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Information on EC 2.7.7.3 - pantetheine-phosphate adenylyltransferase and Organism(s) Homo sapiens and UniProt Accession Q13057

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IUBMB Comments
The enzyme from several bacteria (e.g. Escherichia coli, Bacillus subtilis and Haemophilus influenzae) has been shown to be bifunctional and also to possess the activity of EC 2.3.1.157, glucosamine-1-phosphate N-acetyltransferase.
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This record set is specific for:
Homo sapiens
UNIPROT: Q13057
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
phosphopantetheine adenylyltransferase, 4'-phosphopantetheine adenylyltransferase, pantetheine phosphate adenylyltransferase, pantetheine-phosphate adenylyltransferase, dephospho-coa pyrophosphorylase, enterococcus faecalis ppat, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3'-dephospho-CoA pyrophosphorylase
-
-
-
-
4-phosphopantetheine adenylyltransferase
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dephospho-CoA pyrophosphorylase
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-
-
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dephospho-coenzyme A pyrophosphorylase
-
-
-
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pantetheine phosphate adenylyltransferase
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-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
nucleotidyl group transfer
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-
-
-
PATHWAY SOURCE
PATHWAYS
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-, -, -
SYSTEMATIC NAME
IUBMB Comments
ATP:pantetheine-4'-phosphate adenylyltransferase
The enzyme from several bacteria (e.g. Escherichia coli, Bacillus subtilis and Haemophilus influenzae) has been shown to be bifunctional and also to possess the activity of EC 2.3.1.157, glucosamine-1-phosphate N-acetyltransferase.
CAS REGISTRY NUMBER
COMMENTARY hide
9026-99-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + pantetheine 4'-phosphate
diphosphate + 3'-dephospho-CoA
show the reaction diagram
-
-
-
r
ATP + pantetheine 4'-phosphate
diphosphate + 3'-dephospho-CoA
show the reaction diagram
-
-
-
r
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 + pantetheine 4'-phosphate
diphosphate + 3'-dephospho-CoA
show the reaction diagram
-
-
-
r
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
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2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
slight inhibition in vivo
3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
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additional information
compound library screening, the series of reversible inhibitors show inhibition of cell growth of Gram-positive species but no or only slight inhibition of the human A-549 tumor cells, MIC values, overview. levels of inhibitory activity of compounds against Homo sapiens PPAT are measured in the forward direction. Only compound C shows poor inhibition in vivo
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.005
(1S,2S)-N-(3,4-dichlorobenzyl)-2-(4,6-dimethoxypyrimidin-2-yl)cyclohexanecarboxamide
Homo sapiens
pH 7.0, 22°C, recombinant enzyme
0.024
2'-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6'-ethyl-4-hydroxy-6-oxo-1,6-dihydro-2,4'-bipyrimidine-5-carboxamide
Homo sapiens
pH 7.0, 22°C, recombinant enzyme
0.2
3-[3-(2-[(1S,2S)-2-[(3,4-dichlorobenzyl)carbamoyl]cyclohexyl]-6-ethylpyrimidin-4-yl)-1,2,4-oxadiazol-5-yl]propanoic acid
Homo sapiens
pH 7.0, 22°C, recombinant enzyme
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
assay at room temperature
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
COASY_HUMAN
564
0
62329
Swiss-Prot
Secretory Pathway (Reliability: 5)
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant enzyme PPAT from Escherichia coli strain BL21(DE3) to over 95% purity
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression in Escherichia coli BL21
gene coaD, recombinant expression in Escherichia coli strain BL21(DE3)
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Aghajanian, S.; Worrall, D.M.
Identification and characterization of the gene encoding the human phosphopantetheine adenylyltransferase and dephospho-CoA kinase bifunctional enzyme (CoA synthase)
Biochem. J.
365
13-18
2002
Homo sapiens (Q13057), Homo sapiens, Sus scrofa (Q8MIR4), Sus scrofa
Manually annotated by BRENDA team
de Jonge, B.L.; Walkup, G.K.; Lahiri, S.D.; Huynh, H.; Neckermann, G.; Utley, L.; Nash, T.J.; Brock, J.; San Martin, M.; Kutschke, A.; Johnstone, M.; Laganas, V.; Hajec, L.; Gu, R.F.; Ni, H.; Chen, B.; Hutchings, K.; Holt, E.; McKinney, D.; Gao, N.; Livchak, S.; Thresher, J.
Discovery of inhibitors of 4-phosphopantetheine adenylyltransferase (PPAT) to validate PPAT as a target for antibacterial therapy
Antimicrob. Agents Chemother.
57
6005-6015
2013
Candida albicans (B9WCR8), Enterococcus faecium, Enterococcus faecium ARC521, Escherichia coli (P0A6I6), Haemophilus influenzae (P44805), Haemophilus influenzae KW20 (P44805), Homo sapiens (Q06203), Staphylococcus aureus, Staphylococcus aureus RN4220, Streptococcus mutans (Q8DVH2), Streptococcus mutans UA159 (Q8DVH2), Streptococcus pneumoniae (Q8DNE6), Streptococcus pyogenes, Streptococcus pyogenes ARC838
Manually annotated by BRENDA team