Structure of PDB 5v4x Chain A
Receptor sequence
>5v4xA (length=420) Species:
9606
(Homo sapiens) [
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KPMPLTLVEQILAEFQLQEEDLKKVMRRMQKEMDRGLRLETHEEASVKML
PTYVRSTPEGSEVGDFLSLDLGGTNFRVMLVKVGEWSVKTKHQMYSIPED
AMTGTAEMLFDYISECISDFLDKHQMKHKKLPLGFTFNNVVGLLRDAIKR
RGDFEMDVVAMVNDTVATMISCYYEDHQCEVGMIVGTGCNACYMEEMQNV
ELVEGDEGRMCVNTEWGAFGDSGELDEFLLEYDRLVDESSANPGQQLYEK
LIGGKYMGELVRLVLLRLVDENLLFHGEASEQLRTRGAFETRFVSQVESD
TGDRKQIYNILSTLGLRPSTTDCDIVRRACESVSTRAAHMCSAGLAGVIN
RMRESRVMRITVGVDGSVYKLHPSFKERFHASVRRLTPSCEITFIESEEG
SGRGAALVSAVACKKACMLG
3D structure
PDB
5v4x
Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators.
Chain
A
Resolution
2.08 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 D164
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 I225 N231 E256 E290
N163 D164 I184 N190 E215 E249
BS02
8WJ
A
Y61 V62 R63 S64 T65 P66 E67 W99 M210 Y214 K458 K459
Y53 V54 R55 S56 T57 P58 E59 W86 M169 Y173 K414 K415
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
View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB
RCSB:5v4x
,
PDBe:5v4x
,
PDBj:5v4x
PDBsum
5v4x
PubMed
28512030
UniProt
P35557
|HXK4_HUMAN Hexokinase-4 (Gene Name=GCK)
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