Human thiopurine methyltransferase: no evidence of activation by its substrates

Ieva Stupans, Amra Kirlich, Ross McKinnon

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

A HPLC assay was developed to assay baculovirus expressed human thiopurine methyltransferase activity. Using 6-mercaptopurine as substrate, the expressed thiopurine methyltransferase was found to have an apparent Km of 0.99 mM and a Vmax of 19 nmoles/mg/min. These values are in agreement with those determined using the standard radiometric assay for thiopurine methyltransferase activity. The effects of 6-thioguanine on 6-mercaptopurine metabolism were determined. 6-Thioguanine was found to be a mixed inhibitor of 6-mercaptopurine methylation.
Original languageEnglish
Pages (from-to)343-350
Number of pages8
JournalLife Sciences
Volume62
Issue number4
DOIs
Publication statusPublished - 1998
Externally publishedYes

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