The GPCR Crystallography Boom: Providing an Invaluable Source of Structural Information and Expanding the Scope of Homology Modeling
The GPCR Crystallography Boom: Providing an Invaluable Source of Structural Information and Expanding the Scope of Homology Modeling
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DOI：
10.1007/978-94-007-7423-0_1
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发表时间：
2014-01-01
期刊：
影响因子：
--
通讯作者：
Wang, Keyun
中科院分区：
文献类型：
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作者：
Costanzi, Stefano;Wang, Keyun
G蛋白偶联受体(GPCRs)是一类具有很高药用价值的完整膜蛋白。直到最近，它们的结构一直特别难以捉摸，多年来，视紫红质一直是超家族中唯一具有实验阐明结构的成员。然而，最近的一些技术和科学进步使确定GPCR结构变得更加可行，从而导致了几种受体的结构的解决。除了提供直接的结构信息外，这些实验性的GPCR结构还为构建GPCR模型提供了模板。已经进行了深入的研究，以探索这些模型的准确性，特别是关于与其配体的相互作用，并评估它们的适用性，以合理发现GPCR调节子。鉴于目前的技术水平和该领域的发展速度，GPCR结构研究的未来很可能是一个由越来越多的实验和理论结构组成的景观。
G protein-coupled receptors (GPCRs) are integral membrane proteins of high pharmaceutical interest. Until relatively recently, their structures have been particularly elusive, and rhodopsin has been for many years the only member of the superfamily with experimentally elucidated structures. However, a number of recent technical and scientific advancements made the determination of GPCR structures more feasible, thus leading to the solution of the structures of several receptors. Besides providing direct structural information, these experimental GPCR structures also provide templates for the construction of GPCR models. In depth studies have been performed to probe the accuracy of these models, in particular with respect to the interactions with their ligands, and to assess their applicability the rational discovery of GPCR modulators. Given the current state of the art and the pace of the field, the future of GPCR structural studies is likely to be characterized by a landscape populated by an increasingly higher number of experimental and theoretical structures.