Catechol-O-methyltransferase

Target id: 2472

Nomenclature: Catechol-O-methyltransferase

Abbreviated Name: COMT

Family: Catecholamine turnover

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for Catechol-O-methyltransferase in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 271 22q11.21 COMT catechol-O-methyltransferase
Mouse - 265 16 A3 Comt catechol-O-methyltransferase
Rat - 264 11q23 Comt catechol-O-methyltransferase
Previous and Unofficial Names
Comt1
Database Links
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.1.1.6 S-adenosyl-L-methionine + a catechol = S-adenosyl-L-homocysteine + a guaiacol
Description Reaction Reference
(-)-Noradrenaline -> normetanephrine
(-)-Adrenaline -> metanephrine
3,4-Dihydroxymandelic acid -> vanillylmandelic acid
Dopamine -> 3-methoxytyramine
Cofactors
Cofactor Species Comments Reference
S-adenosyl methionine Human

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
tolcapone Hs Inhibition 9.5 – 9.6 pKi 2
pKi 9.6 (Ki 2.7x10-10 M) soluble enzyme [2]
Description: soluble enzyme
pKi 9.5 (Ki 2.9x10-10 M) membrane-bound enzyme [2]
Description: membrane-bound enzyme
entacapone Hs Inhibition 8.7 – 9.5 pKi 2
pKi 9.5 (Ki 3x10-10 M) soluble enzyme [2]
Description: soluble enzyme
pKi 8.7 (Ki 2x10-9 M) membrane-bound enzyme [2]
Description: membrane-bound enzyme
opicapone Hs Inhibition 9.0 pKi 1
pKi 9.0 (Ki 1x10-9 M) [1]
opicapone Mm Inhibition 8.8 pKi 1
pKi 8.8 (Ki 1.5x10-9 M) [1]
opicapone Rn Inhibition 8.8 pKi 1
pKi 8.8 (Ki 1.5x10-9 M) [1]
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Alcohol dependence
Disease Ontology: DOID:0050741
OMIM: 103780
Disease:  DiGeorge syndrome
Disease Ontology: DOID:11198
OMIM: 188400
Orphanet: ORPHA567
Disease:  Panic disorder 1; PAND1
Disease Ontology: DOID:594
OMIM: 167870
Disease:  Schizophrenia
Disease Ontology: DOID:5419
OMIM: 181500
Orphanet: ORPHA3140
Disease:  Velocardiofacial syndrome
Disease Ontology: DOID:12583
OMIM: 192430
Orphanet: ORPHA567

References

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1. Lanier M, Ambrus G, Cole DC, Davenport R, Ellery J, Fosbeary R, Jennings AJ, Kadotani A, Kamada Y, Kamran R et al.. (2014) A fragment-based approach to identifying S-adenosyl-l-methionine -competitive inhibitors of catechol O-methyl transferase (COMT). J. Med. Chem.57 (12): 5459-63. [PMID:24847974]

2. Lotta T, Vidgren J, Tilgmann C, Ulmanen I, Melén K, Julkunen I, Taskinen J. (1995) Kinetics of human soluble and membrane-bound catechol O-methyltransferase: a revised mechanism and description of the thermolabile variant of the enzyme. Biochemistry34 (13): 4202-10. [PMID:7703232]

How to cite this page

Catecholamine turnover: Catechol-O-methyltransferase. Last modified on 18/01/2016. Accessed on 24/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2472.