Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd, Grenzacherstrasse 124, 065/208A, 4070 Basel, Switzerland.
Drug Discov Today. 2021 Apr;26(4):875-886. doi: 10.1016/j.drudis.2021.01.006. Epub 2021 Jan 14.
Enzymes are essential, physiological catalysts involved in all processes of life, including metabolism, cellular signaling and motility, as well as cell growth and division. They are attractive drug targets because of the presence of defined substrate-binding pockets, which can be exploited as binding sites for pharmaceutical enzyme inhibitors. Understanding the reaction mechanisms of enzymes and the molecular mode of action of enzyme inhibitors is indispensable for the discovery and development of potent, efficacious, and safe novel drugs. The combination of classical concepts of enzymology with new experimental and data analysis methods opens new routes for drug discovery.
酶是生命过程中所有代谢、细胞信号和运动以及细胞生长和分裂等生理过程中必不可少的催化剂。它们是有吸引力的药物靶点,因为存在定义明确的底物结合口袋,可以将其用作药物酶抑制剂的结合位点。了解酶的反应机制和酶抑制剂的分子作用模式对于发现和开发有效、安全的新型药物是不可或缺的。将经典的酶学概念与新的实验和数据分析方法相结合,为药物发现开辟了新的途径。