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TitleAntidiabetic effects of glucokinase regulatory protein small-molecule disruptors.
Journal, issue, pagesNature, Vol. 504, Page 437-440, Year 2013
Publish dateJul 30, 2013 (structure data deposition date)
AuthorsLloyd, D.J. / St Jean, D.J. / Kurzeja, R.J. / Wahl, R.C. / Michelsen, K. / Cupples, R. / Chen, M. / Wu, J. / Sivits, G. / Helmering, J. ...Lloyd, D.J. / St Jean, D.J. / Kurzeja, R.J. / Wahl, R.C. / Michelsen, K. / Cupples, R. / Chen, M. / Wu, J. / Sivits, G. / Helmering, J. / Komorowski, R. / Ashton, K.S. / Pennington, L.D. / Fotsch, C. / Vazir, M. / Chen, K. / Chmait, S. / Zhang, J. / Liu, L. / Norman, M.H. / Andrews, K.L. / Bartberger, M.D. / Van, G. / Galbreath, E.J. / Vonderfecht, S.L. / Wang, M. / Jordan, S.R. / Veniant, M.M. / Hale, C.
External linksNature / PubMed:24226772
MethodsX-ray diffraction
Resolution2.35 Å
Structure data

PDB-4ly9:
Human GKRP complexed to AMG-1694 [(2R)-1,1,1-trifluoro-2-{4-[(2S)-2-{[(3S)-3-methylmorpholin-4-yl]methyl}-4-(thiophen-2-ylsulfonyl)piperazin-1-yl]phenyl}propan-2-ol] and sorbitol-6-phosphate
Method: X-RAY DIFFRACTION / Resolution: 2.35 Å

Chemicals

ChemComp-IOD:
IODIDE ION

ChemComp-S6P:
D-SORBITOL-6-PHOSPHATE

ChemComp-1YY:
(2R)-1,1,1-trifluoro-2-{4-[(2S)-2-{[(3S)-3-methylmorpholin-4-yl]methyl}-4-(thiophen-2-ylsulfonyl)piperazin-1-yl]phenyl}propan-2-ol

ChemComp-GOL:
GLYCEROL

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsCarbohydrate Binding protein / Regulatory protein / disruptor ligand complex / SIS domains / GKRP binds to GK / Liver

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