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Structure paper

TitleOptimising pharmacokinetics of glucokinase activators with matched triplicate design sets the discovery of AZD3651 and AZD9485
Journal, issue, pagesTo be Published
Publish dateJan 24, 2013 (structure data deposition date)
AuthorsWaring, M.J. / Bennett, S.N. / Boyd, S. / Campbell, L. / Davies, R.D.M. / Ogg, D.J. / Hargreaves, D. / Martin, N.G. / Robb, G. / Wilkinson, S. ...Waring, M.J. / Bennett, S.N. / Boyd, S. / Campbell, L. / Davies, R.D.M. / Ogg, D.J. / Hargreaves, D. / Martin, N.G. / Robb, G. / Wilkinson, S. / MacPaul, P. / Wood, J.M.
External linksSearch PubMed
MethodsX-ray diffraction
Resolution2.1 Å
Structure data

PDB-4iwv:
Crystals structure of Human Glucokinase in complex with small molecule activator
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

Chemicals

ChemComp-NA:
Unknown entry

ChemComp-GLC:
alpha-D-glucopyranose

ChemComp-1J9:
(2S)-2-{[1-(2-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]oxy}-N-(5-chloropyridin-2-yl)-3-(2-hydroxyethoxy)propanamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Allosteric Site / Catalysis / Enzyme Activation / Gene Expression Regulation / Glucokinase / Glucose / Homeostasis / Humans / Hypoglycemia / Kinetics / Biological / Models / Molecular / Mutation / Protein Conformation / Scattering / Radiation / X-Rays / TRANSFERASE-TRANSFERASE INHIBITOR complex

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