6-thioguanine

6-thioguanine

6-thioguanine is a poisonous substance that is incorporated into DNA during replication by the HPRT enzyme, causing cell death. It is generated through the action of the enzyme 5-monophosphate synthase, which converts 6-TXPM into 6-thioguanine (6-TG). 6-thioguanine acts as a false metabolite, blocking the synthesis of lymphocytes.From: Nanotechnology in Nutraceuticals [2019], Recombinogenic, genotoxic, and cytotoxic effects of azathioprine using in vivo assays [2021]

Mechanisms of Different Anticancer Drugs

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Published in Anjana Pandey, Saumya Srivastava, Recent Advances in Cancer Diagnostics and Therapy, 2022

Anjana Pandey, Saumya Srivastava

6-Thioguanine is a guanine analog, blocks various purine biosynthesis steps (Wang et al., 2016), and is widely incorporated in DNA itself. It is already reported that there is a close association between 6-TG incorporation into DNA and cell sensitivity. 6-TG is most commonly involved in acute leukemia treatment (Munshi et al., 2014).

Recombinogenic, genotoxic, and cytotoxic effects of azathioprine using in vivo assays

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Published in Journal of Toxicology and Environmental Health, Part A, 2021

A. V. D. Melo Bisneto, L. C. D. Oliveira, A. Silva Fernandes, L. S. Silva, J. H. Véras, C. G. Cardoso, Carolina R. E Silva, A. V. de Moraes Filho, C. C. Carneiro, L. Chen-Chen

To promote pharmacological effects, following oral administration, the Aza molecule is cleaved by enzymatic actions of glutathione transferases, giving rise to the nitroimidazole group and 6-mercaptopurine (6-MP). Subsequently, 6-MP is transformed by hypoxanthine-phosphoribosyl transferase into 6-thioinosine monophosphate, which is converted to 6-thioxanthine monophosphate (6-TXPM) by inosine-5-monophosphate dehydrogenase. Finally, through the action of the enzyme 5-monophosphate synthase, 6-TXPM generated 6-thioguanine (6-TG) which is incorporated into DNA as a false metabolite, blocking the synthesis of lymphocytes (FDA 2011).

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Mechanisms of Different Anticancer Drugs

Recombinogenic, genotoxic, and cytotoxic effects of azathioprine using in vivo assays