GPCR structure and function relationship: identification of a biased apelin receptor mutantapelin receptorG protein-coupled receptorsmolecular dynamicspharmacologysignaling biasBiased ligands of G protein-coupled receptors (GPCRs) may have improved therapeutic benefits and safety profiles. However, the ...
GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1-2 September 2014. Naunyn Schmiedebergs Arch Pharmacol. 2015; 388: 883-903.Heifetz A, Schertler GF, Seifert R, Tate CG, Sexton PM, Gurevich VV...
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Fig1. Structure of GPCR 图1.GPCR的结构[1] 1.2 GPCR的种类和功能 迄今已鉴定出900多个人类相关的GPCRs[2]。GPCRs的分类依据序列以及结构相似性,主要分为以下5个主要家族:视紫红质受体(A类),分泌素受体(B1类),黏附受体(B2类),谷氨酸盐受体(C类)和卷曲/味觉2(F类)[1]。
2021年11月17日,来自北卡罗来纳大学教堂山分校的Bryan L. Roth/ Jonathan F. Fay团队与加州大学旧金山分校的Brian K. Shoichet团队合作在Nature杂志发表题为“Structure, function and pharmacology of human itch GPCRs”的文章,通过冷冻电镜解析了与痒感知相关的GPCR孤儿受体MRGPRX2和MRGPRX4的三维结构,并通过...
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The GPCR Network: a large-scale collaboration to determine human GPCR structure and function. The GPCR Net- work: a large-scale collaboration to determine human GPCR structure and function. Nat Rev Drug Discov 2013;12:25-34... Stevens,Raymond,C.,... - 《Nature Reviews Drug Discovery》 被...
30-40% of marketed drugs, and their key roles in normal physiology and in disease demonstrate that an understanding of their structure and function is valuable to researchers in both basic science and drug discovery. However, until recently, detailed structural information on this protein family ...