Abstract: Cyclin E1 (CCNE1 gene coding) amplification, which is present in various malignant tumors, is closely associated with poor clinical outcomes in patients. At present, the treatment methods for CCNE1 amplified tumors are limited. As a member of Wee kinase family, membrane-associated tyrosine/threonine 1 kinase (PKMYT1) is a cell cycle regulatory enzyme that can affect cell mitosis by regulating the phosphorylation of cyclin-dependent kinase 1 (CDK1). It has been reported that there is a synthetic lethal effect between PKMYT1 inhibition and high expression of CCNE1. Therefore, PKMYT1 inhibitors may be a useful approach for the treatment of CCNE1-amplified tumors with good application prospect. This article mainly introduces the mechanism of action of PKMYT1, its relevance to diseases, and the research progress of small molecule PKMYT1 inhibitors, in order to provide some ideas for its further research and clinical application.