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相关概念视频

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

20.2K
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...
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GPCR Desensitization01:12

GPCR Desensitization

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G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

8.4K
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...
8.4K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

134.9K
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.
134.9K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

9.0K
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,...
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相关实验视频

Updated: Apr 19, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

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快照:GPCR-利干相互作用

Eshan Ghosh1, Kumari Nidhi1, Arun K Shukla1

  • 1Department of Biological Sciences and Bioengineering, Indian Institute of Technology Kanpur, 208016, India.

Cell
|December 20, 2014
PubMed
概括
此摘要是机器生成的。

G-蛋白合受体 (GPCRs) 对于细胞信号传递至关重要. 确定的晶体结构揭示了它们的非活性和活性状态,详细说明了连接体相互作用和整体组织.

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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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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
  • 结构生物学 结构生物学

背景情况:

  • G-蛋白结合受体 (GPCR) 是重要的细胞表面蛋白质,它们调解细胞对外部刺激的反应.
  • GPCRs通过在血中传输信号来起作用,在许多生理过程中发挥关键作用.

研究的目的:

  • 阐明GPCR激活和带结合的结构基础.
  • 为GPCRs和各种连接体之间的相互作用提供原子层面的见解.

主要方法:

  • 使用X射线结晶学来确定GPCRs的结构.
  • 受体结构在非活性和活性构造中得到解决.
  • 进行了化学和功能上不同的联结体复合物的分析.

主要成果:

  • 获得了多个GPCR的高分辨率晶体结构.
  • 结构捕获受体在不同的无活性和活性构造状态.
  • 视觉化了连接体和受体之间的详细原子相互作用.

结论:

  • 晶体结构提供了GPCR整体组织的全面视图.
  • 这些结构为联体受体结合机制提供了前所未有的原子细节.
  • 了解GPCR结构是解读细胞信号通路的关键.