Structure of PDB 5v4w Chain A

Receptor sequence
>5v4wA (length=419) Species: 9606 (Homo sapiens) [Search protein sequence]
LPQPNSQVEQILAEFQLQEEDLKKVMRRMQKEMDRGLRLETHEEASVKML
PTYVRSTPEGSEVGDFLSLDLGGTNFRVMLVKVGEWSVKTKHQMYSIPED
AMTGTAEMLFDYISECISDFLDKHQMKHKKLPLGFTFNVVGLLRDAIKRR
GDFEMDVVAMVNDTVATMISCYYEDHQCEVGMIVGTGCNACYMEEMQNVE
LVEGDEGRMCVNTEWGAFGDSGELDEFLLEYDRLVDESSANPGQQLYEKL
IGGKYMGELVRLVLLRLVDENLLFHGEASEQLRTRGAFETRFVSQVESDT
GDRKQIYNILSTLGLRPSTTDCDIVRRACESVSTRAAHMCSAGLAGVINR
MRESRVMRITVGVDGSVYKLHPSFKERFHASVRRLTPSCEITFIESEEGS
GRGAALVSAVACKKACMLG
3D structure
PDB5v4w Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators.
ChainA
Resolution2.39 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) R85 D205
Catalytic site (residue number reindexed from 1) R77 D163
Enzyme Commision number 2.7.1.1: hexokinase.
Interaction with ligand
Site
#
Ligand Ligand
chain
Binding residues on receptor
(original residue number in PDB)
Binding residues on receptor
(residue number reindexed from 1)
Binding affinity
BS01 GLC A N204 D205 N231 E256 E290 N162 D163 N189 E214 E248
BS02 8WM A Y61 V62 R63 S64 P66 W99 Y214 H218 K458 K459 Y53 V54 R55 S56 P58 W86 Y172 H176 K413 K414 BindingDB: EC50=40nM
Gene Ontology
Molecular Function
GO:0004340 glucokinase activity
GO:0004396 hexokinase activity
GO:0005515 protein binding
GO:0005524 ATP binding
GO:0005536 D-glucose binding
GO:0008865 fructokinase activity
GO:0016301 kinase activity
GO:0016773 phosphotransferase activity, alcohol group as acceptor
GO:0019158 mannokinase activity
GO:0141089 glucose sensor activity
Biological Process
GO:0001678 intracellular glucose homeostasis
GO:0005975 carbohydrate metabolic process
GO:0006006 glucose metabolic process
GO:0006007 glucose catabolic process
GO:0006096 glycolytic process
GO:0006110 regulation of glycolytic process
GO:0006739 NADP metabolic process
GO:0009749 response to glucose
GO:0016310 phosphorylation
GO:0019318 hexose metabolic process
GO:0032024 positive regulation of insulin secretion
GO:0032869 cellular response to insulin stimulus
GO:0042593 glucose homeostasis
GO:0043266 regulation of potassium ion transport
GO:0044320 cellular response to leptin stimulus
GO:0045721 negative regulation of gluconeogenesis
GO:0045725 positive regulation of glycogen biosynthetic process
GO:0046835 carbohydrate phosphorylation
GO:0050796 regulation of insulin secretion
GO:0051156 glucose 6-phosphate metabolic process
GO:0061621 canonical glycolysis
GO:0070509 calcium ion import
GO:1901135 carbohydrate derivative metabolic process
Cellular Component
GO:0005634 nucleus
GO:0005654 nucleoplasm
GO:0005737 cytoplasm
GO:0005739 mitochondrion
GO:0005829 cytosol

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Molecular Function

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Biological Process

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Cellular Component
External links
PDB RCSB:5v4w, PDBe:5v4w, PDBj:5v4w
PDBsum5v4w
PubMed28512030
UniProtP35557|HXK4_HUMAN Hexokinase-4 (Gene Name=GCK)

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