Department of Neurosciences, University of Toledo College of Medicine, Toledo, OH, USA.
Department of Biomedical Informatics, University of Cincinnati, Cincinnati, OH, USA; Division of Biomedical Informatics, Cincinnati Children's Hospital Medical Center, Cincinnati, OH, USA; Division of Biostatistics and Bioinformatics, Department of Environmental and Public Health Sciences, University of Cincinnati, Cincinnati, OH, USA; Department of Pharmacology and System Biology, College of Medicine, University of Cincinnati, Cincinnati, OH, USA; Department of Electrical Engineering and Computer Science, College of Engineering and Applied Sciences, University of Cincinnati, Cincinnati, OH, USA.
Curr Opin Pharmacol. 2022 Feb;62:117-129. doi: 10.1016/j.coph.2021.11.007. Epub 2021 Dec 27.
Biological regulatory networks are dynamic, intertwined, and complex systems making them challenging to study. While quantitative measurements of transcripts and proteins are key to investigate the state of a biological system, they do not inform the "active" state of regulatory networks. In consideration of that fact, "functional" proteomics assessments are needed to decipher active regulatory processes. Phosphorylation, a key post-translation modification, is a reversible regulatory mechanism that controls the functional state of proteins. Recent advancements of high-throughput protein kinase activity profiling platforms allow for a broad assessment of protein kinase networks in complex biological systems. In conjunction with sophisticated computational modeling techniques, these profiling platforms provide datasets that inform the active state of regulatory systems in disease models and highlight potential drug targets. Taken together, system-wide profiling of protein kinase activity has become a critical component of modern molecular biology research and presents a promising avenue for drug discovery.
生物调控网络是动态的、交织的、复杂的系统，这使得它们难以研究。虽然转录物和蛋白质的定量测量是研究生物系统状态的关键，但它们不能说明调控网络的“活跃”状态。考虑到这一事实，需要进行“功能”蛋白质组学评估来破译活跃的调控过程。磷酸化是一种关键的翻译后修饰，是一种可逆的调控机制，控制蛋白质的功能状态。高通量蛋白激酶活性分析平台的最新进展允许对复杂生物系统中的蛋白激酶网络进行广泛评估。与复杂的计算建模技术相结合，这些分析平台提供了数据集，可用于告知疾病模型中调控系统的活跃状态，并突出潜在的药物靶点。总之，蛋白激酶活性的系统分析已成为现代分子生物学研究的关键组成部分，并为药物发现提供了有前途的途径。
