Thiopurine S-methyltransferase

Definition:

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.

References:

[1]. Yi Peng, et al. Structural basis of substrate recognition in thiopurine s-methyltransferase. Biochemistry. 2008 Jun 10;47(23):6216-25. [Content Brief]

[2]. R M Weinshilboum, et al. Human erythrocyte thiopurine methyltransferase: radiochemical microassay and biochemical properties. Clin Chim Acta. 1978 May 2;85(3):323-33. [Content Brief]

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