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相关概念视频

GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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 cells.
Two...
Diversity in Cell Signaling Responses01:22

Diversity in Cell Signaling Responses

The physiological function of a cell and cellular communication are outcomes of a range of extrinsic signals, intracellular signaling pathways, and cellular responses. No two cell types express the same repertoire of signaling components. Receptors are highly selective for their cognate ligands, but once activated, they can alter multiple cellular processes such as DNA transcription, protein synthesis, and metabolic activity. 
Graded and Abrupt Responses
Some signaling systems generate...
GPCR Desensitization01:12

GPCR Desensitization

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...
Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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,...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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.

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相关实验视频

Updated: May 9, 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

在GPCR信号传输中的精度与灵活性.

Matthias Elgeti1, Alexander S Rose, Franz J Bartl

  • 1Institut für Medizinische Physik und Biophysik (CC2), Charité-Universitätsmedizin Berlin, Charitéplatz 1, 10117 Berlin, Germany. matthias.elgeti@charite.de

Journal of the American Chemical Society
|July 26, 2013
PubMed
概括
此摘要是机器生成的。

罗多普辛 (Rhodopsin) 是一种类动物.

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Parallel Interrogation of &#946;-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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相关实验视频

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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:

  • 像罗多素这样的G蛋白结合受体 (GPCR) 对于信号传导至关重要.
  • 罗多普辛的光激活状态能够在视网膜杆细胞中快速精确地传输信号.

研究的目的:

  • 研究罗多普辛的结构动态及其与转化素的相互作用.
  • 阐明从罗多素到转化素快速和高保真信号传输的机制.

主要方法:

  • 福里埃变换红外光谱法 (FTIR) 用于研究蛋白质的结构状态.
  • 全原子分子动力学 (MD) 模拟以在膜环境中建模罗多素.
  • 对合成Gtγ和Gtα亚单元C终端对罗多普辛构造的影响的分析.

主要成果:

  • FTIR揭示了保存的基因 (E(D) RY和Yx7K(R)) 调节罗多普辛的无活性和活性状态.
  • 模拟MD确定了一个内在的非结构化循环 (CL3) 和 conformational子状态.
  • 在保持CL3灵活性的同时,GγCT稳定了活性状态;GαCT稳定了螺旋式CL3基质.

结论:

  • 提出了一种快速,精确的罗多素/转素合机制,涉及逐步的形状空间缩小.
  • 保存的氨基酸残留在这个机制中起着关键作用.
  • 拟议的机制可能可以将其推广到其他GPCR/G蛋白相互作用中.