Since accelerated metabolism produces much higher levels of reactive oxygen species (ROS) in cancer cells compared to ROS levels found in normal cells, human MutT homolog 1 (MTH1), which sanitizes oxidized nucleotide pools, was recently demonstrated to be crucial for the survival of cancer cells, but not required for the proliferation of normal cells. Therefore, dozens of MTH1 inhibitors have been developed with the aim of suppressing cancer growth by accumulating oxidative damage in cancer cells. While several inhibitors were indeed confirmed to be effective, some inhibitors failed to kill cancer cells, complicating MTH1 as a viable target for cancer eradication. In this review, we summarize the current status of developing MTH1 inhibitors as drug candidates, classify the MTH1 inhibitors based on their structures, and offer our perspectives toward the therapeutic potential against cancer through the targeting of MTH1.

与正常细胞中的ROS水平相比，由于加速的新陈代谢在癌细胞中产生更高水平的活性氧（ROS）水平，因此最近证明了人类MutT同系物1（MTH1）可以对氧化的核苷酸池进行消毒，这对于维持生存至关重要。癌细胞，但正常细胞的增殖不是必需的。因此，已经开发了数十种MTH1抑制剂，其目的是通过在癌细胞中积累氧化损伤来抑制癌症的生长。尽管确实证实了几种抑制剂是有效的，但一些抑制剂未能杀死癌细胞，使MTH1成为根除癌症的可行靶标。在这篇综述中，我们总结了开发MTH1抑制剂作为候选药物的现状，根据其结构对MTH1抑制剂进行了分类，