Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

COMT (P21964) - Overview - Molecular Target Synopsis

Protein


COMT, Catechol O-methyltransferase
Enzyme Classification 2.1.1.6
UniProt P21964

Also Known as COMT_HUMAN, COMT

Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOPA, alpha-methyl DOPA and isoproterenol.

5LSA
HUMAN CATECHOL O-METHYLTRANSFERASE IN COMPLEX WITH SAM AND DNC AT 1.50A
RCSB/PDB
Inspect Structure
See all 3D Structures for COMT

Isoforms / Transcripts (Protein Coding)


Drugs


COMT is targeted by Approved Drugs Tolcapone, Entacapone. (see details)
Tolcapone
Entacapone

Sub-cellular localization


UniProt: COMT is active in the following subcellular-locations: cell membrane, cytoplasm.
GO terms: COMT is active in the following subcellular-locations: axon, cell body, cytosol, dendrite, dendritic spine, extracellular exosome, integral component of membrane, intracellular membrane-bounded organelle, membrane, plasma membrane, postsynaptic membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project COMT has gain in 10 cell-lines, loss in 1 cell-lines and no signal in 993 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: EKVX, NCI_H322M, K_562

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: CAL-12T, SNU-182, HCC515

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, HMEC, HUVEC

(see details)

3D Structures


For COMT there are:
10 structures (11 chains) solved
7 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


COMT has been screened with 152 compounds (227 bioactivities), 42 compounds have bioactivities that show binding affinity of <= 500nM (45 bioactivities). (see details)