Recombinant Human Thiopurine S-methyltransferase (TPMT)

Uniprot Id

P51580

Target Species

Human

Target Name

TPMT

Target Full Name

Thiopurine S-methyltransferase

Target Function

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. TPMT activity modulates the cytotoxic effects of thiopurine prodrugs. A natural substrate for this enzyme has yet to be identified.

Target Subcellular Location

Cytoplasm.

Target Protein Families

Class I-like SAM-binding methyltransferase superfamily, TPMT family

Target Research Area

Metabolism

Target Synonyms

HGNC:12014; S adenosyl L methionine thiopurine S methyltransferase; Thiopurine methyltransferase; Thiopurine S methyltransferase; Thiopurine S-methyltransferase; TPMT; TPMT_HUMAN

Target Background

This gene encodes the enzyme that metabolizes thiopurine drugs via S-adenosyl-L-methionine as the S-methyl donor and S-adenosyl-L-homocysteine as a byproduct. Thiopurine drugs such as 6-mercaptopurine are used as chemotherapeutic agents. Genetic polymorphisms that affect this enzymatic activity are correlated with variations in sensitivity and toxicity to such drugs within individuals, causing thiopurine S-methyltransferase deficiency. Related pseudogenes have been identified on chromosomes 3, 18 and X.