Haspin 激酶的功能和抑制：通过抗有丝分裂靶向多种癌症疗法,Journal of Pharmacy and Pharmacology

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Haspin 激酶的功能和抑制：通过抗有丝分裂靶向多种癌症疗法
Journal of Pharmacy and Pharmacology ( IF 2.8 ) Pub Date : 2022-11-05 , DOI: 10.1093/jpp/rgac080
Yongjian Liu ₁ , Hongliu Yang ₁ , Yongsheng Fang ₁ , Yantao Xing ₁ , Xinxin Pang ₁ , Yang Li ₁ , Yuanyuan Zhang ₁ , Yonggang Liu ₁

Affiliation

目的单倍体生殖细胞特异性核蛋白激酶 (Haspin) 是一种丝氨酸/苏氨酸激酶，是一种非典型激酶，在结构上不同于常规蛋白激酶。主要发现在功能上，Haspin 参与重要的细胞周期进程，特别是在关键的有丝分裂中调节着丝粒姐妹染色单体在前期和前期的凝聚力，并随后确保中期染色体正确排列和后期染色体正常分离。然而，越来越多的证据表明，除正常增殖的体细胞外，Haspin 在多种癌细胞中显着上调。其敲低或小分子抑制可以通过破坏有丝分裂的正常进程来阻止癌细胞生长并诱导细胞凋亡。鉴于其表达的组织或细胞的特异性及其目前已知底物的独特性，Haspin 可能是一个有前途的抗癌靶点。因此，Haspin 的选择性合成和天然抑制剂已得到广泛开发，以确定它们在体内和体外对各种癌细胞的抑制能力。总结在这里，我们的观点包括对 Haspin 的作用和结构、其相对有效和选择性的抑制剂以及 Haspin 在多种癌症中的初步研究的全面回顾。

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Function and inhibition of Haspin kinase: targeting multiple cancer therapies by antimitosis

Objectives Haploid germ cell-specific nuclear protein kinase (Haspin) is a serine/threonine kinase as an atypical kinase, which is structurally distinct from conventional protein kinases. Key findings Functionally, Haspin is involved in important cell cycle progression, particularly in critical mitosis regulating centromeric sister chromatid cohesion during prophase and prometaphase, and subsequently ensuring proper chromosome alignment during metaphase and the normal chromosome segregation during anaphase. However, increasing evidence has demonstrated that Haspin is significantly upregulated in a variety of cancer cells in addition to normal proliferating somatic cells. Its knockdown or small molecule inhibition could prevent cancer cell growth and induce apoptosis by disrupting the regular mitotic progression. Given the specificity of its expressed tissues or cells and the uniqueness of its current known substrate, Haspin can be a promising target against cancer. Consequently, selective synthetic and natural inhibitors of Haspin have been widely developed to determine their inhibitory power for various cancer cells in vivo and in vitro. Summary Here our perspective includes a comprehensive review of the roles and structure of Haspin, its relatively potent and selective inhibitors and Haspin’s preliminary studies in a variety of cancers.

更新日期：2022-11-05

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