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関連する概念動画

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

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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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Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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スナップショット:GPCR-リガンド相互作用

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
まとめ
この要約は機械生成です。

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. 決定された結晶構造は,その不活性状態と活性状態を明らかにし,リガンドの相互作用と全体的な組織を詳細に説明します.

さらに関連する動画

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

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関連する実験動画

Last Updated: Apr 19, 2026

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
08:21

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

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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.
  • 構造生物学 構造生物学とは

背景:

  • Gタンパク質結合受容体 (GPCR) は,外部刺激に対する細胞反応を媒介する細胞表面の重要なタンパク質です.
  • GPCRは,プラズマ膜に信号を伝達することで機能し,多くの生理学的プロセスにおいて重要な役割を果たします.

研究 の 目的:

  • GPCRの活性化とリガンド結合の構造的基礎を解明する.
  • GPCRsと様々なリガンドの相互作用に関する原子レベルの洞察を提供するために.

主な方法:

  • X線結晶学を用いてGPCRの構造を決定した.
  • 受容体の構造は,不活性と活性の両方の形状で解消されました.
  • 化学的および機能的に異なるリガンドを持つ複合体の分析が行われました.

主要な成果:

  • 複数のGPCRの高解像度の結晶構造が得られた.
  • 構造は,受容体を異なる不活性および活性構成状態で捕捉した.
  • リガンドと受容体の間の詳細な原子相互作用が視覚化されました.

結論:

  • 結晶構造は,GPCR全体の組織について包括的な見解を提供します.
  • これらの構造は,リガンド受容体結合機構に関する前例のない原子詳細を提供します.
  • GPCRの構造を理解することは,細胞の信号伝達経路を解読する鍵です.