Georgakis Nikolaos, Ioannou Elisavet, Varotsou Christina, Premetis Georgios, Chronopoulou Evangelia G, Labrou Nikolaos E
Laboratory of Enzyme Technology, Department of Biotechnology, School of Applied Biology and Biotechnology, Agricultural University of Athens, Athens, Greece.
Methods Mol Biol. 2020;2089:41-46. doi: 10.1007/978-1-0716-0163-1_3.
Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. Enzymes are one of the most important groups of drug targets; thus, enzyme inhibition is widely used for the treatment of certain disorders. The assessment of an inhibitor against an enzyme is predominantly based on two different parameters: the half-maximal inhibitory concentration (IC) and the inhibition constant (K). This chapter describes an experimental procedure for the determination of the IC value of an enzyme inhibitor. The relationship between IC and K is also discussed.
药物研发是指在通过药物发现过程确定了先导化合物后，将一种新的药物推向市场的过程。酶是最重要的药物靶点类别之一；因此，酶抑制作用被广泛用于治疗某些疾病。评估一种酶抑制剂主要基于两个不同的参数：半数最大抑制浓度（IC）和抑制常数（K）。本章介绍了一种测定酶抑制剂IC值的实验方法。同时也讨论了IC与K之间的关系。
