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関連する概念動画

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.
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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...
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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 affinity and are together...
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...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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関連する実験動画

Updated: May 11, 2026

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

リストラクチャリングGタンパク質結合受容体活性化

Martin Audet1, Michel Bouvier

  • 1Department of Biochemistry, Institute for Research in Immunology and Cancer, Université de Montréal, QC, Canada.

Cell
|October 2, 2012
PubMed
まとめ

Gタンパク質結合受容体 (GPCR) は,細胞シグナル伝達に不可欠です. 最近の構造的な洞察は,新しいリガンド結合と活性化メカニズムを明らかにし,GPCRの研究を進めています.

科学分野:

  • バイオケミストリー バイオケミストリー
  • 分子生物学は分子生物学である.
  • 薬理学 薬理学とは

背景:

  • Gタンパク質結合受容体 (GPCRs) は,信号伝導を媒介する細胞表面の重要なタンパク質である.
  • GPCRの構造的特徴づけは歴史的に困難であり,詳細な機能的研究を制限していました.
  • ロドプシン構造は初期の洞察を提供したが,より広範なGPCR固有の情報が欠けていた.

研究 の 目的:

  • GPCRの構造生物学における最近の進歩をレビューする.
  • 新しい構造がGPCR機能の理解をどのように促すかを強調する.
  • GPCRにおける将来の研究方向への影響を議論する.

主な方法:

  • 最近決定されたGタンパク質結合受容体構造の分析.
  • 新しい構造データと以前のロドプシンベースのモデルの比較.
  • GPCRシグナル伝達に関する既存の知識と構造的発見の統合.

主要な成果:

  • 新しいGPCR構造は,ロドプシンモデルのいくつかの予測を確認しています.
  • 予期せぬリガンド結合モードと活性化メカニズムが明らかになった.
  • 構造データは,GPCR二分化やバイアスシグナル伝達などの新興概念をサポートしています.

さらに関連する動画

Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
10:59

Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET

Published on: August 17, 2022

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
09:21

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

Published on: November 7, 2025

関連する実験動画

Last Updated: May 11, 2026

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

Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET
10:59

Visualizing the Conformational Dynamics of Membrane Receptors Using Single-Molecule FRET

Published on: August 17, 2022

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
09:21

BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells

Published on: November 7, 2025

結論:

  • 最近のGPCR構造の急増は,その機能の理解を大幅に高めています.
  • これらの洞察は,ターゲットを絞った治療法の開発に不可欠です.
  • 将来の研究では,二分化やバイアスアゴニズムなどの複雑なGPCR行動を探求する.