Department of Cancer and Surgery, Imperial College, Hammersmith Hospital Campus, Du Cane Road, London, W12 ONN, UK.
Cell Signal. 2012 Jun;24(6):1173-84. doi: 10.1016/j.cellsig.2012.01.017. Epub 2012 Feb 4.
Kinases play a critical role in regulating many cellular functions including development, differentiation and proliferation. To date, over 518 proteins with kinase activity, comprising ~2-3% of total cellular proteins, have been identified from within the human kinome. Interestingly, approximately 10% of kinases are categorised as pseudokinases since they lack one or more conserved catalytic residues within their kinase domain and were originally thought to have no enzymatic activity. Recently, there has been strong evidence to suggest that some pseudokinsases can not only function as scaffold proteins, but may also possess kinase activity leading to modulation of cell signalling pathways. Altered activity of these pseudokinases can result in impaired cellular function, particularly in malignancies. In this review we are discussing recent evidence that apart from a scaffolding role, pseudokinases also orchestrate cellular processes as active kinases per se in signalling pathways of malignant cells.
激酶在调节许多细胞功能中起着关键作用，包括发育、分化和增殖。迄今为止，已经从人类激酶组中鉴定出超过 518 种具有激酶活性的蛋白质，约占总细胞蛋白的 2-3%。有趣的是，大约 10%的激酶被归类为假激酶，因为它们在激酶结构域内缺乏一个或多个保守的催化残基，最初被认为没有酶活性。最近有强有力的证据表明，一些假激酶不仅可以作为支架蛋白发挥作用，而且还可能具有激酶活性，从而调节细胞信号通路。这些假激酶活性的改变会导致细胞功能受损，特别是在恶性肿瘤中。在这篇综述中，我们讨论了最近的证据，除了支架作用外，假激酶还作为活性激酶本身在恶性细胞的信号通路中协调细胞过程。
