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Structure paper

TitleStructures of human gastrin-releasing peptide receptors bound to antagonist and agonist for cancer and itch therapy.
Journal, issue, pagesProc Natl Acad Sci U S A, Vol. 120, Issue 6, Page e2216230120, Year 2023
Publish dateFeb 7, 2023
AuthorsShuman Peng / Yuting Zhan / Dongqi Zhang / Lu Ren / Anqi Chen / Zhou-Feng Chen / Haitao Zhang /
PubMed AbstractGastrin releasing peptide receptor (GRPR), a member of the bombesin (BBN) G protein-coupled receptors, is aberrantly overexpressed in several malignant tumors, including those of the breast, ...Gastrin releasing peptide receptor (GRPR), a member of the bombesin (BBN) G protein-coupled receptors, is aberrantly overexpressed in several malignant tumors, including those of the breast, prostate, pancreas, lung, and central nervous system. Additionally, it also mediates non-histaminergic itch and pathological itch conditions in mice. Thus, GRPR could be an attractive target for cancer and itch therapy. Here, we report the inactive state crystal structure of human GRPR in complex with the non-peptide antagonist PD176252, as well as two active state cryo-electron microscopy (cryo-EM) structures of GRPR bound to the endogenous peptide agonist gastrin-releasing peptide and the synthetic BBN analog [D-Phe, β-Ala, Phe, Nle] Bn (6-14), in complex with G heterotrimers. These structures revealed the molecular mechanisms for the ligand binding, receptor activation, and G proteins signaling of GRPR, which are expected to accelerate the structure-based design of GRPR antagonists and agonists for the treatments of cancer and pruritus.
External linksProc Natl Acad Sci U S A / PubMed:36724251 / PubMed Central
MethodsEM (single particle) / X-ray diffraction
Resolution2.952 - 3.0 Å
Structure data

32297

7w3z

EMDB-32297, PDB-7w3z:
Cryo-EM Structure of Human Gastrin Releasing Peptide Receptor in complex with the agonist Gastrin Releasing Peptide and Gq heterotrimers
Method: EM (single particle) / Resolution: 3.0 Å

32298

7w40

EMDB-32298, PDB-7w40:
Cryo-EM Structure of Human Gastrin Releasing Peptide Receptor in complex with the agonist Bombesin (6-14) [D-Phe6, beta-Ala11, Phe13, Nle14] and Gq heterotrimers
Method: EM (single particle) / Resolution: 3.0 Å

PDB-7w41:
Crystal Structure of Human Gastrin Releasing Peptide Receptor in complex with the antagonist PD176252
Method: X-RAY DIFFRACTION / Resolution: 2.952 Å

Chemicals

ChemComp-8B8:
(2S)-3-(1H-indol-3-yl)-N-[[1-(5-methoxypyridin-2-yl)cyclohexyl]methyl]-2-methyl-2-[(4-nitrophenyl)carbamoylamino]propanamide

Source
  • homo sapiens (human)
  • synthetic construct (others)
  • escherichia coli (E. coli)
  • pyrococcus abyssi ge5 (archaea)
KeywordsMEMBRANE PROTEIN / GPCR / Gastrin Releasing Peptide Receptor

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