G protein-coupled receptors (GPCRs), also known as seven- (pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular res...

2023年8月31日 · G-protein coupled receptors are involved in responses of cells to many different kinds of signals, from epinephrine, to odors, to light. In fact, a variety of physiological phenomena including vision, taste, smell and the fight-or-flight response are mediated by GPCRs. What are G-protein coupled receptors?

G蛋白耦联受体（GPCRs）全部位于细胞膜上并且参与大部分生理功能的调节。 相较于其它药物靶来说，它们较易驾驭，因此市面上约35%的药物都以G蛋白耦联受体作为靶。 本文中将会介绍最重要的三种。 首先我们要明白到底什么是“G蛋白耦联受体”。 从名字来看，它是一个受体。 更确切来说，它是一个“和G蛋白连接才能工作的受体”。 大部分G蛋白耦联受体包含一条由约300至400个氨基酸组成的多肽链，少数G蛋白耦联受体的多肽链长度多达1100个单位的氨基酸。 G蛋白耦联 …

2024年4月10日 · In this study, we first review the structural advancements, activation mechanisms, and functional diversity of GPCRs. We then focus on GPCR drug discovery by revealing the detailed drug-target...

2018年1月8日 · G-protein-coupled receptors (GPCRs) relay numerous extracellular signals by triggering intracellular signaling through coupling with G proteins and arrestins. Recent...

G Protein Coupled Receptors (GPCRs) perceive many extracellular signals and transduce them to heterotrimeric G proteins, which further transduce these signals intracellular to appropriate downstream effectors and thereby play an important role in various signaling pathways.

2004年2月3日 · The basic G protein cycle consists of a G protein-coupled receptor (GPCR) activating the G protein by promoting the exchange of guanosine triphosphate (GTP) for guanosine diphosphate (GDP), which allows the α and βγ subunits to separate and activate downstream targets.

GPCRs consist of a single polypeptide that is folded into a globular shape and embedded in a cell's plasma membrane. Seven segments of this molecule span the entire width of the membrane —...

2019年5月16日 · A time-resolved look at how a GPCR engages a G protein reveals intermediates in the process that dictate both specificity for the interaction and the initial steps kicking off downstream signaling.

2024年4月1日 · G-Protein Activation/Deactivation Cycle: G-proteins, consisting of Gα, Gβ, and Gγ subunits, are inactive when bound to GDP and active when bound to GTP. Upon receptor activation, the GPCR facilitates the exchange of GDP for GTP on the Gα subunit.