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Pathway Description
Tioguanine Action Pathway
Homo sapiens
Drug Action Pathway
Tioguanine is an antineoplastic agent from the purine analog class. This drug also has antimetabolite action. Tioguanine is indicated for remission induction and remission consolidation in the treatment of acute nonlymphocytic leukemias. When this drug enters the cells, it competes with hypoxanthine and guanine for the hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP is a cytotoxic agent, it will interfere with the synthesis of guanine nucleotides by inhibiting the glutamine-5-phosphoribosylpyrophosphate aminotransferase (de novo pathway of purine ribonucleotide synthesis) enzyme by pseudofeedback. Furthermore, TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine nucleotides are incorporated into both the DNA and the RNA. The final result is the sequential blockade of the usage and synthesis of purines, leading to apoptosis in the S phase of the cell cycle. This drug is administered as an oral tablet. An overdose of tioguanine may result in symptoms like nausea, vomiting, malaise, hypotension, and diaphoresis.
References
Tioguanine Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Schwartz EL, Ishiguro K, Sartorelli AC: Induction of leukemia cell differentiation by chemotherapeutic agents. Adv Enzyme Regul. 1983;21:3-20. doi: 10.1016/0065-2571(83)90005-5.
Pubmed: 6400065
Schwartz EL, Ishiguro K, Sartorelli AC: Induction of leukemia cell differentiation by chemotherapeutic agents. Adv Enzyme Regul. 1983;21:3-20. doi: 10.1016/0065-2571(83)90005-5.
Pubmed: 6400065
Elgemeie GH: Thioguanine, mercaptopurine: their analogs and nucleosides as antimetabolites. Curr Pharm Des. 2003;9(31):2627-42. doi: 10.2174/1381612033453677.
Pubmed: 14529546
Bai J, Lai L, Yeo HC, Goh BC, Tan TM: Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione. Int J Biochem Cell Biol. 2004 Feb;36(2):247-57. doi: 10.1016/s1357-2725(03)00236-x.
Pubmed: 14643890
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