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Literature summary for 6.2.1.3 extracted from

  • Kim, J.H.; Lewin, T.M.; Coleman, R.A.
    Expression and characterization of recombinant rat acyl-CoA synthetases 1, 4, and 5: selective inhibition by triacsin C and thiazolidinediones (2001), J. Biol. Chem., 276, 24667-24673.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of ACS-Flag fusion proteins in Escherichia coli Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
cis-9,10-methylene octadecanoic acid IC50: 0.025 mM for ACS1-Flag fusion protein, 0.03-0.04 mM for ACS4-Flag fusion protein, no effect on ACS5-Flag fusion protein Rattus norvegicus
GW1929 IC50: above 0.05 mM for ACS1-Flag fusion protein, 0.05 mM for ACS4-Flag fusion protein, no effect on ACS5-Flag fusion protein Rattus norvegicus
additional information 3-phenoxybenzoic acid, p-coumaric acid, ibuprofen, ferulic acid and firefly luciferin, at concentrations up to 0.05 mM have no effect on three ACS isoenzymes Rattus norvegicus
NEM strongly inhibits ACS5 and weakly inhibits ACS1, no effect on ACS5 Rattus norvegicus
pioglitazone IC50: 0.0015 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus
rosiglitazone IC50: 0.0005 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus
thiazolidinediones specific inhibitors of ACS4 Rattus norvegicus
Triacsin C strongly inhibits ACS1 and ACS4, no effect on ACS5 Rattus norvegicus
troglitazone IC50: 0.0015 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0024
-
CoA pH 7.5, 37°C, ACS5 Rattus norvegicus
0.0041
-
CoA pH 7.5, 37°C, ACS4 Rattus norvegicus
0.005
-
palmitate pH 7.5, 37°C, ACS1 Rattus norvegicus
0.0054
-
palmitate pH 7.5, 37°C, ACS4 Rattus norvegicus
0.0064
-
CoA pH 7.5, 37°C, ACS1 Rattus norvegicus
0.0086
-
palmitate pH 7.5, 37°C, ACS5 Rattus norvegicus
0.034
-
ATP pH 7.5, 37°C, ACS4 Rattus norvegicus
0.649
-
ATP pH 7.5, 37°C, ACS1 Rattus norvegicus
0.666
-
ATP pH 7.5, 37°C, ACS5 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + palmitate + CoA
-
Rattus norvegicus AMP + diphosphate + palmitoyl-CoA
-
?

Synonyms

Synonyms Comment Organism
ACS1
-
Rattus norvegicus
ACS4
-
Rattus norvegicus
ACS5
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.4 9 ACS1 and ACS4 Rattus norvegicus
7.4 8 ACS5 Rattus norvegicus

Temperature Stability [°C]

Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
43
-
half-life: about 10 min for ACS1, shorter thah 1 min fpr ACS4 and about 4 min for ACS5 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
IC50: 0.0005 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus rosiglitazone
0.0015
-
IC50: 0.0015 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus troglitazone
0.0015
-
IC50: 0.0015 mM for ACS1-Flag fusion protein, no effect on ACS4-Flag fusion protein and ACS5-Flag fusion protein Rattus norvegicus pioglitazone
0.025
-
IC50: 0.025 mM for ACS1-Flag fusion protein, 0.03-0.04 mM for ACS4-Flag fusion protein, no effect on ACS5-Flag fusion protein Rattus norvegicus cis-9,10-methylene octadecanoic acid
0.05
-
IC50: above 0.05 mM for ACS1-Flag fusion protein, 0.05 mM for ACS4-Flag fusion protein, no effect on ACS5-Flag fusion protein Rattus norvegicus GW1929