Department of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.
Paul Scherrer Institute, Villigen, Switzerland.
Nat Methods. 2019 Feb;16(2):151-162. doi: 10.1038/s41592-018-0302-x. Epub 2019 Jan 21.
G-protein-coupled receptors (GPCRs) transduce physiological and sensory stimuli into appropriate cellular responses and mediate the actions of one-third of drugs. GPCR structural studies have revealed the general bases of receptor activation, signaling, drug action and allosteric modulation, but so far cover only 13% of nonolfactory receptors. We broadly surveyed the receptor modifications/engineering and methods used to produce all available GPCR crystal and cryo-electron microscopy (cryo-EM) structures, and present an interactive resource integrated in GPCRdb ( http://www.gpcrdb.org ) to assist users in designing constructs and browsing appropriate experimental conditions for structure studies.
G 蛋白偶联受体（GPCRs）将生理和感官刺激转导为适当的细胞反应，并介导三分之一药物的作用。GPCR 结构研究揭示了受体激活、信号转导、药物作用和变构调节的一般基础，但迄今为止仅涵盖 13%的非嗅觉受体。我们广泛调查了受体的修饰/工程以及用于产生所有可用 GPCR 晶体和冷冻电镜（cryo-EM）结构的方法，并提供了一个集成在 GPCRdb（http://www.gpcrdb.org）中的交互式资源，以帮助用户设计构建体并浏览适合结构研究的实验条件。
