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Literature summary for 2.3.1.21 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
Search for more literature for 2.3.1.21

Activating Compound

Activating Compound Comment Organism Structure
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
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
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)

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

Inhibitors

Inhibitors Comment Organism Structure
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
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
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
etomoxiryl-CoA IC50: 0.00121 mM in INS(832/13) cells, IC50: 0.00287 in L6E9 myotubes Homo sapiens
etomoxiryl-CoA
-
 Mus musculus
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
malonyl-CoA allosteric inhibition Homo sapiens
malonyl-CoA allosteric inhibition Mus musculus
malonyl-CoA allosteric inhibition Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
 Mus musculus 5739
-
mitochondrion
-
 Homo sapiens 5739
-
mitochondrion
-
 Rattus norvegicus 5739
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
palmitoyl-CoA + L-carnitine Mus musculus the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?
palmitoyl-CoA + L-carnitine Homo sapiens the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?
palmitoyl-CoA + L-carnitine Rattus norvegicus the enzyme is the main regulatory enzyme involved in fatty acid oxidation CoA + L-palmitoylcarnitine
-
 ?

Organism

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

Purification (Commentary)

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000015
-
 IC50: 0.000015 mM in muscle Rattus norvegicus etomoxiryl-CoA
0.00004
-
 IC50: 0.00004 mM in muscle Rattus norvegicus C75-CoA
0.00024
-
 IC50: 0.00024 mM recombinant isozyme L-CPT I Rattus norvegicus C75-CoA
0.00025
-
 IC50: 0.00025 mM in liver Rattus norvegicus etomoxiryl-CoA
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
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
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
0.0007
-
 potent competitive inhibition, IC50: 0.0007 mM in liver Rattus norvegicus C75-CoA
0.00121 0.00287 IC50: 0.00121 mM in INS(832/13) cells, IC50: 0.00287 in L6E9 myotubes Homo sapiens etomoxiryl-CoA
0.0031
-
 IC50: 0.0031 mM recombinant isozyme M-CPT I Rattus norvegicus etomoxiryl-CoA
0.0041
-
 IC50: 0.0041 mM recombinant isozyme L-CPT I Rattus norvegicus etomoxiryl-CoA