The thiopurines: An update View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2005-12

AUTHORS

Sally Coulthard, Linda Hogarth

ABSTRACT

The thiopurine drugs, 6-mercaptopurine (6-MP), 6-thioguanine (6-TG) are commonly used cytotoxic agents. A derivative of 6-MP, azathioprine, is commonly used as an immunosuppressant. A prominent route for the metabolism of these agents is mediated by the enzyme thiopurine methyltransferase (TPMT). This enzyme exhibits considerable inter-individual variation in activity, partly due to the presence of common genetic polymorphisms, which influence cytotoxicity of the thiopurine drugs. Variations in the number of tandem repeats in the 5' promoter region have also been shown to influence TPMT expression in vitro. In this article, we review the impact of variations in TPMT activity on sensitivity to the thiopurine drugs in vitro and also in vivo in terms of their clinical efficacy and toxicity. A possible relationship between TPMT and secondary malignancies is also reviewed. More... »

PAGES

523-532

References to SciGraph publications

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s10637-005-4020-8

DOI

http://dx.doi.org/10.1007/s10637-005-4020-8

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1043851224

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/16267626


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