摘要
Plk1是一类从酵母到人类都高度保守的丝氨酸/苏氨酸蛋白激酶。Plk1与不同的细胞周期检查点的精密调控有关,从而确保了细胞周期事件按照严格的时间和顺序正常进行。Plk1在增殖活跃的细胞中呈高水平表达,Plk1的高度表达和肿瘤患者的低存活率之间具有显著的统计相关性。Plk1可能是非常有效的抗癌药物设计的靶点。目前已有几种Plk1的小分子抑制剂在体内外的实验中显示出了良好的应用前景。
Polo-like kinase 1 (Plkl) contain an N-terminal Ser/Thr kinase catalytic domain ana a Cterminal region that contains two polo-boxes. As a key regulator of multiple steps during cell cycle across eukaryotic species, many proteins interact with Plkl. Plkl is highly expressed in malignant cells and serves as a negative prognostic marker in specific human cancer types. Plk1 is a potential target for cancer therapy. Some novel small-molecule inhibitors of polo-like kinase 1 provide novel opportunities for cancer-drug discovery, such as BI 2536, ON01910.
出处
《中国生物工程杂志》
CAS
CSCD
北大核心
2007年第5期142-145,共4页
China Biotechnology