STRUCTURAL STUDIES OF RHODOPSIN

这个子项目是许多研究子项目中的一个 由NIH/NCRR资助的中心赠款提供的资源。子项目和 研究者（PI）可能从另一个NIH来源获得了主要资金， 因此可以在其他CRISP条目中表示。列出的机构是 中心，不一定是研究者的机构。 我们正在进行一系列的生物学上重要形式的视紫红质的结构表征，视紫红质是视网膜中发现的感光膜蛋白，以及相关蛋白质。 视紫红质是第一个G蛋白偶联受体的晶体结构信息成为可用。 它仍然是一种典型的气相化学还原法。 这使得它相当感兴趣，因为GPCR是许多商业上重要的药物的主要靶标。 我们正在结晶视紫红质和视紫红质/转导素复合物，以获得激活的GPCR及其与同源G蛋白的复合物的结构。 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这种和其他GPCR的生物活性至关重要的区域。 这些区域将成为其他生物化学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.