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TitleStructural insights into constitutive activity of 5-HT receptor.
Journal, issue, pagesProc Natl Acad Sci U S A, Vol. 120, Issue 14, Page e2209917120, Year 2023
Publish dateApr 4, 2023
AuthorsLicong He / Qiaoyu Zhao / Jianzhong Qi / Yifan Wang / Wenyu Han / Zhangcheng Chen / Yao Cong / Sheng Wang /
PubMed AbstractWhile most therapeutic research on G-protein-coupled receptors (GPCRs) focuses on receptor activation by (endogenous) agonists, significant therapeutic potential exists through agonist-independent ...While most therapeutic research on G-protein-coupled receptors (GPCRs) focuses on receptor activation by (endogenous) agonists, significant therapeutic potential exists through agonist-independent intrinsic constitutive activity that can occur in various physiological and pathophysiological settings. For example, inhibiting the constitutive activity of 5-HTR-a receptor that is found almost exclusively in the brain and mediates excitatory neurotransmission-has demonstrated a therapeutic effect on cognitive/memory impairment associated with several neuropsychiatric disorders. However, the structural basis of such constitutive activity remains unclear. Here, we present a cryo-EM structure of serotonin-bound human 5-HTR-Gs heterotrimer at 3.0-Å resolution. Detailed analyses of the structure complemented by comprehensive interrogation of signaling illuminate key structural determinants essential for constitutive 5-HTR activity. Additional structure-guided mutagenesis leads to a nanobody mimic Gαs for 5-HTR that can reduce its constitutive activity. Given the importance of 5-HTR for a large number of neuropsychiatric disorders, insights derived from these studies will accelerate the design of more effective medications, and shed light on the molecular basis of constitutive activity.
External linksProc Natl Acad Sci U S A / PubMed:36989299 / PubMed Central
MethodsEM (single particle)
Resolution3.0 Å
Structure data

34073

7ys6

EMDB-34073, PDB-7ys6:
Cryo-EM structure of the Serotonin 6 (5-HT6) receptor-DNGs-scFv16 complex
Method: EM (single particle) / Resolution: 3.0 Å

Chemicals

ChemComp-SRO:
SEROTONIN / neurotransmitter*YM / Serotonin

Source
  • homo sapiens (human)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / GPCR / serotonin receptor / 5-HT6R / cryo-EM / constitutive activity

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