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Literature summary for 2.3.1.21 extracted from

  • Liu, H.; Zheng, G.; Treber, M.; Dai, J.; Woldegiorgis, G.
    Cysteine-scanning mutagenesis of muscle carnitine palmitoyltransferase I reveals a single cysteine residue (Cys-305) is important for catalysis (2005), J. Biol. Chem., 280, 4524-4531.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant isozymes M-CPT I in Pichia pastoris strain GS115 Homo sapiens

Protein Variants

Protein Variants Comment Organism
A305C site-directed mutagenesis, the revertant mutant shows about wild-type activity Homo sapiens
C305A site-directed mutagenesis, inactive mutant Homo sapiens
C448A site-directed mutagenesis, the mutant shows unaltered catalytic activity and sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C504A site-directed mutagenesis, the mutant shows unaltered catalytic activity and sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C526A site-directed mutagenesis, the mutant shows unaltered catalytic activity but increased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C548S site-directed mutagenesis, the mutant shows unaltered catalytic activity and sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C562A site-directed mutagenesis, the mutant shows unaltered catalytic activity and sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C586A site-directed mutagenesis, the mutant shows unaltered catalytic activity but reduced sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C608A site-directed mutagenesis, the mutant shows unaltered catalytic activity and sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens
C659A site-directed mutagenesis, the mutant shows unaltered catalytic activity but increased sensitivity to malonyl-CoA compared to the wild-type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
malonyl-CoA IC50: 0.0005 mM for the recombinant wild-type enzyme, IC50: 0.00052 mM for the recombinant revertant A305C, IC50 values of recombinant mutant isozymes M-CPT I, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.066
-
palmitoyl-CoA pH 8.0, 37°C, recombinant revertant A305C Homo sapiens
0.073
-
palmitoyl-CoA pH 8.0, 37°C, recombinant wild-type enzyme Homo sapiens
0.824
-
L-carnitine pH 8.0, 37°C, recombinant wild-type enzyme Homo sapiens
0.92
-
L-carnitine pH 8.0, 37°C, recombinant revertant A305C Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
palmitoyl-CoA + L-carnitine Homo sapiens CPT I catalyzes the conversion of long-chain fatty acyl-CoAs to acyl carnitines in the presence of L-carnitine, a rate-limiting step in the transport of long-chain fatty acids from the cytoplasm to the mitochondrial matrix CoA + L-palmitoylcarnitine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme M-CPT I
-

Reaction

Reaction Comment Organism Reaction ID
palmitoyl-CoA + L-carnitine = CoA + L-palmitoylcarnitine the catalytic triad is composed of Cys305, His473, and Asp454, with Cys305 serving as a probable nucleophile, thus acting as a site for covalent attachment of the acyl molecule and formation of a stable acyl-enzyme intermediate, mechanism Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
heart isozyme M-CPT I Homo sapiens
-
muscle isozyme M-CPT I Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
activity of mutant enzymes Homo sapiens
0.0028
-
recombinant revertant A305C Homo sapiens
0.0029
-
recombinant wild-type enzyme Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
palmitoyl-CoA + L-carnitine
-
Homo sapiens CoA + L-palmitoylcarnitine
-
?
palmitoyl-CoA + L-carnitine CPT I catalyzes the conversion of long-chain fatty acyl-CoAs to acyl carnitines in the presence of L-carnitine, a rate-limiting step in the transport of long-chain fatty acids from the cytoplasm to the mitochondrial matrix Homo sapiens CoA + L-palmitoylcarnitine
-
?

Synonyms

Synonyms Comment Organism
muscle carnitine palmitoyltransferase I
-
Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0005
-
IC50: 0.0005 mM for the recombinant wild-type enzyme Homo sapiens malonyl-CoA
0.00052
-
IC50: 0.00052 mM for the recombinant revertant A305C, IC50 values of recombinant mutant isozymes M-CPT I overview Homo sapiens malonyl-CoA