Lundstrom K
BioXtal, Chemin des Croisettes 22, 1066 Epalinges, Switzerland.
Cell Mol Life Sci. 2006 Nov;63(22):2597-607. doi: 10.1007/s00018-006-6252-y.
Structure-based drug discovery has proven useful in improving and shortening the drug development process. The approach of structural genomics to study a large number of targets in parallel has been commonly applied to protein families and even whole genomes. Paradoxically, although membrane proteins represent the largest type of drug targets, up to 70% today, determination of their structure has been modest compared to that of soluble proteins. Because membrane proteins are important for drug discovery an emphasis has been placed on developing technologies and methods to determine membrane protein structures. Several structural genomics initiatives have been established, focusing on the structural biology of membrane proteins.
基于结构的药物发现已被证明在改进和缩短药物开发过程中很有用。结构基因组学并行研究大量靶点的方法已普遍应用于蛋白质家族甚至整个基因组。矛盾的是,尽管膜蛋白是最大类型的药物靶点,如今占比高达70%,但其结构测定与可溶性蛋白相比却蛋白相比进展有限。由于膜蛋白对药物发现很重要,因此人们一直致力于开发测定膜蛋白结构的技术和方法。已经启动了几个结构基因组学项目,专注于膜蛋白的结构生物学研究。