4isf Summary


Human glucokinase in complex with novel activator (2S)-3-cyclohexyl-2-(6-fluoro-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-N-(1,3-thiazol-2-yl)propanamide

The structure was published by Cheruvallath, Z.S., Gwaltney, S.L., Sabat, M., et al., Hosfield, D., Lee, B., and Wu, Y., in 2013 in a paper entitled "Design, synthesis and SAR of novel glucokinase activators." (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.09 Å and deposited in 2013.

The experimental data on which the structure is based was also deposited.

The PDB entry contains the structure of Glucokinase. This molecule has the UniProt identifier P35557 (HXK4_HUMAN)search. The sample contained 458 residues which is 97% of the natural sequence. Out of 458 residues 427 were observed and are deposited in the PDB.

It also contains one or more heterogenic compounds (e.g., ligands, co-factors, ions, modified amino acids, etc.); see here for a complete list.

The molecule is most likely monomeric.

The following tables show cross-reference information to other databases (to obtain a list of all PDB entries sharing the same property or classification, click on the magnifying glass icon):

Chain Name UniProt Name of source organism % of UniProt sequence present in the sample Residues in the sample molecules % of residues observed
A Glucokinase P35557 (16-465) (HXK4_HUMAN)search Homo sapienssearch 97% 458 93%

This entry contains 1 unique UniProt protein:

UniProt accession Name Organism PDB
P35557 (16 - 465) Glucokinase Homo sapiens

Chain Sequence family (Pfam)
A (P35557) PF00349: Hexokinasesearch, PF03727: Hexokinasesearch

Chain ID Molecular function (GO) Biological process (GO) Cellular component (GO)
A (P35557) phosphotransferase activity, alcohol group as acceptorsearch ATP bindingsearch hexokinase activitysearch glucose bindingsearch mannokinase activitysearch ADP bindingsearch glucokinase activitysearch catalytic activitysearch protein bindingsearch protein phosphatase bindingsearch nucleotide bindingsearch fructokinase activitysearch kinase activitysearch magnesium ion bindingsearch transferase activitysearch carbohydrate metabolic processsearch endocrine pancreas developmentsearch glucose metabolic processsearch cellular response to leptin stimulussearch metabolic processsearch glycolytic processsearch calcium ion importsearch regulation of insulin secretionsearch cellular response to insulin stimulussearch carbohydrate phosphorylationsearch positive regulation of glycolytic processsearch transmembrane transportsearch phosphorylationsearch negative regulation of epinephrine secretionsearch positive regulation of insulin secretionsearch fructose 2,6-bisphosphate metabolic processsearch positive regulation of phosphorylationsearch positive regulation of glycogen biosynthetic processsearch detection of glucosesearch hexose transportsearch cellular response to glucose starvationsearch NADP metabolic processsearch cellular glucose homeostasissearch positive regulation of cytosolic calcium ion concentrationsearch regulation of glucose transportsearch glucose transportsearch glycogen biosynthetic processsearch regulation of potassium ion transportsearch glucose 6-phosphate metabolic processsearch regulation of glycolytic processsearch glucose homeostasissearch small molecule metabolic processsearch negative regulation of gluconeogenesissearch second-messenger-mediated signalingsearch response to glucosesearch nucleoplasmsearch cell cortexsearch nucleussearch cytoplasmsearch cytosolsearch mitochondrionsearch secretory granulesearch

Chain InterPro annotation
A Hexokinasesearch Hexokinase, conserved sitesearch Hexokinase, N-terminalsearch Hexokinase, C-terminalsearch