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

TPMT (P51580) - Overview - Molecular Target Synopsis

Protein


TPMT, Thiopurine S-methyltransferase
Enzyme Classification 2.1.1.67
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.

2H11
AMINO-TERMINAL TRUNCATED THIOPURINE S-METHYLTRANSFERASE COMPLEXED WITH S-ADENOSYL-L-HOMOCYSTEINE
RCSB/PDB
Inspect Structure
See all 3D Structures for TPMT

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
245ENSG00000137364ENST00000309983ENSP00000312304P51580-1

Sub-cellular localization


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



UniProt
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)