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Structure paper

TitleStructure of GPR101-Gs enables identification of ligands with rejuvenating potential.
Journal, issue, pagesNat Chem Biol, Vol. 20, Issue 4, Page 484-492, Year 2024
Publish dateNov 9, 2023
AuthorsZhao Yang / Jun-Yan Wang / Fan Yang / Kong-Kai Zhu / Guo-Peng Wang / Ying Guan / Shang-Lei Ning / Yan Lu / Yu Li / Chao Zhang / Yuan Zheng / Shu-Hua Zhou / Xin-Wen Wang / Ming-Wei Wang / Peng Xiao / Fan Yi / Cheng Zhang / Peng-Ju Zhang / Fei Xu / Bao-Hua Liu / Hua Zhang / Xiao Yu / Ning Gao / Jin-Peng Sun /
PubMed AbstractGPR101 is an orphan G protein-coupled receptor actively participating in energy homeostasis. Here we report the cryo-electron microscopy structure of GPR101 constitutively coupled to Gs heterotrimer, ...GPR101 is an orphan G protein-coupled receptor actively participating in energy homeostasis. Here we report the cryo-electron microscopy structure of GPR101 constitutively coupled to Gs heterotrimer, which reveals unique features of GPR101, including the interaction of extracellular loop 2 within the 7TM bundle, a hydrophobic chain packing-mediated activation mechanism and the structural basis of disease-related mutants. Importantly, a side pocket is identified in GPR101 that facilitates in silico screening to identify four small-molecule agonists, including AA-14. The structure of AA-14-GPR101-Gs provides direct evidence of the AA-14 binding at the side pocket. Functionally, AA-14 partially restores the functions of GH/IGF-1 axis and exhibits several rejuvenating effects in wild-type mice, which are abrogated in Gpr101-deficient mice. In summary, we provide a structural basis for the constitutive activity of GPR101. The structure-facilitated identification of GPR101 agonists and functional analysis suggest that targeting this orphan receptor has rejuvenating potential.
External linksNat Chem Biol / PubMed:37945893
MethodsEM (single particle)
Resolution2.89 - 3.3 Å
Structure data

37356

8w8q

EMDB-37356, PDB-8w8q:
Cryo-EM structure of the GPR101-Gs complex
Method: EM (single particle) / Resolution: 2.89 Å

37357

8w8r

EMDB-37357, PDB-8w8r:
Cryo-EM structure of the AA-14-bound GPR101-Gs complex
Method: EM (single particle) / Resolution: 3.3 Å

37358

8w8s

EMDB-37358, PDB-8w8s:
Cryo-EM structure of the AA14-bound GPR101 complex
Method: EM (single particle) / Resolution: 3.3 Å

Chemicals

ChemComp-U7D:
1-(4-methylpyridin-2-yl)-3-[3-(trifluoromethyl)phenyl]thiourea

Source
  • homo sapiens (human)
  • escherichia coli (E. coli)
KeywordsMEMBRANE PROTEIN / GPCR / orphan receptor / GPR101 / constitutive activity / cryo-EM / structural protein

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