Structural basis for recognition of anti-migraine drug lasmiditan by the serotonin receptor 5-HT1F-G protein complex
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.3The 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.
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The cryo-EM data were collected at the Cryo-Electron Microscopy Research Center,Shanghai Institute of Materia Medica,Chinese Academy of SciencesShanghai,China;This work was partially supported by the Ministry of Science and Technology of China;Strategic Priority Research Program of the Chinese Academy of Sciences;Shanghai Municipal Science and Technology Major Project;the National Natural Science Foundation of China;National Science&Technology Major Project"Key New Drug Creation and Manufacturing Program"
2021-10-13（万方平台首次上网日期，不代表论文的发表时间）
共3页
1036-1038
