Drug methylation in cancer therapy: lessons from the TPMT polymorphism

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Enhanced proteolysis of thiopurine S-methyltransferase (TPMT) encoded by mutant alleles in humans (TPMT*3A, TPMT*2): mechanisms for the genetic polymorphism of TPMT activity.

TPMT is a cytosolic enzyme that catalyzes the S-methylation of aromatic and heterocyclic sulfhydryl compounds, including medications such as mercaptopurine and thioguanine. TPMT activity exhibits autosomal codominant genetic polymorphism, and patients inheriting TPMT deficiency are at high risk of potentially fatal hematopoietic toxicity. The most prevalent mutant alleles associated with TPMT d...

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ژورنال

عنوان ژورنال: Oncogene

سال: 2003

ISSN: 0950-9232,1476-5594

DOI: 10.1038/sj.onc.1206944