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Structure paper

TitleIdentification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors.
Journal, issue, pagesAcs Chem. Biol., Vol. 10, Page 310-319, Year 2015
Publish dateMay 23, 2014 (structure data deposition date)
AuthorsHoman, K.T. / Larimore, K.M. / Elkins, J.M. / Szklarz, M. / Knapp, S. / Tesmer, J.J.
External linksAcs Chem. Biol. / PubMed:25238254
MethodsX-ray diffraction
Resolution1.85 - 2.56 Å
Structure data

PDB-4pni:
Bovine G protein-coupled receptor kinase 1 in complex with GSK2163632A
Method: X-RAY DIFFRACTION / Resolution: 1.85 Å

PDB-4pnk:
G protein-coupled receptor kinase 2 in complex with GSK180736A
Method: X-RAY DIFFRACTION / Resolution: 2.56 Å

Chemicals

ChemComp-KQQ:
3-[(2-{[1-(N,N-dimethylglycyl)-6-methoxy-4,4-dimethyl-1,2,3,4-tetrahydroquinolin-7-yl]amino}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]thiophene-2-carboxamide

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-KZQ:
(4S)-4-(4-fluorophenyl)-N-(2H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

Source
  • bos taurus (domestic cattle)
  • homo sapiens (human)
KeywordsTransferase/Transferase inhibitor / AGC FAMILY KINASE / SER/THR KINASE / RGS HOMOLOGY DOMAIN / G PROTEIN COUPLED RECEPTOR KINASE / GRK / GRK1 / RHODOPSIN KINASE / HYDROLYASE / GPCR / PHOSPHORYLATION / Transferase-Transferase inhibitor complex / PROTEIN KINASE / HYDROLASE / ATP BINDING / PERIPHERAL MEMBRANE PROTEIN

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