视紫红质的晶体学模型及其在其他G蛋白偶联受体研究中的应用。

Slawomir Filipek, David C Teller, Krzysztof Palczewski, Ronald Stenkamp
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引用次数: 129

摘要

G蛋白偶联受体(gpcr)是一种完整的膜蛋白,可响应环境信号并启动激活细胞过程的信号转导途径。视紫红质是在视网膜的杆状细胞中发现的一种GPCR,在那里它起着光色素的作用。它的分子结构是通过低温电子显微镜和x射线晶体学研究知道的,这重塑了视觉科学中许多重要的结构/功能问题。此外,这第一个GPCR结构为其他GPCR的研究提供了一个结构模板,包括许多已知的药物靶点。在介绍了视紫质的主要结构元素的概述之后,将总结最近的文献,包括在分析其他gpcr中使用视紫质结构。利用视紫红质结构模型来了解其他gpcr的结构和功能,为验证结构模型提供了强有力的证据。
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The crystallographic model of rhodopsin and its use in studies of other G protein-coupled receptors.

G protein-coupled receptors (GPCRs) are integral membrane proteins that respond to environmental signals and initiate signal transduction pathways activating cellular processes. Rhodopsin is a GPCR found in rod cells in retina where it functions as a photopigment. Its molecular structure is known from cryo-electron microscopic and X-ray crystallographic studies, and this has reshaped many structure/function questions important in vision science. In addition, this first GPCR structure has provided a structural template for studies of other GPCRs, including many known drug targets. After presenting an overview of the major structural elements of rhodopsin, recent literature covering the use of the rhodopsin structure in analyzing other GPCRs will be summarized. Use of the rhodopsin structural model to understand the structure and function of other GPCRs provides strong evidence validating the structural model.

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