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関連する概念動画

G-protein Coupled Receptors01:21

G-protein Coupled Receptors

91.4K
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.
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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

6.9K
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...
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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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Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
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Microbial Biosensors01:17

Microbial Biosensors

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Microbial biosensors are analytical devices that utilize living microbes to detect specific substances through measurable signals. These devices consist of two main components: biosensing organisms and signal-transducing elements. Biosensing organisms, such as Escherichia coli or Saccharomyces cerevisiae, are typically housed in multiwell plates connected to transducers, enabling rapid, real-time detection of target analytes.Signal Generation MechanismWhen a target analyte—such as...
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Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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汎用バイオセンサプラットフォームによる文脈依存のGPCR活動の直接尋問

Remi Janicot1, Marcin Maziarz1, Jong-Chan Park1

  • 1Department of Biochemistry & Cell Biology, Chobanian & Avedisian School of Medicine, Boston University, Boston, MA 02118, USA.

Cell
|February 27, 2024
PubMed
まとめ

研究者は,細胞内のGタンパク質結合受容体 (GPCR) の活性を測定するための新しいバイオセンサプラットフォームを開発しました. このツールは,GPCRのシグナル伝達に関する高精度な洞察を提供し,薬物の発見と細胞の反応を理解するのに役立ちます.

キーワード:
BRET についてGタンパク質GPCR についてGTPase について抗精神病薬偏ったシグナルバイオセンサ薬物の発見繊維症神経伝達物質

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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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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
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関連する実験動画

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Monitoring GPCR-&#946;-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
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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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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

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A "Dual-Addition" Calcium Fluorescence Assay for the High-Throughput Screening of Recombinant G Protein-Coupled Receptors
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科学分野:

  • 生物化学
  • 分子生物学
  • 薬理学について

背景:

  • Gタンパク質結合受容体 (GPCRs) は,主要な薬物標的である.
  • 現在のツールでは,生理学的な環境でGPCRを研究する精度が不足しています.
  • GPCRの行動を理解することは,新しい治療法の開発に不可欠です.

研究 の 目的:

  • GPCR活動を測定するためのスケーラブルなプラットフォームを作成します.
  • どのGPCRでもGタンパク質の活性化の高精度評価を可能にします.
  • 内生細胞と原始細胞のGPCRシグナル伝達を調査する.

主な方法:

  • コンパクトなONEベクターGタンパク質光学 (ONE-GO) バイオセンサコンストラクションの開発.
  • 主要な心血管細胞および神経細胞を含む多様な細胞タイプにおける多数のGPCRの特徴化.
  • GPCRを病気に関連した条件で研究するためのプラットフォームの適用

主要な成果:

  • GPCRのGタンパク質結合の選択性に関する洞察を明らかにした.
  • 自然なGPCR変異体に対する抗精神病薬の薬理学的なプロファイルが決定された.
  • 内生GPCRによって特定された細胞型特異的および疾患状態依存のGタンパク質サブタイプシグナルバイアス.

結論:

  • オープンソースのONE-GOプラットフォームは,文脈依存のGPCR活動を研究するための広範なアクセシビリティを提供します.
  • このツールは,健康と病気におけるGPCR機能のより深い理解を促進します.
  • 生理学的に重要なシステムにおけるGPCR信号の直接の尋問を可能にします.