Volume 31, No 9, Sep 2021

ISSN: 1001-0602 
EISSN: 1748-7838 2018 
impact factor 17.848* 
(Clarivate Analytics, 2019)

Volume 31 Issue 9, September 2021: 1036-1038

LETTERS TO THE EDITOR

Structural basis for recognition of anti-migraine drug lasmiditan by the serotonin receptor 5-HT1F–G protein complex

Sijie Huang^1,2,3,† , Peiyu Xu^1,2,† , Yangxia Tan^1,2,† , Chongzhao You^1,2 , Yumu Zhang^1,2,3 , Yi Jiang^1,2,* , H. Eric Xu^1,2,3,*

¹The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China
²University of Chinese Academy of Sciences, Beijing, China
³School of Life Science and Technology, ShanghaiTech University, Shanghai, China
^†These authors contributed equally: Sijie Huang, Peiyu Xu, Yangxia Tan
Correspondence: Yi Jiang(yijiang@simm.ac.cn)H. Eric Xu(eric.xu@simm.ac.cn)

Dear Editor,

The serotonin 5-HT1 receptor subtypes, including 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F, are G protein-coupled receptors (GPCRs) that respond to the endogenous neurotransmitter serotonin and couple preferentially to the Gi/o family of G proteins.1 Drugs targeting 5-HT1 receptors are used to treat migraine, depression, and schizophrenia.2 Clinical use of traditional anti-migraine drugs, triptans, caused side effects arising from therapeutic vasoconstrictive actions when targeting 5-HT1B/1D receptors.3 The requirement of new anti-migraine drugs without vasoconstrictive effects led to the development of lasmiditan, a highly selective 5-HT1F receptor agonist with minimized on-target side effects.4

https://doi.org/10.1038/s41422-021-00527-4

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