AURKA基因编码一种丝氨酸/苏氨酸激酶,调节有丝分裂细胞周期进程。AURKA在活跃的增殖细胞中表达,特别是在细胞周期的G2和有丝分裂阶段中,在促进细胞分裂中具有多种作用,包括微管成核蛋白向中心体募集以介导纺锤体组装和调节进入有丝分裂。AURKA扩增已在多种肿瘤类型中观察到,包括白血病、结直肠癌和胰腺癌。AURKA的过度表达可促进细胞转化,并可能增强其他癌基因的活性,如RAS。AURKA的小分子抑制剂(以及相关的Aurora B和C激酶)目前作为细胞增殖和潜在的抗有丝分裂化疗药物的一般抑制剂来研究。
AURKA (Aurora kinase A) is a cell-cycle regulatory serine/threonine kinase that promotes entry into and proper progression through mitosis. AURKA is expressed in actively proliferating cells, specifically in the G2 and mitotic phases of the cell cycle, and has multiple roles in promoting cell division, including recruitment of microtubule-nucleating proteins to centrosomes to mediate spindle assembly and regulating entry into mitosis. AURKA amplification has been observed in multiple tumor types, including leukemia, colorectal, and pancreatic cancers. Overexpression of AURKA can promote cellular transformation and may potentiate the activity of other oncogenes, such as RAS. Small-molecule inhibitors of AURKA (and the related Aurora B and C kinases) are currently being investigated as general inhibitors of cell proliferation and potential anti-mitotic chemotherapeutic drugs.
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