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Literature summary extracted from

  • Lopez-Vinas, E.; Bentebibel, A.; Gurunathan, C.; Morillas, M.; de Arriaga, D.; Serra, D.; Asins, G.; Hegardt, F.G.; Gomez-Puertas, P.
    Definition by functional and structural analysis of two malonyl-CoA sites in carnitine palmitoyltransferase 1A (2007), J. Biol. Chem., 282, 18212-18224.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.21 expression of wild-type and mutant isozyme CPT1A in Saccharomyces cerevisiae Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.3.1.21 A478G site-directed mutagenesis, the mutant shows decreased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
2.3.1.21 E26K site-directed mutagenesis, the mutant shows decreased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
2.3.1.21 E26K/K561E site-directed mutagenesis, the double mutant shows the same sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
2.3.1.21 K561E site-directed mutagenesis, the mutant shows decreased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
2.3.1.21 M593S site-directed mutagenesis, the mutant is insensitive to malonyl-CoA Homo sapiens
2.3.1.21 R243T site-directed mutagenesis, the mutant shows highly decreased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
2.3.1.21 R243T/A478G site-directed mutagenesis, the mutant shows highly decreased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.21 malonyl-CoA IC50: 0.0073 mM for the recombinant wild-type isozyme CPT1A, IC50: 0.0384 mM for CPT1A mutant R243T, IC50 values of other mutants, overview, determination of two binding sites, the A site and the O site, the latter involved residue Arg243, binding structure, interactions between N- and C-terminal residues are involved in malonyl-CoA binding to the A site, isozyme CPT1A in malonyl-CoA molecular docking, overview Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.1.21 0.007
-
 palmitoyl-CoA 30°C, recombinant CPT1A mutant R243T Homo sapiens
2.3.1.21 0.056
-
 L-carnitine 30°C, recombinant CPT1A mutant R243T Homo sapiens
2.3.1.21 0.135
-
 L-carnitine 30°C, recombinant wildtype isozyme CPT1A Homo sapiens
2.3.1.21 0.4
-
 palmitoyl-CoA 30°C, recombinant wildtype isozyme CPT1A Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.21 mitochondrion
-
 Homo sapiens 5739
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.21 palmitoyl-CoA + L-carnitine Homo sapiens
-
 CoA + L-palmitoylcarnitine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.21 Homo sapiens
-
 isozyme CPT1A
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.21 liver isozyme CPT1A Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.21 palmitoyl-CoA + L-carnitine
-
 Homo sapiens CoA + L-palmitoylcarnitine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.21 carnitine palmitoyltransferase 1A
-
 Homo sapiens
2.3.1.21 CPT1
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.21 30
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.21 additional information
-
 additional information inhibition kinetics with malonyl-CoA Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.21 0.0073 0.0384 IC50: 0.0073 mM for the recombinant wild-type isozyme CPT1A, IC50: 0.0384 mM for CPT1A mutant R243T, IC50 values of other mutants, overview, determination of two binding sites, the A site and the O site, the latter involved residue Arg243, binding struct Homo sapiens malonyl-CoA