STRUCTURAL STUDIES OF RHODOPSIN

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 我们正在进行一系列生物学上重要的视紫红质形式的结构表征，视紫红质是视网膜中发现的光敏膜蛋白，以及相关蛋白。视紫红质是第一个可以获得晶体结构信息的G蛋白偶联受体。它仍然是一个典型的GPCR。这使得它引起了相当大的兴趣，因为GPCRs是许多商业上重要药物的主要目标。我们正在结晶视紫红质和视紫红质/转导蛋白复合体，以获得激活的GPCR及其与其同源G蛋白的复合体的结构。通过观察与信号转导相关的结构变化，我们将确定三维分子结构中对该GPCRs和其他GPCRs的生物活性至关重要的区域。这些地区将成为其他生化研究和药物开发活动的重点。

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. We are carrying out a series of structural characterizations of biologically important forms of rhodopsin, the light-sensing membrane protein found in retina, and related proteins. Rhodopsin was the first G protein-coupled receptor for which crystallographic structural information became available. It remains a prototypical GPCR. This makes it of considerable interest because GPCRs are the major target of many commercially important drugs. We are crystallizing rhodopsin and rhodopsin/transducin complexes to obtain the structure of an activated GPCR and its complex with its cognate G protein. By observing the structural changes associated with signal transduction, we will identify regions in the three-dimensional molecular structure that are crucial for the biological activity of this and other GPCRs. Those regions will become the focus of other biochemical studies and drug-development activities.