Methylation of mercaptopurine,
thioguanine and their nucleotide metabolites by heterologously expressed human thipurine S-methyltransferase.
Thiopurine drugs including azathioprine, mercaptopurine and
thioguanine suppress the immune system and are used in a range of diseases such as lymphoma and leukemia, psoriasis, severe eczema and inflammatory bowel disease.
The oncologists at Ochsner, after warning the patient and his family that this malignancy represented the most aggressive form of leukemia, recommended that he immediately begin treatment with the chemotherapy drugs
thioguanine and cytosine arabinoside.
Background & objectives: Mercaptopurine, azathioprine, and
thioguanine, used as antineoplastic agents and immunosuppressants are catabolized by thiopurine methyltransferase (TPMT) enzyme, which exhibits genetic polymorphism.
Mercaptopurine treatment leads to the incorporation of
thioguanine into DNA ([G.sup.s]-DNA).
In the early 1950s, Elion and Hitchings developed
thioguanine and 6-mercaptopurine, which helped cure childhood leukemia.
A comparative trial of daunorubicin, cytosine arabinoside, and
thioguanine, and a combination of the three agents for the treatment of acute myelocytic leukemia.
The patient received induction therapy for B-ALL, consisting of dexamethasone, vincristine, idarubicin, cyclophosphamide, cytarabine, and
thioguanine, along with intrathecal methotrexate.
The one false-negative,
thioguanine, may have been missed because of the weak germline expression in C.
of patients Therapeutic effect
Thioguanine 12 RCDI 10 patients tolerated TG.