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Literature summary extracted from

  • Bentebibel, A.; Sebastian, D.; Herrero, L.; Lopez-Vinas, E.; Serra, D.; Asins, G.; Gomez-Puertas, P.; Hegardt, F.G.
    Novel effect of C75 on carnitine palmitoyltransferase I activity and palmitate oxidation (2006), Biochemistry, 45, 4339-4350.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.3.1.21 C75 a potential drug for the treatment of obesity, a competitive, irreversible inhibitor of fatty acid synthase, and a malonyl-CoA analogue that antagonizes the allosteric inhibitory effect of malonyl-CoA on CPT I Mus musculus
2.3.1.21 C75 a potential drug for the treatment of obesity, a competitive, irreversible inhibitor of fatty acid synthase, and a malonyl-CoA analogue that antagonizes the allosteric inhibitory effect of malonyl-CoA on CPT I Homo sapiens
2.3.1.21 C75 a potential drug for the treatment of obesity, a competitive, irreversible inhibitor of fatty acid synthase, and a malonyl-CoA analogue that antagonizes the allosteric inhibitory effect of malonyl-CoA on CPT I Rattus norvegicus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.21 overexpression of isozymes M-CPT I and L-CPT I in Saccharomyces cerevisiae Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.21 C75-CoA potent competitive inhibition, IC50: 0.00025 mM in INS(832/13) cells, IC50: 0.00046 in L6E9 myotubes, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA and inhibits fatty acid oxidation, e.g. in pancreatic INS(823/13), muscle L6E9, or kidney HEK293 cell lines, inhibition mechanism, overview, molecular model of docking of C75-CoA to L-CPT I Homo sapiens
2.3.1.21 C75-CoA potent competitive inhibition, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA and inhibits fatty acid oxidation, a single intraperitoneal injection of C75 in mice produced short-term inhibition of CPT I activity in mitochondria from the liver, soleus, and pancreas, inhibition mechanism, overview Mus musculus
2.3.1.21 C75-CoA potent competitive inhibition, IC50: 0.0007 mM in liver, IC50: 0.00004 in muscle, IC50: 0.00024 mM recombinant isozyme L-CPT I, IC50: 0.00036 recombinant isozyme M-CPT I, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA and inhibits fatty acid oxidation, inhibition mechanism, overview, molecular model of docking of C75-CoA to L-CPT I Rattus norvegicus
2.3.1.21 etomoxiryl-CoA IC50: 0.00121 mM in INS(832/13) cells, IC50: 0.00287 in L6E9 myotubes Homo sapiens
2.3.1.21 etomoxiryl-CoA
-
 Mus musculus
2.3.1.21 etomoxiryl-CoA IC50: 0.00025 mM in liver, IC50: 0.000015 in muscle, IC50: 0.0041 mM recombinant isozyme L-CPT I, IC50: 0.0031 recombinant isozyme M-CPT I Rattus norvegicus
2.3.1.21 malonyl-CoA allosteric inhibition Homo sapiens
2.3.1.21 malonyl-CoA allosteric inhibition Mus musculus
2.3.1.21 malonyl-CoA allosteric inhibition Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.21 mitochondrion
-
 Mus musculus 5739
-
2.3.1.21 mitochondrion
-
 Homo sapiens 5739
-
2.3.1.21 mitochondrion
-
 Rattus norvegicus 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 Mus musculus the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine Homo sapiens the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine Rattus norvegicus the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.21 Homo sapiens
-
 tissue-specific isozymes L-CPT1 and M-CPT1
-
2.3.1.21 Mus musculus
-
 male C57BL/6J mice, tissue-specific isozymes L-CPT1 and M-CPT1
-
2.3.1.21 Rattus norvegicus
-
 male Sprague-Dawley rats, tissue-specific isozymes L-CPT I and M-CPT I
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.21 native enzyme partially by microsome preparation Mus musculus
2.3.1.21 native enzyme partially by microsome preparation Homo sapiens
2.3.1.21 native enzyme partially by microsome preparation, recombinant isozymes M-CPT I and L-CPT I from Saccharomyces cerevisiae Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.21 HEK-293 cell kidney cell line Homo sapiens
-
2.3.1.21 INS-1 823/13 cell pancreatic cell line Homo sapiens
-
2.3.1.21 kidney
-
 Homo sapiens
-
2.3.1.21 L6E9 cell muscle cell line Rattus norvegicus
-
2.3.1.21 liver
-
 Mus musculus
-
2.3.1.21 liver isozyme L-CPT I Rattus norvegicus
-
2.3.1.21 muscle
-
 Homo sapiens
-
2.3.1.21 muscle isozyme M-CPT I Rattus norvegicus
-
2.3.1.21 pancreas
-
 Mus musculus
-
2.3.1.21 pancreas
-
 Homo sapiens
-
2.3.1.21 soleus
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.21 palmitoyl-CoA + L-carnitine the enzyme is the main regulatory enzyme involved in fatty acid oxidation Mus musculus CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine the enzyme is the main regulatory enzyme involved in fatty acid oxidation Homo sapiens CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine the enzyme is the main regulatory enzyme involved in fatty acid oxidation Rattus norvegicus CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine deuterium-labeled L-carnitine substrate Mus musculus CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine deuterium-labeled L-carnitine substrate Homo sapiens CoA + L-palmitoylcarnitine
-
 ?
2.3.1.21 palmitoyl-CoA + L-carnitine deuterium-labeled L-carnitine substrate Rattus norvegicus CoA + L-palmitoylcarnitine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.21 carnitine palmitoyltransferase I
-
 Mus musculus
2.3.1.21 carnitine palmitoyltransferase I
-
 Homo sapiens
2.3.1.21 carnitine palmitoyltransferase I
-
 Rattus norvegicus
2.3.1.21 CPT I
-
 Mus musculus
2.3.1.21 CPT I
-
 Homo sapiens
2.3.1.21 CPT I
-
 Rattus norvegicus

Temperature Optimum [°C]

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

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.21 7.4
-
 assay at Mus musculus
2.3.1.21 7.4
-
 assay at Homo sapiens
2.3.1.21 7.4
-
 assay at Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.21 additional information
-
 additional information tissue-specific inhibition kinetics Homo sapiens
2.3.1.21 additional information
-
 additional information tissue-specific inhibition kinetics Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.21 0.000015
-
 IC50: 0.000015 mM in muscle Rattus norvegicus etomoxiryl-CoA
2.3.1.21 0.00004
-
 IC50: 0.00004 mM in muscle Rattus norvegicus C75-CoA
2.3.1.21 0.00024
-
 IC50: 0.00024 mM recombinant isozyme L-CPT I Rattus norvegicus C75-CoA
2.3.1.21 0.00025
-
 IC50: 0.00025 mM in liver Rattus norvegicus etomoxiryl-CoA
2.3.1.21 0.00025
-
 potent competitive inhibition, IC50: 0.00025 mM in INS(832/13) cells, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA and inhibits fatty acid oxidation, e.g. in pancreatic INS(823/13), m Homo sapiens C75-CoA
2.3.1.21 0.00036
-
 IC50: 0.00036 mM recombinant isozyme M-CPT I, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA Rattus norvegicus C75-CoA
2.3.1.21 0.00046
-
 IC50: 0.00046 mM in L6E9 myotubes, binds tightly but reversibly to CPT I, C75 applied in vivo is transformed to C75-CoA and inhibits fatty acid oxidation, e.g. in pancreatic INS(823/13), m Homo sapiens C75-CoA
2.3.1.21 0.0007
-
 potent competitive inhibition, IC50: 0.0007 mM in liver Rattus norvegicus C75-CoA
2.3.1.21 0.00121 0.00287 IC50: 0.00121 mM in INS(832/13) cells, IC50: 0.00287 in L6E9 myotubes Homo sapiens etomoxiryl-CoA
2.3.1.21 0.0031
-
 IC50: 0.0031 mM recombinant isozyme M-CPT I Rattus norvegicus etomoxiryl-CoA
2.3.1.21 0.0041
-
 IC50: 0.0041 mM recombinant isozyme L-CPT I Rattus norvegicus etomoxiryl-CoA