McCusker Emily C, Bane Steven E, O'Malley Michelle A, Robinson Anne Skaja
Department of Chemistry and Biochemistry, University of Delaware, Newark, Delaware 19711, USA.
Biotechnol Prog. 2007 May-Jun;23(3):540-7. doi: 10.1021/bp060349b. Epub 2007 Mar 31.
G protein-coupled receptors (GPCRs) are an important, medically relevant class of integral membrane proteins. Laboratories throughout all disciplines of science devote time and energy into developing practical methods for the discovery, isolation, and characterization of these proteins. Since the crystal structure of rhodopsin was solved 6 years ago, the race to determine high-resolution structures of more GPCRs has gained momentum. Since certain GPCRs are currently produced at sufficient levels for X-ray crystallography trials, it is speculated that heterologous expression of GPCRs may no longer be a bottleneck in obtaining crystal structures. This Review focuses on the current approaches in heterologous expression of GPCRs and explores the problems associated with obtaining crystal structures from GPCRs expressed in different systems. Although milligram amounts of certain GPCRs are attainable, the majority of GPCRs are still either produced at very low levels or not at all. Developing reliable expression techniques for GPCRs is still a major priority for the structural characterization of GPCRs.
G蛋白偶联受体（GPCRs）是一类重要的、与医学相关的整合膜蛋白。各个科学学科的实验室都投入时间和精力来开发用于发现、分离和表征这些蛋白质的实用方法。自6年前视紫红质的晶体结构被解析以来，确定更多GPCRs高分辨率结构的竞赛愈演愈烈。由于目前某些GPCRs的产量足以进行X射线晶体学试验，据推测，GPCRs的异源表达可能不再是获得晶体结构的瓶颈。本综述重点关注GPCRs异源表达的当前方法，并探讨从不同系统中表达的GPCRs获得晶体结构所涉及的问题。尽管可以获得毫克量的某些GPCRs，但大多数GPCRs的产量仍然很低或根本不产生。开发可靠的GPCRs表达技术仍然是GPCRs结构表征的首要任务。
