Wee1 kinase plays an important role in regulating G2/M checkpoint and S phase, and the inhibition of it will lead to mitotic catastrophe in cancer cells with p53 mutation or deletion. Therefore, the mechanism of Wee1 kinase in cancer treatment and the development of its inhibitors have become a research hotspot.

However, although a variety of Wee1 inhibitors with different scaffolds and considerable activity have been successfully identified, so far no one has systematically summarized the structure-activity relationships (SARs) of Wee1 inhibitors. Previous reviews mainly focused on its mechanism and clinical application.

To facilitate the rational design and development of Wee1 inhibitors in the future, this paper systematically summarizes its structural types, SARs and binding modes according to the Wee1 inhibitors reported in scientific journals, and also summarizes the regulatory effect of Wee1 kinase on cell cycle and the progress of its inhibitors in clinical application.

Wee1激酶在调节G2 / M检查点和S期中起着重要作用，对其的抑制将导致p53突变或缺失的癌细胞发生有丝分裂灾难。因此，Wee1激酶在癌症治疗中的作用机理及其抑制剂的研究已成为研究热点。

然而，尽管已经成功地鉴定出了具有不同支架和相当大活性的多种Wee1抑制剂，但到目前为止，还没有人系统地总结Wee1抑制剂的结构-活性关系（SAR）。以往的评论主要集中在其机理和临床应用上。

为便于将来合理设计和开发Wee1抑制剂，本文根据科学期刊上报道的Wee1抑制剂系统总结了其结构类型，SAR和结合方式，并总结了Wee1激酶对细胞周期和细胞凋亡的调控作用。抑制剂在临床上的应用进展。