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Structure paper

TitleCyclic peptide inhibitors function as molecular glues to stabilize Gq/11 heterotrimers.
Journal, issue, pagesProc. Natl. Acad. Sci. USA, Vol. 122, Page e2418398122-e2418398122, Year 2025
Publish dateAug 31, 2023 (structure data deposition date)
AuthorsMuhle, J. / Alenfelder, J. / Rodrigues, M.J. / Jurgenliemke, L. / Guixa-Gonzalez, R. / Gratz, L. / Andres, F. / Bacchin, A. / Hennig, M. / Schihada, H. ...Muhle, J. / Alenfelder, J. / Rodrigues, M.J. / Jurgenliemke, L. / Guixa-Gonzalez, R. / Gratz, L. / Andres, F. / Bacchin, A. / Hennig, M. / Schihada, H. / Crusemann, M. / Konig, G.M. / Schertler, G. / Kostenis, E. / Deupi, X.
External linksProc. Natl. Acad. Sci. USA / PubMed:40333756
MethodsX-ray diffraction
Resolution1.43 - 1.7 Å
Structure data

PDB-8qeg:
Crystal structure of the G11 protein heterotrimer bound to YM-254890 inhibitor
Method: X-RAY DIFFRACTION / Resolution: 1.7 Å

PDB-8qeh:
Crystal structure of the G11 protein heterotrimer bound to FR900359 inhibitor
Method: X-RAY DIFFRACTION / Resolution: 1.43 Å

Chemicals

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

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-DAM:
N-METHYL-ALPHA-BETA-DEHYDROALANINE

ChemComp-HF2:
(2R)-2-hydroxy-3-phenylpropanoic acid

ChemComp-THC:
N-METHYLCARBONYLTHREONINE

ChemComp-OTH:
N,O-dimethyl-L-threonine

ChemComp-HL2:
(2S,3R)-2-amino-3-hydroxy-4-methylpentanoic acid

ChemComp-MAA:
N-methyl-L-alanine

ChemComp-ALA:
ALANINE

ChemComp-ACE:
ACETYL GROUP

ChemComp-HOH:
WATER

ChemComp-ZN:
Unknown entry

ChemComp-CL:
Unknown entry


ChemComp, No image

ChemComp-UDL:
Unknown entry

ChemComp-PPI:
PROPANOIC ACID

ChemComp-DMS:
DIMETHYL SULFOXIDE / DMSO, precipitant*YM

Source
  • homo sapiens (human)
KeywordsSIGNALING PROTEIN / G protein / YM-254890 / cell signaling / GNA11 / GNB1 / GNG2 / G alpha 11 / FR900359

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