Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-hydroxyoestrogen | - |
Homo sapiens | |
ascorbic acid | - |
Homo sapiens | |
caffeic acid | - |
Homo sapiens | |
CGP 28014 | - |
Homo sapiens | |
entacapone | - |
Homo sapiens | |
gallic acid | - |
Homo sapiens | |
additional information | role of COMT inhibitors in Parkinsons disease as a new therapeutic approach to Parkinsons 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 Parkinsons disease. This article reviews human pharmacokinetic and pharmacodynamic properties of these drugs as well as their clinical efficacy and safety | Homo sapiens | |
nebicapone | - |
Homo sapiens | |
nitecapone | - |
Homo sapiens | |
pyrogallol | - |
Homo sapiens | |
quercetin | - |
Homo sapiens | |
tolcapone | - |
Homo sapiens | |
tropolone | - |
Homo sapiens | |
U-0521 | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00015 | - |
2-hydroxyestradiol | membrane-bound enzyme form | Oryctolagus cuniculus | |
0.00027 | - |
2-hydroxyestradiol | soluble enzyme form | Oryctolagus cuniculus | |
0.0009 | 0.003 | epinephrine | membrane-bound enzyme form | Rattus norvegicus | |
0.00091 | - |
isoproterenol | membrane-bound enzyme form | Oryctolagus cuniculus | |
0.0033 | - |
dopamine | membrane-bound enzyme form, brain | Homo sapiens | |
0.0055 | 0.114 | norepinephrine | membrane-bound enzyme form | Rattus norvegicus | |
0.01 | - |
catechol | recombinant enzyme expressed in Escherichia coli, membrane-bound enzyme form | Homo sapiens | |
0.012 | - |
epinephrine | membrane-bound enzyme form | Mus musculus | |
0.015 | - |
dopamine | recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form | Homo sapiens | |
0.024 | - |
norepinephrine | recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form | Homo sapiens | |
0.043 | - |
R-salsolinol | membrane-bound enzyme form | Sus scrofa | |
0.108 | - |
catechol | recombinant enzyme expressed in Escherichia coli, soluble enzyme form | Homo sapiens | |
0.121 | - |
isoproterenol | soluble enzyme form | Oryctolagus cuniculus | |
0.156 | - |
R-salsolinol | soluble enzyme form | Sus scrofa | |
0.168 | 0.345 | epinephrine | soluble enzyme form | Rattus norvegicus | |
0.207 | - |
dopamine | recombinant enzyme expressed in Sf9 cells, soluble enzyme form | Homo sapiens | |
0.242 | - |
epinephrine | soluble enzyme form | Mus musculus | |
0.266 | - |
levodopa | recombinant enzyme expressed in Sf9 cells, membrane-bound enzyme form | Homo sapiens | |
0.28 | - |
dopamine | soluble enzyme form, brain | Homo sapiens | |
0.304 | 0.464 | norepinephrine | soluble enzyme form | Rattus norvegicus | |
0.369 | - |
norepinephrine | recombinant enzyme expressed in Sf9 cells, soluble enzyme form | Homo sapiens | |
0.613 | - |
levodopa | recombinant enzyme expressed in Sf9 cells, soluble enzyme form | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
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 | - |
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 | - |
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 | - |
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 | - |
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 | - |
soluble | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Mus musculus | - |
- |
soluble | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Homo sapiens | - |
- |
soluble | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Sus scrofa | - |
- |
soluble | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Oryctolagus cuniculus | - |
- |
soluble | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Rattus norvegicus | - |
- |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
24300 | - |
S-COMT | Homo sapiens |
30000 | - |
MB-COMT | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Oryctolagus cuniculus | - |
- |
- |
Rattus norvegicus | P22734 | - |
- |
Sus scrofa | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
additional information | S-COMT is a nonglycosylated protein | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
aorta | - |
Oryctolagus cuniculus | - |
brain | - |
Homo sapiens | - |
brain | - |
Sus scrofa | - |
brain | - |
Rattus norvegicus | - |
kidney | - |
Rattus norvegicus | - |
liver | - |
Mus musculus | - |
liver | - |
Rattus norvegicus | - |
placenta | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
S-adenosyl-L-methionine + 2-hydroxyestradiol | - |
Oryctolagus cuniculus | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + catechol | - |
Homo sapiens | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + dopamine | - |
Homo sapiens | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + epinephrine | - |
Mus musculus | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + epinephrine | - |
Rattus norvegicus | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + isoproterenol | - |
Oryctolagus cuniculus | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + levodopa | - |
Homo sapiens | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + norepinephrine | - |
Homo sapiens | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + norepinephrine | - |
Rattus norvegicus | S-adenosyl-L-homocysteine + ? | - |
? | |
S-adenosyl-L-methionine + R-salsolinol | - |
Sus scrofa | S-adenosyl-L-homocysteine + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
MB-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Mus musculus |
MB-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Homo sapiens |
MB-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Sus scrofa |
MB-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Oryctolagus cuniculus |
MB-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Rattus norvegicus |
S-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Mus musculus |
S-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Homo sapiens |
S-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Sus scrofa |
S-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Oryctolagus cuniculus |
S-COMT | two molecular forms: a soluble form (S-COMT) and in another form associated with membranes (MB-COMT) | Rattus norvegicus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00027 | - |
tolcapone | - |
Homo sapiens | |
0.0003 | - |
entacapone | - |
Homo sapiens | |
0.00102 | - |
nitecapone | - |
Homo sapiens |