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相关概念视频

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

132.8K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
132.8K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

18.2K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
18.2K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

5.3K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
5.3K
Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

6.7K
Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
6.7K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

11.9K
Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
11.9K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

7.8K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
7.8K

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相关实验视频

Updated: Feb 26, 2026

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

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距离较远的结构区域之间的断决定了GPCR:G蛋白合中的选择性.

Elizaveta Mukhaleva1,2, Edgardo J Sánchez Rivas3, Sergio Branciamore1,2

  • 1Department of Computational and Quantitative Medicine, Beckman Research Institute of the City of Hope, Monrovia, California 91016, United States.

Biochemistry
|February 25, 2026
PubMed
概括
此摘要是机器生成的。

了解G蛋白合受体-G (GPCR-G) 蛋白合选择性是关键. 使用机器学习和模拟识别的Gα蛋白核心内的合作相互作用可以为特定的信号通路设计Gα蛋白.

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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

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相关实验视频

Last Updated: Feb 26, 2026

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
09:12

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

Published on: September 10, 2016

10.1K
Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

17.3K
A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

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科学领域:

  • 生物化学 生物化学
  • 分子生物学分子生物学
  • 计算生物学 计算生物学

背景情况:

  • G蛋白合受体-G (GPCR-G) 蛋白合选择性机制尚未完全理解.
  • 广泛的结构和功能研究尚未解决这些分子基础.

研究的目的:

  • 阐明控制GPCR-G蛋白合选择性的分子机制.
  • 为了确定影响这种选择性的Gα蛋白核心中的关键残留群体.

主要方法:

  • 可解释机器学习贝叶斯网络模型.
  • 分子动力学模拟. 分子动力学模拟.
  • 实验验证包括亚型交换突变.

主要成果:

  • 在Gα蛋白核心 (N端,h4s6环,H5螺旋) 中识别出不同的合作热点残留物.
  • 揭示了Gα核心和H5螺旋之间对选择性相互作用的全性依赖.
  • 证明了Gαs核心中的Gαq样突变会改变与Gαq.的受体合.

结论:

  • 在Gα核心内的合作相互作用对于GPCR-G蛋白合选择性至关重要.
  • 这些相互作用可以被设计成具有定制信号偏好的Gα蛋白.