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Structure paper

TitleA GPCR-G protein-β-arrestin megacomplex enabled by a versatile allosteric modulator.
Journal, issue, pagesCell, Vol. 189, Issue 5, Page 1434-1450.e22, Year 2026
Publish dateMar 5, 2026
AuthorsGuodong He / Qinxin Sun / Xinyu Xu / Fang Kong / Shuhao Zhang / Kexin Ye / Xiaoou Sun / Bin Lin / Xin Chen / Chuangye Yan / Xiangyu Liu /
PubMed AbstractApproximately one-third of clinical drugs mediate their therapeutic effects through G protein-coupled receptors (GPCRs), highlighting their immense therapeutic relevance. Novel approaches to modulate ...Approximately one-third of clinical drugs mediate their therapeutic effects through G protein-coupled receptors (GPCRs), highlighting their immense therapeutic relevance. Novel approaches to modulate GPCR activity have the potential to yield unique pharmacological profiles. Conventionally, the G protein and β-arrestin signaling pathways downstream of GPCRs have been viewed as mutually exclusive. Using the in-house developed survival pressure selection (SPS) method, a high-throughput platform for GPCR agonist discovery, we identified an allosteric ligand that stabilizes a GPCR-G protein-β-arrestin megacomplex, thereby mediating sustained receptor signaling following internalization. Remarkably, this compound, atazanavir, exhibits pan-receptor activation across multiple family A GPCRs, including GPR119, βAR, and βAR, demonstrating the broad applicability of this regulatory mechanism. This discovery uncovers a distinct mechanism of GPCR regulation, opening alternative avenues for the development of therapeutics targeting GPCRs.
External linksCell / PubMed:41605208
MethodsEM (single particle)
Resolution3.22 - 3.33 Å
Structure data

62880

9l80

EMDB-62880, PDB-9l80:
Structure of GPR119-Gs complex bound to an allosteric modulator
Method: EM (single particle) / Resolution: 3.33 Å

62884

9l84

EMDB-62884, PDB-9l84:
Structure of beta1-AR-Gs complex bound to epinephrine and an allosteric modulator
Method: EM (single particle) / Resolution: 3.22 Å

62885

9l8l

EMDB-62885, PDB-9l8l:
Structure of GPCR megacomplex bound to agonists
Method: EM (single particle) / Resolution: 3.22 Å

Chemicals

ChemComp-DR7:
(3S,8S,9S,12S)-3,12-BIS(1,1-DIMETHYLETHYL)-8-HYDROXY-4,11-DIOXO-9-(PHENYLMETHYL)-6-[[4-(2-PYRIDINYL)PHENYL]METHYL]-2,5,

ChemComp-ALE:
L-EPINEPHRINE

ChemComp-P0G:
8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one

Source
  • homo sapiens (human)
  • rattus norvegicus (Norway rat)
  • bos taurus (domestic cattle)
  • lama glama (llama)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / GPCR

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