Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

TPMT (P51580) - Overview - Molecular Target Synopsis


TPMT, Thiopurine S-methyltransferase
Enzyme Classification
UniProt P51580

Also Known as TPMT_HUMAN, TPMT

Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (also called mercaptopurine, 6-MP or its brand name Purinethol) and 6-thioguanine (also called tioguanine or 6-TG) using S-adenosyl-L-methionine as the methyl donor (PubMed:657528, PubMed:18484748). TPMT activity modulates the cytotoxic effects of thiopurine prodrugs. A natural substrate for this enzyme has yet to be identified. Monomer.

Isoforms / Transcripts (Protein Coding)

Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform

Sub-cellular localization

UniProt: TPMT is active in the following subcellular-locations: cytoplasm.
GO terms: TPMT is active in the following subcellular-locations: cytosol.

GO terms

Gene Copy Number Variation

In COSMIC - Cell Lines Project TPMT has gain in 4 cell-lines, loss in 1 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression

In NCI60, the highest expressing cell lines are: OVCAR_4, 786_0, OVCAR_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G28T, KYSE-70, 786-O

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: NHLF, NHEK, HSMM

(see details)

3D Structures

For TPMT there are:
2 structures (3 chains) solved
2 are solved in complex with at least one small molecule ligand

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry

TPMT has been screened with 42 compounds (42 bioactivities). (see details)