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Structure paper

TitleGPCR activation and GRK2 assembly by a biased intracellular agonist.
Journal, issue, pagesNature, Vol. 620, Issue 7974, Page 676-681, Year 2023
Publish dateAug 2, 2023
AuthorsJia Duan / Heng Liu / Fenghui Zhao / Qingning Yuan / Yujie Ji / Xiaoqing Cai / Xinheng He / Xinzhu Li / Junrui Li / Kai Wu / Tianyu Gao / Shengnan Zhu / Shi Lin / Ming-Wei Wang / Xi Cheng / Wanchao Yin / Yi Jiang / Dehua Yang / H Eric Xu /
PubMed AbstractPhosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated by biased ligands. The ...Phosphorylation of G-protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) desensitizes G-protein signalling and promotes arrestin signalling, which is also modulated by biased ligands. The molecular assembly of GRKs on GPCRs and the basis of GRK-mediated biased signalling remain largely unknown owing to the weak GPCR-GRK interactions. Here we report the complex structure of neurotensin receptor 1 (NTSR1) bound to GRK2, Gα and the arrestin-biased ligand SBI-553. The density map reveals the arrangement of the intact GRK2 with the receptor, with the N-terminal helix of GRK2 docking into the open cytoplasmic pocket formed by the outward movement of the receptor transmembrane helix 6, analogous to the binding of the G protein to the receptor. SBI-553 binds at the interface between GRK2 and NTSR1 to enhance GRK2 binding. The binding mode of SBI-553 is compatible with arrestin binding but clashes with the binding of Gα protein, thus providing a mechanism for its arrestin-biased signalling capability. In sum, our structure provides a rational model for understanding the details of GPCR-GRK interactions and GRK2-mediated biased signalling.
External linksNature / PubMed:37532940
MethodsEM (single particle)
Resolution2.81 - 3.07 Å
Structure data

36474

8jpb

EMDB-36474, PDB-8jpb:
cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1
Method: EM (single particle) / Resolution: 3.07 Å

36475

8jpc

EMDB-36475, PDB-8jpc:
cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 2
Method: EM (single particle) / Resolution: 3.07 Å

36476

8jpd

EMDB-36476, PDB-8jpd:
Focused refinement structure of GRK2 in NTSR1-GRK2-Galpha(q) complexes
Method: EM (single particle) / Resolution: 2.81 Å

36477

8jpe

EMDB-36477, PDB-8jpe:
Focused refinement structure of Galpha(q) in NTSR1-GRK2-Galpha(q) complexes
Method: EM (single particle) / Resolution: 2.91 Å

36478

8jpf

EMDB-36478, PDB-8jpf:
Focused refiment structure of NTSR1 in NTSR1-GRK2-Galpha(q) complexes
Method: EM (single particle) / Resolution: 3.02 Å

Chemicals

ChemComp-STU:
STAUROSPORINE / anticancer, antifungal, antibiotic, alkaloid*YM / Staurosporine

ChemComp-GDP:
GUANOSINE-5'-DIPHOSPHATE / GDP, energy-carrying molecule*YM / Guanosine diphosphate

ChemComp-MG:
Unknown entry

ChemComp-ALF:
TETRAFLUOROALUMINATE ION

ChemComp-SRW:
2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol

Source
  • homo sapiens (human)
  • bos taurus (cattle)
  • synthetic construct (others)
KeywordsSIGNALING PROTEIN / Biased signaling

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