Any feedback?
Information on EC 2.7.1.40 - pyruvate kinase and Organism(s) Staphylococcus aureus and UniProt Accession Q6GG09
for references in articles please use BRENDA:EC2.7.1.40Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
2.7.1.40 pyruvate kinaseIUBMB Comments
UTP, GTP, CTP, ITP and dATP can also act as donors. Also phosphorylates hydroxylamine and fluoride in the presence of CO2.
Specify your search results
Word Map
- 2.7.1.40
- hexokinase
-
phosphofructokinase
- erythrocyte
- fructose
- glucose-6-phosphate
- hepatocytes
- glycogen
- anemia
-
carboxykinase
-
gluconeogenesis
- aldolase
- pep
-
hemolytic
- malate
- citrate
- creatine
- glucokinase
- adenylate
- carboxylase
-
warburg
-
gluconeogenic
- enolase
- phosphoglycerate
- pentose
- 6-phosphate
-
malic
- glucagon
- glyceraldehyde-3-phosphate
- reticulocyte
-
lipogenesis
- 6-phosphogluconate
- fructose-1,6-bisphosphate
-
lipogenic
- 2,6-bisphosphate
- g6pase
-
1,6-bisphosphatase
-
liver-type
-
splenectomy
- hk2
- dikinase
-
glutaminolysis
-
calprotectin
- triose
- shikonin
- 2,3-diphosphoglycerate
- fructose-6-phosphate
-
glycogenolysis
- drug development
- medicine
- biofuel production
-
reticulocytosis
-
transfusion-dependent
-
spherocytosis
- nutrition
- diagnostics
The taxonomic range for the selected organisms is: Staphylococcus aureus
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
Synonyms
pyruvate kinase, m2-pk, pyruvate kinase m2, l-pk, pyk, tum2-pk, pyruvate kinase type m2, liver pyruvate kinase, pyruvate kinase m2 isoform, m2-pyruvate kinase, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
CTHBP
-
-
-
-
cytosolic thyroid hormone binding protein
-
-
-
-
fluorokinase
-
-
-
-
kinase, fluoro- (phosphorylating)
-
-
-
-
kinase, pyruvate (phosphorylating)
-
-
-
-
L-PK
-
-
-
-
phosphoenol transphosphorylase
-
-
-
-
phosphoenolpyruvate kinase
-
-
-
-
pyruvate kinase muscle isozyme
-
-
-
-
pyruvate phosphotransferase
-
-
-
-
pyruvic kinase
-
-
-
-
R-type/L-type pyruvate kinase
-
-
-
-
red cell/liver pyruvate kinase
-
-
-
-
THBP1
-
-
-
-
VEG17
-
-
-
-
vegetative protein 17
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospho group transfer
-
-
-
-
PATHWAY SOURCE
PATHWAYS
BRENDA
KEGG
-
-, -, -, -, -, -, -, -, -, -, -, -, -, -, -, -, -
SYSTEMATIC NAME
IUBMB Comments
ATP:pyruvate 2-O-phosphotransferase
UTP, GTP, CTP, ITP and dATP can also act as donors. Also phosphorylates hydroxylamine and fluoride in the presence of CO2.
CAS REGISTRY NUMBER
COMMENTARY
9001-59-6
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ATP
inhibition of full-length enzyme at concentration above 2.5 mM
D-fructose 1,6-bisphosphate
inhibition of full-length enzyme at 10 mM
(1S,3S)-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
-
-
(1S,3S)-2-bromo-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
-
-
(1S,3S)-2-chloro-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
-
-
(1S,4S)-6-chloro-1,4-bis(5-chloro-1H-indol-3-yl)-2,3,4,9-tetrahydro-1H-carbazole
-
-
(2-[(1E)-1-[2-(5-bromo-2-hydroxybenzoyl)hydrazinylidene]ethyl]-1-methyl-1H-indol-6-yl)dibromanium
-
-
(2E)-1,3-bis(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
6% inhibition at 0.001 mM
(2E)-1-(3-bromo-2-hydroxyphenyl)-3-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
41% inhibition at 0.001 mM
(2E)-1-(4-bromo-2-hydroxyphenyl)-3-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
-
(2E)-1-(5-bromo-1H-indol-2-yl)-3-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
21% inhibition at 0.001 mM
(2E)-1-(5-bromo-2-hydroxyphenyl)-3-(1H-indol-2-yl)prop-2-en-1-one
-
10% inhibition at 0.001 mM
(2E)-1-(5-bromo-2-hydroxyphenyl)-3-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
15% inhibition at 0.001 mM
(2E)-1-(6-bromo-1H-indol-2-yl)-3-(5-bromo-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-2-[(5-bromo-2-methoxyphenyl)methylidene]-2,3,4,9-tetrahydro-1H-carbazol-1-one
-
22% inhibition at 0.001 mM
(2E)-3-(3-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
-
(2E)-3-(4-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
-
-
(2E)-3-(6-bromo-1H-indol-2-yl)-1-(1H-indol-2-yl)prop-2-en-1-one
-
38% inhibition at 0.001 mM
(2E)-3-(6-bromo-1H-indol-3-yl)-1-(1H-indol-2-yl)prop-2-en-1-one
-
45% inhibition at 0.001 mM
(2E)-3-(6-bromo-1H-indol-3-yl)-1-(1H-indol-3-yl)prop-2-en-1-one
-
28% inhibition at 0.001 mM
(5-bromo-2-hydroxyphenyl)([(E)-[1-(1-methyl-1H-indol-2-yl)ethylidene]amino]oxy)methanone
-
34% inhibition at 0.01 mM
(5-bromo-2-methoxyphenyl)([(E)-[1-(1-methyl-1H-indol-2-yl)ethylidene]amino]oxy)methanone
-
33% inhibition at 0.01 mM
(6R,10S)-2-chloro-6,10-bis(5-chloro-1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
-
-
(6R,10S)-3-chloro-6,10-bis(6-chloro-1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
-
-
(6R,10S)-6,10-di(1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
-
-
(6R,11S)-6,11-di(1H-indol-3-yl)-6,7,8,9,10,11-hexahydro-5H-cycloocta[b]indole
-
-
(E)-5-bromo-2-hydroxy-N'-(1-(4,5,6-trifluoro-1Hindol-2-yl)ethylidene)benzohydrazide
-
-
(E)-5-bromo-2-hydroxy-N'-(1-(5-hydroxy-1H-indol-2-yl)ethylidene)benzohydrazide
-
-
(E)-5-bromo-2-hydroxy-N'-(1-(5-methoxy-1H-indol-2-yl)ethylidene)benzohydrazide
-
-
(E)-5-bromo-N'-(1-(4,5-difluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(5,6-difluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(5-bromo-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(5-bromo-1H-indol-2-yl)propylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(5-chloro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(5-fluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(6-bromo-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
-
(E)-5-bromo-N'-(1-(7-fluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
-
39% inhibition at 500 nM
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-2-hydroxy-5-chlorobenzohydrazide
-
36% inhibition at 0.001 mM
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-2-hydroxy-5-iodobenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-3,5-dibromo-2-hydroxybenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-3,5-dibromo-2-methoxybenzohydrazide
-
57% inhibition at 0.001 mM
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-4-bromo-2-hydroxybenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-(prop-2-ynyloxy)benzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-hydroxy-4-methoxybenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-hydroxybenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-methoxybenzohydrazide
-
-
(E)-N'-(1-(1H-indol-2-yl)ethylidene)benzohydrazide
-
28% inhibition at 0.01 mM
(E)-N'-(1-(1H-indol-2-yl)ethylidene)picolinohydrazid
-
15% inhibition at 0.01 M
(E)-N'-(1-(1H-indol-2-yl)propylidene)-5-bromo-2-hydroxybenzohydrazide
-
crystal structure determination of the inhibitor compound
(E)-N'-[1-(1H-indol-2-yl)ethylidene]-2-hydroxy-3,5-diisopropylbenzohydrazide
-
40% inhibition at 0.01 mM
(E)-N'-[1-(1H-indol-2-yl)ethylidene]-5-bromo-2-ethoxybenzohydrazide
-
-
(E/Z)-N'-((1H-indol-2-yl)(phenyl)methylene)-5-bromo-2-hydroxybenzohydrazide
-
-
(Z)-N'-(1-(1H-indol-2-yl)-2,2-dimethylpropylidene)-5-bromo-2-hydroxybenzohydrazide
-
crystal structure determination of the inhibitor compound
1-(6-bromo-1-benzothiophen-2-yl)-2-(4-bromophenyl)ethan-1-one
-
43% inhibition at 0.001 mM
2,4-dihydroxy-N'-[(E)-(2-hydroxy-6,7,8,9-tetrahydrodibenzo[b,d]furan-1-yl)methylidene]benzohydrazide
-
-
2-(5-bromo-1H-benzimidazol-2-yl)-1-(5-bromo-1H-indol-2-yl)ethan-1-one
-
-
2-(5-bromo-1H-benzimidazol-2-yl)-1-(5-bromo-2-hydroxyphenyl)ethan-1-one
-
-
2-(5-bromo-1H-benzimidazol-2-yl)-1-(6-bromo-1H-indol-2-yl)ethan-1-one
-
-
2-(5-bromo-2-hydroxyphenyl)-1-(1H-indol-2-yl)ethan-1-one
-
28% inhibition at 0.001 mM
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(1-methyl-1H-indol-2-yl)ethan-1-one
-
41% inhibition at 0.001 mM
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-bromo-2-hydroxyphenyl)ethan-1-one
-
-
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-bromo-2-methoxyphenyl)ethan-1-one
-
22% inhibition at 0.001 mM
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(4-bromo-2-hydroxyphenyl)ethan-1-one
-
-
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(5-bromo-1H-indol-2-yl)ethan-1-one
-
-
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(5-bromo-2-methoxyphenyl)ethan-1-one
-
-
2-bromo-6-[[(6-bromo-1,3-benzothiazol-2-yl)amino]methyl]phenol
-
17% inhibition at 0.001 mM
2-hydroxy-5-iodo-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
2-[(1E)-1-[2-[(5-bromo-2-methoxyphenyl)(dioxido-l6-sulfanylidene)methyl]hydrazinylidene]ethyl]-1H-indole
-
12% inhibition at 0.01 mM
2-[(1E)-1-[2-[(5-bromo-2-methoxyphenyl)(dioxido-l6-sulfanylidene)methyl]hydrazinylidene]ethyl]-4,5-difluoro-1H-indole
-
11% inhibition at 0.01 mM
2-[5-(5-bromo-2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]-1H-indole
-
19% inhibition at 0.001 mM
2-[6-(5-bromo-2-methoxyphenyl)pyridin-2-yl]-1H-indole
-
6% inhibition at 0.001 mM
3-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]naphthalene-2-carbohydrazide
-
-
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)ethylidene]naphthalene-2-carbohydrazide
-
-
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)propylidene]naphthalene-2-carbohydrazide
-
-
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1H-indol-2-yl)propylidene]naphthalene-2-carbohydrazide
-
-
4-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
611% inhibition at 500 nM
4-bromo-2-[(E)-[(6-bromo-1,3-benzothiazol-2-yl)imino]methyl]phenol
-
41% inhibition at 0.001 mM
4-bromo-2-[2-(6-bromo-1H-indol-2-yl)pyridin-4-yl]phenol
-
41% inhibition at 0.001 mM
4-bromo-2-[5-(1H-indol-2-yl)-1,3,4-oxadiazol-2-yl]phenol
-
8% inhibition at 0.001 mM
4-hydroxy-N'-(7-hydroxy-2,3-dihydro-8H-[1,4]dioxino[2,3-f]indol-8-yl)phthalazine-1-carbohydrazide
-
-
4-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]-1,10-biphenyl-3-carbohydrazide
-
20% inhibition at 0.01 mM
4-[(4-[3-[(1-hydroxy-2-methylpropan-2-yl)sulfamoyl]-4-methylphenyl]phthalazin-1-yl)amino]-N-methylbenzamide
-
-
5-bromo-2-(6-bromo-1,3-benzothiazol-2-yl)-1H-isoindole-1,3(2H)-dione
-
34% inhibition at 0.001 mM
5-bromo-2-(ethoxymethoxy)-N'-((1E)-1-(1H-indol-2-yl)ethylidene)benzohydrazide
-
-
5-bromo-2-hydroxy-4-methoxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-benzimidazol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)propylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)propylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(5-hydroxy-1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(5-iodo-1H-indol-2-yl)ethylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(1E)-1-(5-methoxy-1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
-
54% inhibition at 0.001 mM
5-bromo-2-hydroxy-N'-[(1E)-1-[5-(trifluoromethyl)-1Hindol-2-yl]ethylidene]benzohydrazide
-
46% inhibition at 0.01 mM
5-bromo-2-hydroxy-N'-[(3E)-5-methyl-2-methylidene-1,2-dihydro-3H-indol-3-ylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(E)-(1-methyl-1H-indol-2-yl)(phenyl)methylidene]benzohydrazide
-
-
5-bromo-2-hydroxy-N'-[(E)-(1-methyl-1H-indol-2-yl)methylidene]benzohydrazide
-
-
5-bromo-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]-2-methoxy-N-methylbenzohydrazide
-
33% inhibition at 0.001 mM
5-bromo-N'-[(1E)-1-(2,4-dihydroxyphenyl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(4,5-difluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5,6-difluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5,6-difluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)propylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(5-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(6-bromo-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(6-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(6-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(1E)-1-(6-fluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N'-[(3E)-5-bromo-2-methylidene-1,2-dihydro-3H-indol-3-ylidene]-2-hydroxybenzohydrazide
-
-
5-bromo-N-(6-bromo-1,3-benzothiazol-2-yl)-2-hydroxy-N-methylbenzamide
-
5% inhibition at 0.001 mM
N'-[(1E)-1-(1,3-benzothiazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
-
-
N'-[(1E)-1-(1,3-benzoxazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
-
26% inhibition at 500 nM
N'-[(1E)-1-(1-benzothiophen-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
-
-
N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
-
-
N'-[(1E)-1-(1H-benzimidazol-2-yl)propylidene]-5-bromo-2-hydroxybenzohydrazide
-
-
N'-[(1E)-1-(2,4-dihydroxyphenyl)ethylidene]-3-(5,6-dimethyl-1,3-dihydro-2H-isoindol-2-yl)benzohydrazide
-
-
N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)ethylidene]-3-hydroxynaphthalene-2-carbohydrazide
-
-
N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)propylidene]-3-hydroxynaphthalene-2-carbohydrazide
-
-
N'-[(1E)-1-(5-bromo-1H-indol-2-yl)ethylidene]-3-hydroxynaphthalene-2-carbohydrazide
-
-
N'-[(1E)-1-(5-bromo-1H-indol-2-yl)propylidene]-3-hydroxynaphthalene-2-carbohydrazide
-
-
N'-[(3E)-5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxybenzohydrazide
-
-
N'-[(3Z)-1-ethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxynaphthalene-2-carbohydrazide
-
-
N-(1,3-benzothiazol-2-yl)-2-hydroxy-5-sulfanylbenzamide
-
13% inhibition at 0.001 mM
N-(4-methylphenyl)-2-[(4-sulfamoylphenyl)amino]pyridine-3-carboxamide
-
-
N-(5-bromo-1,3-benzothiazol-2-yl)-2-hydroxy-5-sulfanylbenzamide
-
48% inhibition at 0.001 mM
N-(6-bromo-1,3-benzothiazol-2-yl)-2-hydroxybenzamide
-
65% inhibition at 0.001 mM
2-(4-bromophenyl)-1-(1H-indol-2-yl)ethan-1-one
-
41% inhibition at 0.001 mM
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-chloro-2-hydroxyphenyl)ethan-1-one
-
-
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-chloro-2-hydroxyphenyl)ethan-1-one
-
43% inhibition at 0.001 mM
additional information
-
development of highly potent inhibitors which demonstrate complete selectivity for the bacterial enzyme compared to all human orthologues, molecular docking, overview
-
additional information
-
inhibitor development, synthesis, optimization, and structure-activity relationship analysis, inhibitor potencies in growth inhibition of strains RN4220, ATCC 25923, and ATCC 29213, overview. No inhibition by (E)-5-bromo-2-hydroxy-N'-(1-(5-phenyl-1H-indol-2-yl)ethylidene)benzohydrazide, (Z)-N'-(1-(1H-indol-2-yl)-2,2-dimethylpropylidene)-5-bromo-2-hydroxybenzohydrazide, and 5-bromo-N'-[(1E)-2,2-dimethyl-1-(1-methyl-1H-indol-2-yl)propylidene]-2-hydroxybenzohydrazide
-
additional information
-
bisindolyl-cycloalkane indoles result from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds are inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), analysis of the compounds as MRSA PK inhibitors, structure-activity relationships of structurally varied compounds, overview. MIC value (mg/ml) of the compounds versus Staphylococcus aureus strains ATCC 25923 and MRSA ATCC 43300. No inhibition by (1S,4S)-7-chloro-1,4-bis(6-chloro-1H-indol-3-yl)-2,3,4,9-tetrahydro-1H-carbazole
-
additional information
-
synthesis and evaluation of several series of compounds as inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase. Structure-activity analysis, overview. (2E)-3-(5-bromo-1H-indol-3-yl)-1-(1H-indol-3-yl)prop-2-en-1-one and (2E)-1-(3-bromo-2-hydroxyphenyl)-3-(1H-indol-2-yl)prop-2-en-1-one are not inhibitory
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ATP
slight activation of the full-length enzyme, not the C-terminally truncated enzyme
additional information
no activation by fructose 1,6-bisphosphate
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
steady-state kinetics of recombinant wild-type and truncated PKin the absence or presence of 1 mM AMP as a function of phosphoenolpyruvate
-
additional information
additional information
-
steady-state kinetics of recombinant wild-type and truncated PKin the absence or presence of 1 mM AMP as a function of phosphoenolpyruvate
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0168
(1S,3S)-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0061
(1S,3S)-2-bromo-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0068
(1S,3S)-2-chloro-1,3-di(1H-indol-3-yl)-1,2,3,4-tetrahydrocyclopenta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0085
(1S,4S)-1,4-di(1H-indol-3-yl)-2,3,4,9-tetrahydro-1H-carbazole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.05
(1S,4S)-6-chloro-1,4-bis(5-chloro-1H-indol-3-yl)-2,3,4,9-tetrahydro-1H-carbazole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.000185
(2-[(1E)-1-[2-(5-bromo-2-hydroxybenzoyl)hydrazinylidene]ethyl]-1-methyl-1H-indol-6-yl)dibromanium
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000553
(2E)-1-(4-bromo-2-hydroxyphenyl)-3-(1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000132
(2E)-1-(4-bromo-2-hydroxyphenyl)-3-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000005
(2E)-1-(6-bromo-1H-indol-2-yl)-3-(1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000008
(2E)-1-(6-bromo-1H-indol-2-yl)-3-(5-bromo-2-methoxyphenyl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000403
(2E)-3-(3-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000014
(2E)-3-(4-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.00178
(2E)-3-(5-bromo-1H-indol-3-yl)-1-(1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000355
(2E)-3-(5-bromo-2-hydroxyphenyl)-1-(1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000024
(2E)-3-(5-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000343
(2E)-3-(6-bromo-1H-indol-2-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.0026
(6R,10S)-2-chloro-6,10-bis(5-chloro-1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0025
(6R,10S)-3-chloro-6,10-bis(6-chloro-1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0102
(6R,10S)-6,10-di(1H-indol-3-yl)-5,6,7,8,9,10-hexahydrocyclohepta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.0113
(6R,11S)-6,11-di(1H-indol-3-yl)-6,7,8,9,10,11-hexahydro-5H-cycloocta[b]indole
Staphylococcus aureus
-
precombinant enzyme, pH 7.5, 30°C
0.000015
(E)-5-bromo-2-hydroxy-N'-(1-(4,5,6-trifluoro-1Hindol-2-yl)ethylidene)benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000214
(E)-5-bromo-2-hydroxy-N'-(1-(5-hydroxy-1H-indol-2-yl)ethylidene)benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000178
(E)-5-bromo-2-hydroxy-N'-(1-(5-methoxy-1H-indol-2-yl)ethylidene)benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000024
(E)-5-bromo-N'-(1-(4,5-difluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.00002
(E)-5-bromo-N'-(1-(5,6-difluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000049
(E)-5-bromo-N'-(1-(5-bromo-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000451
(E)-5-bromo-N'-(1-(5-bromo-1H-indol-2-yl)propylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000052
(E)-5-bromo-N'-(1-(5-chloro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000049
(E)-5-bromo-N'-(1-(5-fluoro-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000024
(E)-5-bromo-N'-(1-(6-bromo-1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000863
(E)-N'-((1H-indol-2-yl)methylene)-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000151
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-2-hydroxy-5-iodobenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.008615
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000074
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-3,5-dibromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.00815
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-3-bromobenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.001312
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-4-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000064
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-(prop-2-ynyloxy)benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000324
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-hydroxy-4-methoxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000085
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000182
(E)-N'-(1-(1H-indol-2-yl)ethylidene)-5-bromo-2-methoxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000126
(E)-N'-(1-(1H-indol-2-yl)propylidene)-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000049
(E)-N'-[(1H-indol-2-yl)methylene]-5-bromo-2-methoxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000063
(E)-N'-[1-(1H-indol-2-yl)ethylidene]-5-bromo-2-ethoxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000445
(E/Z)-N'-((1H-indol-2-yl)(phenyl)methylene)-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.00001
1-(6-bromo-1H-indol-2-yl)-2-(4-bromophenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000116
2-(3-bromo-2-hydroxyphenyl)-1-(6-bromo-1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000012
2-(4-bromophenyl)-1-(1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000003
2-(5-bromo-1H-benzimidazol-2-yl)-1-(5-bromo-1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000011
2-(5-bromo-1H-benzimidazol-2-yl)-1-(5-bromo-2-hydroxyphenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000002
2-(5-bromo-1H-benzimidazol-2-yl)-1-(6-bromo-1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000011
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000043
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-bromo-2-hydroxyphenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000004
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(3-chloro-2-hydroxyphenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000214
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(4-bromo-2-hydroxyphenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000023
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(5-bromo-1H-indol-2-yl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000008
2-(6-bromo-1,3-benzothiazol-2-yl)-1-(5-bromo-2-methoxyphenyl)ethan-1-one
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000483
2-hydroxy-5-iodo-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000042
3-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]naphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000059
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)ethylidene]naphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000052
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)propylidene]naphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000031
3-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1H-indol-2-yl)propylidene]naphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000251
5-bromo-2-(ethoxymethoxy)-N'-((1E)-1-(1H-indol-2-yl)ethylidene)benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000841
5-bromo-2-hydroxy-4-methoxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000227
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-benzimidazol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000461
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)propylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000084
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000114
5-bromo-2-hydroxy-N'-[(1E)-1-(1H-indol-2-yl)propylidene]benzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000055
5-bromo-2-hydroxy-N'-[(1E)-1-(4,5,6-trifluoro-1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000043
5-bromo-2-hydroxy-N'-[(1E)-1-(5-iodo-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000794
5-bromo-2-hydroxy-N'-[(1E)-1-(5-methoxy-1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.006043
5-bromo-2-hydroxy-N'-[(E)-(1-methyl-1H-indol-2-yl)(phenyl)methylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.003087
5-bromo-2-hydroxy-N'-[(E)-(1-methyl-1H-indol-2-yl)methylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000145
5-bromo-N'-[(1E)-1-(4,5-difluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000061
5-bromo-N'-[(1E)-1-(5,6-difluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000016
5-bromo-N'-[(1E)-1-(5,6-difluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000146
5-bromo-N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000168
5-bromo-N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)propylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000228
5-bromo-N'-[(1E)-1-(5-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000165
5-bromo-N'-[(1E)-1-(5-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000017
5-bromo-N'-[(1E)-1-(6-bromo-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000228
5-bromo-N'-[(1E)-1-(6-chloro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000165
5-bromo-N'-[(1E)-1-(6-fluoro-1-methyl-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000045
5-bromo-N'-[(1E)-1-(6-fluoro-1H-indol-2-yl)ethylidene]-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000008
5-bromo-N-(5-bromo-1,3-benzothiazol-2-yl)-1H-indole-2-carboxamide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000003
5-bromo-N-(6-bromo-1,3-benzothiazol-2-yl)-2-hydroxybenzamide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000102
6-bromo-3-(4-bromophenyl)-1H-indole
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.00006
bromodeoxytopsentin
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000016
cis-3-4-dihydrohamacanthin B
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000224
N'-[(1E)-1-(1,3-benzothiazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000286
N'-[(1E)-1-(1-benzothiophen-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000126
N'-[(1E)-1-(1H-benzimidazol-2-yl)propylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000115
N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)ethylidene]-3-hydroxynaphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000079
N'-[(1E)-1-(5-bromo-1-methyl-1H-indol-2-yl)propylidene]-3-hydroxynaphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000026
N'-[(1E)-1-(5-bromo-1H-indol-2-yl)ethylidene]-3-hydroxynaphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000018
N'-[(1E)-1-(5-bromo-1H-indol-2-yl)propylidene]-3-hydroxynaphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.00091
N'-[(3Z)-1-ethyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]-3-hydroxynaphthalene-2-carbohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000051
N-(5-bromo-1,3-benzothiazol-2-yl)-1H-indole-2-carboxamide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000381
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000381
5-bromo-2-hydroxy-N'-[(1E)-1-(1-methyl-1H-indol-2-yl)ethylidene]benzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
0.000091
N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH 7.5, 30°C
0.000091
N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH and temperature not specified in the publication
0.000091
N'-[(1E)-1-(1H-benzimidazol-2-yl)ethylidene]-5-bromo-2-hydroxybenzohydrazide
Staphylococcus aureus
-
pH not specified in the publication, 30°C
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
significant evolutionary distance existing between the type I and type II isoenzymes in Gram-negative bacteria
malfunction
the catalytic activities of the C-terminally truncated mutant toward both phophoenolpyruvate and ADP are profoundly decreased compared to those of wild-type enzyme
physiological function
the C-terminal domain is not required for substrate binding or allosteric regulation observed in the holoenzyme, the kinetic efficiency of the truncated enzyme is decreased by 24 and 16fold, in ligand-free state, toward phophoenolpyruvate and ADP, respectively, but is restored by 3fold in AMP-bound state. The C-terminal domain (Gly473-Leu585) plays a substantial role in enzyme activity and comformational stability, and the C-terminal domain is involved in maintaining the specificity of allosteric regulation
metabolism
physiological function
additional information
metabolism
-
pyruvate kinase is a critical protein catalyzing the final step of glycolysis, which involves the transfer of a phosphoryl group from phosphoenolpyruvate to ADP, producing pyruvate and ATP
metabolism
-
pyruvate kinase (PK) is an essential hub protein in the interactome of MRSA. PK plays a central role in the carbohydrate metabolism. It catalyzes the final rate-limiting step in the glycolysis which converts phosphoenolpyruvate (PEP) to pyruvate under ATP formation from ADP in an irreversible process
physiological function
-
pyruvate kinase (PK) is an essential hub protein in the interactome of MRSA. PK plays a central role in the carbohydrate metabolism. It catalyzes the final rate-limiting step in the glycolysis which converts phosphoenolpyruvate (PEP) to pyruvate under ATP formation from ADP in an irreversible process
physiological function
-
pyruvate kinase (PK) is responsible for catalyzing the final step of glycolysis, which involves the transfer of the phosphoryl group of phosphoenolpyruvate (PEP) to ADP to produce pyruvate and ATP. Pyruvate kinase has been identified as a highly interconnected essential hub protein in methicillin-resistant Staphylococcus aureus (MRSA), with structural features distinct from the human homologues
additional information
the C-terminally truncated enzyme exhibits high affinity toward both phophoenolpyruvate and ADP and exhibits hyperbolic kinetics toward phophoenolpyruvate in the presence of activators AMP and ribose 5-phosphate consistent with kinetic properties of full-length enzyme
additional information
-
the C-terminally truncated enzyme exhibits high affinity toward both phophoenolpyruvate and ADP and exhibits hyperbolic kinetics toward phophoenolpyruvate in the presence of activators AMP and ribose 5-phosphate consistent with kinetic properties of full-length enzyme
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
215000
His-tagged C-terminally truncated enzyme mutant, gel filtration
53100
4 * 65100, about, full-length enzyme, sequence calculation, 4 * 53100, about, C-terminally truncated enzyme mutant, sequence calculation
65100
4 * 65100, about, full-length enzyme, sequence calculation, 4 * 53100, about, C-terminally truncated enzyme mutant, sequence calculation
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
homotetramer
4 * 65100, about, full-length enzyme, sequence calculation, 4 * 53100, about, C-terminally truncated enzyme mutant, sequence calculation
tetramer
-
structure-based molecular modeling and crystal structure analysis, overview
additional information
additional information
the C-terminal domain is not required for the tetramerization of the enzyme, homotetramerization also occurs in a truncated enzyme lacking the domain
additional information
-
the C-terminal domain is not required for the tetramerization of the enzyme, homotetramerization also occurs in a truncated enzyme lacking the domain
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
construction of a C-terminally truncated mutant PKCT with a stop after residue 390. The catalytic activities of PKCT toward both phophoenolpyruvate and ADP are profoundly decreased compared to those of wild-type enzyme
additional information
-
construction of a C-terminally truncated mutant PKCT with a stop after residue 390. The catalytic activities of PKCT toward both phophoenolpyruvate and ADP are profoundly decreased compared to those of wild-type enzyme
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant His-tagged full-length and C-terminally truncated enzymes from Escherichia coli strain BL-21(DE3) by nickel affiniy chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
gene pyk, phylogenetic tree, expression of His-tagged full-length and C-terminally truncated enzymes in Escherichia coli strain BL-21(DE3)
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
drug development
-
the enzyme is a potential target for development of novel antibiotics
drug development
-
structural features of MRSA that are distinct from the human enzyme features makes the Staphylococcus enzyme an antimicrobial target
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Axerio-Cilies, P.; See, R.H.; Zoraghi, R.; Worral, L.; Lian, T.; Stoynov, N.; Jiang, J.; Kaur, S.; Jackson, L.; Gong, H.; Swayze, R.; Amandoron, E.; Kumar, N.S.; Moreau, A.; Hsing, M.; Strynadka, N.C.; McMaster, W.R.; Finlay, B.B.; Foster, L.J.; Young, R.N.; Reiner, N.E.; Cherkasov, A.
Cheminformatics-driven discovery of selective, nanomolar inhibitors for staphylococcal pyruvate kinase
ACS Chem. Biol.
7
350-359
2012
Staphylococcus aureus
Zoraghi, R.; See, R.H.; Gong, H.; Lian, T.; Swayze, R.; Finlay, B.B.; Brunham, R.C.; McMaster, W.R.; Reiner, N.E.
Functional analysis, overexpression, and kinetic characterization of pyruvate kinase from methicillin-resistant Staphylococcus aureus
Biochemistry
49
7733-7747
2010
Escherichia coli (A0A0H3JER5), Escherichia coli (P0AD62), Escherichia coli, Staphylococcus aureus (Q6GG09), Staphylococcus aureus, Staphylococcus aureus MRSA252 (Q6GG09)
Kumar, N.S.; Amandoron, E.A.; Cherkasov, A.; Finlay, B.B.; Gong, H.; Jackson, L.; Kaur, S.; Lian, T.; Moreau, A.; Labriere, C.; Reiner, N.E.; See, R.H.; Strynadka, N.C.; Thorson, L.; Wong, E.W.; Worrall, L.; Zoraghi, R.; Young, R.N.
Optimization and structure-activity relationships of a series of potent inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase as novel antimicrobial agents
Bioorg. Med. Chem.
20
7069-7082
2012
Staphylococcus aureus
Labriere, C.; Gong, H.; Finlay, B.B.; Reiner, N.E.; Young, R.N.
Further investigation of inhibitors of MRSA pyruvate kinase towards the conception of novel antimicrobial agents
Eur. J. Med. Chem.
125
1-13
2017
Staphylococcus aureus, Staphylococcus aureus ATCC 29213
El-Sayed, M.; Zoraghi, R.; Reiner, N.; Suzen, S.; Ohlsen, K.; Lalk, M.; Altanlar, N.; Hilgeroth, A.
Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase
J. Enzyme Inhib. Med. Chem.
31
1666-1671
2016
Staphylococcus aureus, Staphylococcus aureus ATCC 43300
EXTERNAL LINKS (specific for EC-Number 2.7.1.40)
Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.
Release 2023.1 (January 2023)
Legal
Curated at
Member of
