Gershkovich A A
Ukr Biokhim Zh (1978). 1994 Jan-Feb;66(1):10-29.
The design and application of a successfully developed type of fluorogenic substrates for proteolytic enzymes are discussed. Proteolytic enzymes play a key role not only in the regulation of cellular protein turnover but also in the control of many other physiological functions. Substrates consisting of the appropriate peptides with chromophore or fluorophore at the C-termini are often employed to detect protease activity. Proteases exhibit the primary specificity to the particular amino acid residue and hydrolyze the following peptide bond. However, it is impossible to investigate the specific recognition of the other side of a scissible bond. Intramolecularly quenched fluorescent substrates are very useful instruments for research and medical purpose due to their high sensitivity and selectivity to proteases.
本文讨论了一种成功开发的用于蛋白水解酶的荧光底物的设计与应用。蛋白水解酶不仅在细胞内蛋白质周转的调节中起关键作用,而且在许多其他生理功能的控制中也起着关键作用。通常使用在C端带有发色团或荧光团的合适肽组成的底物来检测蛋白酶活性。蛋白酶对特定氨基酸残基具有主要特异性,并水解随后的肽键。然而,不可能研究可裂解键另一侧的特异性识别。由于其对蛋白酶具有高灵敏度和选择性,分子内淬灭荧光底物是用于研究和医学目的的非常有用的工具。