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Literature summary extracted from

  • Bonifacio, M.J.; Palma, P.N.; Almeida, L.; Soares-da-Silva, P.
    Catechol-O-methyltransferase and its inhibitors in Parkinsons disease (2007), CNS Drug Rev., 13, 352-379.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.6 2-hydroxyoestrogen
-
Homo sapiens
2.1.1.6 ascorbic acid
-
Homo sapiens
2.1.1.6 caffeic acid
-
Homo sapiens
2.1.1.6 CGP 28014
-
Homo sapiens
2.1.1.6 entacapone
-
Homo sapiens
2.1.1.6 gallic acid
-
Homo sapiens
2.1.1.6 additional information role of COMT inhibitors in Parkinson’s disease as a new therapeutic approach to Parkinson’s disease involving conversion of levodopa to dopamine at the target region in the brain and facilitation of the continuous action of this amine at the receptor sites. A historical overview of the discovery and development of COMT inhibitors is presented with a special emphasis on nebicapone, presently under clinical development, as well as entacapone and tolcapone, which are already approved as adjuncts in the therapy of Parkinson’s disease. This article reviews human pharmacokinetic and pharmacodynamic properties of these drugs as well as their clinical efficacy and safety Homo sapiens
2.1.1.6 nebicapone
-
Homo sapiens
2.1.1.6 nitecapone
-
Homo sapiens
2.1.1.6 pyrogallol
-
Homo sapiens
2.1.1.6 quercetin
-
Homo sapiens
2.1.1.6 tolcapone
-
Homo sapiens
2.1.1.6 tropolone
-
Homo sapiens
2.1.1.6 U-0521
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.1.1.6 0.00015
-
2-hydroxyestradiol membrane-bound enzyme form Oryctolagus cuniculus
2.1.1.6 0.00027
-
2-hydroxyestradiol soluble enzyme form Oryctolagus cuniculus
2.1.1.6 0.0009 0.003 epinephrine membrane-bound enzyme form Rattus norvegicus
2.1.1.6 0.00091
-
isoproterenol membrane-bound enzyme form Oryctolagus cuniculus
2.1.1.6 0.0033
-
dopamine membrane-bound enzyme form, brain Homo sapiens
2.1.1.6 0.0055 0.114 norepinephrine membrane-bound enzyme form Rattus norvegicus
2.1.1.6 0.01
-
catechol recombinant enzyme expressed in Escherichia coli, membrane-bound enzyme form Homo sapiens
2.1.1.6 0.012
-
epinephrine membrane-bound enzyme form Mus musculus
2.1.1.6 0.015
-
dopamine recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form Homo sapiens
2.1.1.6 0.024
-
norepinephrine recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form Homo sapiens
2.1.1.6 0.043
-
R-salsolinol membrane-bound enzyme form Sus scrofa
2.1.1.6 0.108
-
catechol recombinant enzyme expressed in Escherichia coli, soluble enzyme form Homo sapiens
2.1.1.6 0.121
-
isoproterenol soluble enzyme form Oryctolagus cuniculus
2.1.1.6 0.156
-
R-salsolinol soluble enzyme form Sus scrofa
2.1.1.6 0.168 0.345 epinephrine soluble enzyme form Rattus norvegicus
2.1.1.6 0.207
-
dopamine recombinant enzyme expressed in Sf9 cells, soluble enzyme form Homo sapiens
2.1.1.6 0.242
-
epinephrine soluble enzyme form Mus musculus
2.1.1.6 0.266
-
levodopa recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form Homo sapiens
2.1.1.6 0.28
-
dopamine soluble enzyme form, brain Homo sapiens
2.1.1.6 0.304 0.464 norepinephrine soluble enzyme form Rattus norvegicus
2.1.1.6 0.369
-
norepinephrine recombinant enzyme expressed in Sf9 cells, soluble enzyme form Homo sapiens
2.1.1.6 0.613
-
levodopa recombinant enzyme expressed in Sf9 cells, soluble enzyme form Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.1.1.6 membrane two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT). MB-COMT is an integral membrane protein with the catalytic portion of the enzyme oriented toward the cytoplasmic side of the membrane Mus musculus 16020
-
2.1.1.6 membrane two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT). MB-COMT is an integral membrane protein with the catalytic portion of the enzyme oriented toward the cytoplasmic side of the membrane Homo sapiens 16020
-
2.1.1.6 membrane two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT). MB-COMT is an integral membrane protein with the catalytic portion of the enzyme oriented toward the cytoplasmic side of the membrane Sus scrofa 16020
-
2.1.1.6 membrane two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT). MB-COMT is an integral membrane protein with the catalytic portion of the enzyme oriented toward the cytoplasmic side of the membrane Oryctolagus cuniculus 16020
-
2.1.1.6 membrane two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT). MB-COMT is an integral membrane protein with the catalytic portion of the enzyme oriented toward the cytoplasmic side of the membrane Rattus norvegicus 16020
-
2.1.1.6 soluble two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Mus musculus
-
-
2.1.1.6 soluble two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Homo sapiens
-
-
2.1.1.6 soluble two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Sus scrofa
-
-
2.1.1.6 soluble two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Oryctolagus cuniculus
-
-
2.1.1.6 soluble two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Rattus norvegicus
-
-

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.1.1.6 24300
-
S-COMT Homo sapiens
2.1.1.6 30000
-
MB-COMT Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.6 Homo sapiens
-
-
-
2.1.1.6 Mus musculus
-
-
-
2.1.1.6 Oryctolagus cuniculus
-
-
-
2.1.1.6 Rattus norvegicus P22734
-
-
2.1.1.6 Sus scrofa
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.1.1.6 additional information S-COMT is a nonglycosylated protein Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.6 aorta
-
Oryctolagus cuniculus
-
2.1.1.6 brain
-
Homo sapiens
-
2.1.1.6 brain
-
Sus scrofa
-
2.1.1.6 brain
-
Rattus norvegicus
-
2.1.1.6 kidney
-
Rattus norvegicus
-
2.1.1.6 liver
-
Mus musculus
-
2.1.1.6 liver
-
Rattus norvegicus
-
2.1.1.6 placenta
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.6 S-adenosyl-L-methionine + 2-hydroxyestradiol
-
Oryctolagus cuniculus S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + catechol
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + dopamine
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + epinephrine
-
Mus musculus S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + epinephrine
-
Rattus norvegicus S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + isoproterenol
-
Oryctolagus cuniculus S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + levodopa
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + norepinephrine
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + norepinephrine
-
Rattus norvegicus S-adenosyl-L-homocysteine + ?
-
?
2.1.1.6 S-adenosyl-L-methionine + R-salsolinol
-
Sus scrofa S-adenosyl-L-homocysteine + ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.6 MB-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Mus musculus
2.1.1.6 MB-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Homo sapiens
2.1.1.6 MB-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Sus scrofa
2.1.1.6 MB-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Oryctolagus cuniculus
2.1.1.6 MB-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Rattus norvegicus
2.1.1.6 S-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Mus musculus
2.1.1.6 S-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Homo sapiens
2.1.1.6 S-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Sus scrofa
2.1.1.6 S-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Oryctolagus cuniculus
2.1.1.6 S-COMT two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.6 0.00027
-
tolcapone
-
Homo sapiens
2.1.1.6 0.0003
-
entacapone
-
Homo sapiens
2.1.1.6 0.00102
-
nitecapone
-
Homo sapiens