Description
6-Thioguanine is a nucleotide analog of guanine that exhibits anticancer chemotherapeutic, immunosuppressive, and anti-parasitic activities. 6-Thioguanine is incorporated into DNA, altering stability of the topoisomerase II-DNA cleavage complex and increasing DNA fragmentation; these actions result in growth arrest and inhibition of proliferation across many cancer cell lines. In acute lymphoblastic leukemia (ALL) cells, 6-thioguanine increases mitochondrial dysfunction and generation of ROS, inducing a cytotoxic effect. In other in vitro models, 6-thioguanine decreases expression of TNF-related apoptosis-inducing ligand (TRAIL). Additionally, this compound inhibits growth of Toxoplasma gondii.
References
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Thomas CW, Myhre GM, Tschumper R, et al. Selective inhibition of inflammatory gene expression in activated T lymphocytes: a mechanism of immune suppression by thiopurines. J Pharmacol Exp Ther. 2005 Feb;312(2):537-45. PMID: 15388785.
Pfefferkorn ER, Bzik DJ, Honsinger CP. Toxoplasma gondii: mechanism of the parasitostatic action of 6-thioxanthine. Exp Parasitol. 2001 Dec;99(4):235-43. PMID: 11888251.
Morgan CJ, Chawdry RN, Smith AR, et al. 6-Thioguanine-induced growth arrest in 6-mercaptopurine-resistant human leukemia cells. Cancer Res. 1994 Oct 15;54(20):5387-93. PMID: 7923170.
