Mittl Peer Re, Grütter Markus G
Institute for Biochemistry, University of Zürich, Winterthurer Strasse 190, 8057 Zürich, Switzerland.
Curr Opin Struct Biol. 2006 Dec;16(6):769-75. doi: 10.1016/j.sbi.2006.10.014. Epub 2006 Nov 16.
As a result of the recent enormous technological progress, experimental structure determination has become an integral part of the development of drugs against disease-related target proteins. The post-translational modification of proteins is an important regulatory process in living organisms; one such example is lytic processing by peptidases. Many different peptidases represent disease targets and are being used in structure-based drug design approaches. The development of drugs such as aliskiren and tipranavir, which inhibit renin and HIV protease, respectively, testifies to the success of this approach.
由于最近取得的巨大技术进步，实验性结构测定已成为开发针对与疾病相关的靶蛋白的药物的一个组成部分。蛋白质的翻译后修饰是生物体中一个重要的调节过程；一个这样的例子是肽酶的裂解加工。许多不同的肽酶是疾病靶点，并被用于基于结构的药物设计方法中。分别抑制肾素和HIV蛋白酶的药物阿利吉仑和替拉那韦的开发证明了这种方法的成功。
