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Structure paper

TitleStructural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog.
Journal, issue, pagesMol. Pharmacol., Vol. 85, Page 237-248, Year 2014
Publish dateJun 18, 2013 (structure data deposition date)
AuthorsHoman, K.T. / Wu, E. / Wilson, M.W. / Singh, P. / Larsen, S.D. / Tesmer, J.J.
External linksMol. Pharmacol. / PubMed:24220010
MethodsX-ray diffraction
Resolution2.32 - 2.4 Å
Structure data

PDB-4l9i:
Bovine G Protein Coupled Receptor Kinase 1 in Complex with Paroxetine
Method: X-RAY DIFFRACTION / Resolution: 2.32 Å

PDB-4mk0:
Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

Chemicals

ChemComp-8PR:
Paroxetine / antidepressant, inhibitor*YM

ChemComp-MES:
2-(N-MORPHOLINO)-ETHANESULFONIC ACID / pH buffer*YM

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-GOL:
GLYCEROL

ChemComp-29X:
5-{[(3S,4R)-4-(4-fluorophenyl)piperidin-3-yl]methoxy}-1H-isoindol-1-one

Source
  • bos taurus (cattle)
  • homo sapiens (human)
KeywordsTransferase / membrane protein/inhibitor / AGC family kinase / SER/THR KINASE / RGS HOMOLOGY DOMAIN / G PROTEIN COUPLED RECEPTOR KINASE / GRK / GRK1 / RHODOPSIN KINASE / SSRI / HYDROLYASE / GPCR / PHOSPHORYLATION / membrane protein-inhibitor complex / SIGNALING PROTEIN/inhibitor / INHIBITOR COMPLEX / PROTEIN KINASE / HYDROLASE / ATP BINDING / PERIPHERAL MEMBRANE PROTEIN / SIGNALING PROTEIN-inhibitor complex

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