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Information on EC 2.7.1.1 - hexokinase and Organism(s) Plasmodium falciparum and UniProt Accession Q02155

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IUBMB Comments
D-Glucose, D-mannose, D-fructose, sorbitol and D-glucosamine can act as acceptors; ITP and dATP can act as donors. The liver isoenzyme has sometimes been called glucokinase.
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This record set is specific for:
Plasmodium falciparum
UNIPROT: Q02155
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The taxonomic range for the selected organisms is: Plasmodium falciparum
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Synonyms
hexokinase, hexokinase ii, hexokinase 2, hexokinase i, hk ii, hxk, liver glucokinase, hexokinase 1, hexokinase-2, hkdc1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ATP-D-hexose 6-phosphotransferase
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-
-
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ATP-dependent hexokinase
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-
-
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brain form hexokinase
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-
-
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glucokinase
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-
-
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glucose ATP phosphotransferase
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-
-
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hexokinase (phosphorylating)
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-
-
-
hexokinase D
-
-
-
-
hexokinase PI
-
-
-
-
hexokinase PII
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-
-
-
hexokinase type IV
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-
-
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hexokinase type IV glucokinase
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-
-
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hexokinase, tumor isozyme
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-
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HK
-
-
-
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HK4
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-
-
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HXK
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-
-
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kinase, hexo- (phosphorylating)
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-
-
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muscle form hexokinase
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-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
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-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:D-hexose 6-phosphotransferase
D-Glucose, D-mannose, D-fructose, sorbitol and D-glucosamine can act as acceptors; ITP and dATP can act as donors. The liver isoenzyme has sometimes been called glucokinase.
CAS REGISTRY NUMBER
COMMENTARY hide
9001-51-8
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + D-glucose
ADP + D-glucose 6-phosphate
show the reaction diagram
-
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + D-glucose
ADP + D-glucose 6-phosphate
show the reaction diagram
-
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R)-6-bromo-3-ethenyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
weak activity on hexokinase, 51% growth inhibition on asexual stage Plasmodium falciparum parasite
2-(4-chlorophenyl)-1,2-benzothiazol-3(2H)-one
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2-(4-chlorophenyl)-5-fluoro-1,2-benzothiazol-3(2H)-one
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2-phenyl-1,2-benzothiazol-3(2H)-one
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5-fluoro-N-phenyl-2-sulfanylbenzamide
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dimethyl 2-[[(2E)-3-(4-ethoxyphenyl)prop-2-enoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
among most potent inhibitors identified in screen, lacks activity against parasites
dimethyl 2-[[4-(3-methylphenoxy)butanoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
among most potent inhibitors identified in screen, lacks activity against parasites
2-deoxy-D-glucose
-
compound is nearly 2fold less toxic Plasmodium falciparum lines overexpressing hexokinase compared with control parasites. Although catalytic activity is higher in in overexpressing cells, they accumulate phospho-2-deoxy-D-glucose at the same rate as control parasites
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.098
D-glucose
pH and temperature not specified in the publication
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0274
(1R)-6-bromo-3-ethenyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Plasmodium falciparum
pH 7.9, 22°C
0.00027
2-(4-chlorophenyl)-1,2-benzothiazol-3(2H)-one
Plasmodium falciparum
pH and temperature not specified in the publication
0.00016
2-(4-chlorophenyl)-5-fluoro-1,2-benzothiazol-3(2H)-one
Plasmodium falciparum
pH and temperature not specified in the publication
0.00023
2-phenyl-1,2-benzothiazol-3(2H)-one
Plasmodium falciparum
pH and temperature not specified in the publication
0.0031
5-fluoro-N-phenyl-2-sulfanylbenzamide
Plasmodium falciparum
pH and temperature not specified in the publication
0.0011
dimethyl 2-[[(2E)-3-(4-ethoxyphenyl)prop-2-enoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
Plasmodium falciparum
pH 7.9, 22°C
0.0019
dimethyl 2-[[4-(3-methylphenoxy)butanoyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3,4-dicarboxylate
Plasmodium falciparum
pH 7.9, 22°C
0.00001
ebselen
Plasmodium falciparum
pH and temperature not specified in the publication
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
Plasmodium falciparum hexokinase is associated with the membrane via its C-terminal hydrophobic sequence, and this membrane association improves the efficiency of glucose phosphorylation immediately upon entering the host cell. Plasmodium hexokinase ensures a dramatic increase in reduced glutathione production in infected erythrocytes
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
a green fluorescent protein-labelled hexokinase shows the GFP fluorescence diffusely throughout the cytosol
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug target
given the absence of energy stores in this parasite and the key role of the Plasmodium falciparum hexose transporter, the pathway involving Plasmodium falciparum hexokinase and the bifunctional glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase is promising as a pharmacotherapeutic target, particularly because Plasmodium falciparum hexokinase shows a low sequence identity with human hexokinases
metabolism
Plasmodium falciparum hexokinase activity is important for the NADPH-dependent reduction of oxidized glutathione in the parasite by providing glucose-6-phosphate, which allows glucose-6-phosphate dehydrogenase to generate NADPH for downstream redox reactions
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
HXK_PLAFA
493
0
55346
Swiss-Prot
other Location (Reliability: 1)
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
high-throughput assay for screening small molecule collections to identify inhibitors of the Plasmodium falciparum hexokinase. The assay employs an ADP-GloTM reporter system in a 1536-well plate format, is robust with a signal-to-background of 3.4, a percent coefficient of variation of 6.8 and a Z'-factor of 0.75
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Davis, M.I.; Patrick, S.; Blanding, W.M.; Dwivedi, V.; Suryadi, J.; Golden, J.E.; Coussens, N.P.; Lee, O.W.; Shen, M.; Boxer, M.B.; Hall, M.D.; Sharlow, E.R.; Drew, M.E.; Morris, J.C.
Identification of novel Plasmodium falciparum hexokinase inhibitors with anti-parasitic activity
Antimicrob. Agents Chemother.
60
6023-6033
2016
Plasmodium falciparum (Q02155), Plasmodium falciparum
Manually annotated by BRENDA team
Tjhin, E.T.; Staines, H.M.; van Schalkwyk, D.A.; Krishna, S.; Saliba, K.J.
Studies with the Plasmodium falciparum hexokinase reveal that PfHT limits the rate of glucose entry into glycolysis
FEBS Lett.
587
3182-3187
2013
Plasmodium falciparum
Manually annotated by BRENDA team
Heneberg, P.
Redox regulation of hexokinases
Antioxid. Redox Signal.
30
415-442
2019
Oryctolagus cuniculus, Trypanosoma brucei, Mus musculus (P17710), Homo sapiens (P19367), Homo sapiens (P52789), Homo sapiens (P52790), Plasmodium falciparum (Q02155)
Manually annotated by BRENDA team