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The therapeutic effect of the thiopurines, 6-thioguanine (6-TG), 6-mercaptopurine, and its prodrug azathioprine, depends on the incorporation of 6-TG into cellular DNA. Unlike normal DNA bases, 6-TG absorbs UVA radiation, and UVA-mediated photochemical damage of DNA 6-TG has potentially harmful side effects. When free 6-TG is UVA irradiated in solution in the presence of molecular oxygen, reactive...
The thiopurine 6-thioguanine (S 6 G) is used to treat acute leukaemia. Its cytotoxic effect requires an active DNA mismatch repair (MMR) system. S 6 G is incorporated into DNA where a small fraction undergoes in situ conversion to S 6 -thiomethylguanine (S 6 meG). After replication, S 6 meG-containing base pairs interact with MMR. This interaction is ultimately...
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