Lundstrom Kenneth
BioXtal, Chemin des Croisettes 22, CH-1066 Epalinges, Switzerland.
Curr Opin Drug Discov Devel. 2004 May;7(3):342-6.
Of the 25,000 crystal structure entries deposited in public databases less than 1% are for membrane proteins; this gives a clear indication of the difficulties relating to structural biology and determination of this type of protein. To date, structural genomics networks have mainly focused on soluble proteins, despite the fact that membrane proteins constitute 60 to 70% of current drug targets. Technological improvement on a broad basis is the key to higher success rates, but this is generally not possible unless large functional networks are established. Several structural genomics initiatives, concentrating partly or fully on membrane proteins, have been established during the last few years and the Membrane Protein Network (MePNet; BioXtal, Switzerland) focuses specifically on the pharmaceutically attractive G protein-coupled receptors (GPCRs). Within MePNet, over 100 full-length GPCRs have been subjected to overexpression in bacterial, yeast and mammalian cells, followed by purification and crystallization studies.
在公共数据库中存储的25000个晶体结构条目中，膜蛋白的条目不到1%；这清楚地表明了与这类蛋白质的结构生物学和测定相关的困难。迄今为止，结构基因组学网络主要集中于可溶性蛋白质，尽管事实上膜蛋白构成了当前药物靶点的60%至70%。广泛的技术改进是提高成功率的关键，但除非建立大型功能网络，否则这通常是不可能的。在过去几年中，已经建立了几个部分或完全专注于膜蛋白的结构基因组学计划，而膜蛋白网络（MePNet；瑞士BioXtal公司）则特别关注具有药物吸引力的G蛋白偶联受体（GPCR）。在MePNet内部，已有100多种全长GPCR在细菌、酵母和哺乳动物细胞中进行了过表达，随后进行了纯化和结晶研究。
