Protein kinases constitute a large group of enzymes in eukaryotes and have an important role in many cellular processes. Several of these proteins are active kinases, such as haploid germ cell-specific nuclear protein kinase (Haspin), an atypical eukaryotic protein kinase that lacks sequence similarity with other eukaryotic protein kinases. Haspin is a serine/threonine kinase that associates with chromosome and phosphorylates threonine 3 of histone 3 during mitosis. Haspin overexpression or deletion results in defective mitosis. It has been shown that Haspin inhibitors have potent anti-tumoral effects. Given that the only Haspin substrate is threonine 3 of histone 3, inhibition of Haspin might have fewer adverse effects compared with other anticancer agents. Here, we highlight the chemical structures and actions of currently known Haspin inhibitors.

蛋白激酶构成了真核生物中的一大类酶，并且在许多细胞过程中都起着重要作用。这些蛋白中的几种是活性激酶，例如单倍体生殖细胞特异性核蛋白激酶（Haspin），这是一种非典型的真核蛋白激酶，与其他真核蛋白激酶缺乏序列相似性。Haspin是一种丝氨酸/苏氨酸激酶，在有丝分裂过程中与染色体缔合并使组蛋白3的苏氨酸3磷酸化。Haspin过表达或缺失会导致有丝分裂不良。已经表明，Haspin抑制剂具有有效的抗肿瘤作用。鉴于唯一的Haspin底物是组蛋白3的苏氨酸3，与其他抗癌药相比，抑制Haspin的不良反应可能更少。这里，