Bhalla Nikhil, Estrela Pedro
Okinawa Institute of Science and Technology Graduate University (OIST) 1919-1 Tancha, Onna, Kunigami District, Okinawa Prefecture 904-0412, Japan.
Department of Electronic and Electrical Engineering, University of Bath, Bath BA2 7AY, United Kingdom.
Curr Top Med Chem. 2017;17(22):2470-2481. doi: 10.2174/1568026617666170531113233.
For successful drug discovery it is important to understand the fundamentals of the underlying causes and consequences of the diseases for which the drug is being developed. One such physiological process in eukaryotic cells is protein phosphorylation, which is the main post-translational modification of proteins responsible for the onset or progression of Alzheimer's disease, diabetes and various cancers. Protein phosphorylation is facilitated by kinases and inhibitors of kinases act as drugs in controlling or curing these diseases by reducing protein phosphorylation. This review discusses the technologies capable of detecting kinase activity and screening candidate compounds to identify novel inhibitors of protein kinases.
对于成功的药物研发而言,了解所研发药物针对的疾病的根本病因及后果的基本原理非常重要。真核细胞中的一种此类生理过程是蛋白质磷酸化,它是蛋白质的主要翻译后修饰,与阿尔茨海默病、糖尿病及各种癌症的发生或发展有关。激酶促进蛋白质磷酸化,而激酶抑制剂可作为药物,通过减少蛋白质磷酸化来控制或治愈这些疾病。本文综述了能够检测激酶活性并筛选候选化合物以鉴定新型蛋白激酶抑制剂的技术。