai, L., Ge, Y., Ma, K., Xu, R., Li, S., Song, M., Zhu, H., et al. (2022) · Journal of Neuroinflammation · doi:10.1186/s12974-022-02389-y · Cited by 96
Metadata
- Authors
- McCorvy, J. D., & Roth, B. L.
- Venue
- Pharmacology & Therapeutics
- Publisher
- Elsevier BV
- Published
- 2015-06
- Volume
- 150
- Pages
- 129-142
- ISSN
- 0163-7258 (ISSN-L)
- OpenAlex
- W2011312787
- Cited by
- 372
- References
- 175
- FWCI
- 10.29
- Type
- journal article
- Language
- en
- Open access
- green
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