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相关概念视频

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

118.4K
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.
118.4K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

1.9K
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,...
1.9K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

7.1K
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...
7.1K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

11.8K
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...
11.8K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

5.5K
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...
5.5K
GPCR Desensitization01:12

GPCR Desensitization

6.0K
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...
6.0K

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相关实验视频

Updated: Jun 26, 2025

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

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工程G蛋白合受体用于稳定.

João Paulo L Velloso1,2,3, Alex G C de Sá1,2,3, Douglas E V Pires4

  • 1School of Chemistry and Molecular Biosciences, The Australian Centre for Ecogenomics, The University of Queensland, Brisbane, Queensland, Australia.

Protein science : a publication of the Protein Society
|May 15, 2024
PubMed
概括

GPCR-tm是一种新的机器学习工具,可以预测突变如何影响G蛋白结合受体 (GPCR) 稳定性. 这种计算方法有助于稳定GPCRs,用于药物发现和结构研究.

关键词:
与G蛋白结合的受体.机器学习 (ML) 是指机器学习.蛋白质工程工程 蛋白质工程稳定性 预测 预测结构性特征的结构性特征.

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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

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

  • 生物化学和结构生物学.
  • 计算生物学和生物信息学
  • 药物发现和药理学.

背景情况:

  • G蛋白结合受体 (GPCR) 是关键的药物标,但它们固有的不稳定性阻碍了研究.
  • 传统的蛋白质工程用于GPCR稳定是耗时且具有计算挑战性的.
  • 现有的可溶性蛋白的计算方法不适合GPCRs.

研究的目的:

  • 开发一种新的,个性化的,结构驱动的计算工具,用于预测突变对GPCR稳定性的影响.
  • 提供基于机器学习的解决方案,以克服用于结构表征和药物查的GPCR工程的局限性.

主要方法:

  • 开发GPCR-tm,这是一个基于Web的机器学习工具,利用结构驱动的功能.
  • 应用基于图形的签名来表示突变环境.
  • 验证使用十倍交叉验证和盲目测试套件.

主要成果:

  • GPCR-tm表现出与现有方法相匹配或优于现有方法的性能.
  • 达到了0.74的皮尔森相关系数 (交叉验证) 和0.46 (盲测).
  • 识别了基于结构图的结构特征,作为对稳定性突变影响的关键预测因素.

结论:

  • GPCR-tm根据它们对蛋白质稳定性的影响精确地排列突变,从而促进了合理的稳定策略.
  • 该工具有助于克服GPCR结构研究和药物发现方面的挑战.
  • 为了更广泛的科学用途,GPCR-tm可以通过用户友好的Web服务器访问.