Department of Biochemistry and Molecular Biology, School of Biomedical Sciences, Monash University, Wellington Road, Clayton, VIC 3800, Australia.
Biochem Soc Trans. 2013 Aug;41(4):975-80. doi: 10.1042/BST20130075.
Approximately 10% of the human kinome has been classified as pseudokinases due to the absence of one or more of three motifs known to play key roles in the catalytic activities of protein kinases. Structural and functional studies are now emerging, reclassifying this 'dead' kinase family as essential signalling molecules that act as crucial modulators of signal transduction. This raises the prospect that pseudokinases may well represent an as-yet-unexplored class of drug targets. However, the extent to which nucleotide binding and catalytic activity contribute to the biological functions of pseudokinases remains an area of great controversy. In the present review, we discuss the advantages and disadvantages of the different methods employed to characterize the nucleotide-binding properties and activity of pseudokinases.
大约 10%的人类激酶组被归类为假激酶，因为它们缺乏三个已知在蛋白激酶的催化活性中起关键作用的基序之一或多个。结构和功能研究正在出现，将这个“死亡”的激酶家族重新分类为重要的信号分子，作为信号转导的关键调节剂。这提出了一个前景，即假激酶可能代表一个尚未探索的药物靶点类别。然而，核苷酸结合和催化活性在多大程度上促进假激酶的生物学功能仍然是一个极具争议的领域。在本综述中，我们讨论了用于表征假激酶的核苷酸结合特性和活性的不同方法的优缺点。
