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 (O55060) - Overview - Molecular Target Synopsis

Protein


Tpmt, Thiopurine S-methyltransferase
Enzyme Classification 2.1.1.67
UniProt O55060

Also Known as TPMT_MOUSE, Tpmt

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

3BGD
THIOPURINE S-METHYLTRANSFERASE
RCSB/PDB
Inspect Structure
See all 3D Structures for Tpmt

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
240O55060-1

Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project Tpmt has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

3D Structures


For Tpmt there are:
3 structures (6 chains) solved
3 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

Tpmt is solved in complex with the approved drug(s):

PM6/MERCAPTOPURINE (3BGD_A, 3BGD_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


Tpmt has been screened with compounds ( bioactivities). (see details)