TH1760 is a cell penetrant, potent and selective inhibitor of NUDT15 (NUDIX-type 15) that directly binds into the NUDT15 catalytic pocket. TH1760 sensitized cells to 6-thioguanine.
cell penetrant, potent and selective inhibitor of NUDT15 (NUDIX-type 15) that directly binds into the NUDT15 catalytic pocket
Nature chemical biology, 16(10), 1120-1128 (2020-07-22)
The NUDIX hydrolase NUDT15 was originally implicated in sanitizing oxidized nucleotides, but was later shown to hydrolyze the active thiopurine metabolites, 6-thio-(d)GTP, thereby dictating the clinical response of this standard-of-care treatment for leukemia and inflammatory diseases. Nonetheless, its physiological roles
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