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関連する概念動画

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

13.3K
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...
13.3K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

2.4K
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,...
2.4K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

5.9K
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...
5.9K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

7.6K
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...
7.6K
G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

4.8K
GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
4.8K
Osteoclasts in Bone Remodeling01:31

Osteoclasts in Bone Remodeling

3.2K
Osteoclasts are cells responsible for bone resorption and remodeling. They originate from hematopoietic progenitor cells present in the bone marrow. Numerous progenitor cells fuse to form multinucleated cells, each with 10-20 nuclei. A single osteoclast has a diameter of 150 to 200 µM. These cells have ruffled borders that break down the underlying bone tissue and release minerals such as calcium into the blood in bone resorption. Osteoclasts cling to bones with their ruffled edges during...
3.2K

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関連する実験動画

Updated: Sep 10, 2025

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

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異なる骨細胞におけるGPCRの機能

Yan Zhang1,2, Nai-Ning Wang1,3, Zi-Han Qiu1

  • 1Key Laboratory of Biomedical Information Engineering of Ministry of Education, Key Laboratory of Biology Multiomics and Diseases in Shaanxi Province Higher Education Institutions, and Biomedical Informatics & Genomics Center, School of Life Science and Technology, Xi'an Jiaotong University, Xi'an, Shaanxi, 710049, China.

International journal of biological sciences
|August 27, 2025
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 (GPCRs) は,骨疾患の主要な標的である. このレビューは骨細胞のGPCRを詳細に説明し,骨粗鬆症や関節炎などの骨格疾患に対する新しい治療法についての洞察を提供します.

キーワード:
GPCR についてMSC についてコンドロサイトオステオブラストオステオクラスト

さらに関連する動画

Isolation, Purification, and Differentiation of Osteoclast Precursors from Rat Bone Marrow
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Isolation, Purification, and Differentiation of Osteoclast Precursors from Rat Bone Marrow

Published on: May 19, 2019

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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

Published on: June 9, 2017

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関連する実験動画

Last Updated: Sep 10, 2025

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

9.0K
Isolation, Purification, and Differentiation of Osteoclast Precursors from Rat Bone Marrow
11:11

Isolation, Purification, and Differentiation of Osteoclast Precursors from Rat Bone Marrow

Published on: May 19, 2019

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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

Published on: June 9, 2017

16.5K

科学分野:

  • 骨格生物学と薬理学
  • 細胞 及び 分子 医学

背景:

  • Gタンパク質結合受容体 (GPCRs) は,骨細胞機能と骨格の恒常性を調節する上で重要な役割を果たします.
  • GPCRのシグナル伝達が調節不良であることは,様々な骨疾患に関連しており,その治療的可能性を強調しています.

研究 の 目的:

  • 様々な骨細胞のGPCR発現と機能を体系的に検討し,分類する.
  • GPCR が骨格の健康のために細胞の可塑性を調整する分子メカニズムを解明する.
  • 骨関連疾患に対するGPCR標的治療の進歩のための枠組みを提供すること.

主な方法:

  • GPCR発現とメゼンキマ幹細胞,骨質芽細胞,骨細胞,マクロファージ,骨質芽細胞,軟骨細胞における機能的役割の体系的なレビュー.
  • cAMP/PKA,PLC-β/IP3およびNF-κBを含む正規の信号伝達経路の統合
  • 骨格のホメオスタシスと病原性におけるGPCRの関与の分析

主要な成果:

  • 異なる骨細胞系におけるGPCRおよびその機能の特定数 (例えば,MSCでは12,骨質細胞/骨細胞では21,マクロファージ/骨質細胞では23,コンドロ細胞では31)
  • GPCRが統合されたシグナリング軸を通して細胞の可塑性を動的に調節する方法を実証した.
  • GPCRは,マトリックス鉱化,機械伝導,炎症性骨再吸収,内分泌骨格化の重要な調節因子として特定された.

結論:

  • GPCRは骨格の恒常性の中央調節体であり,骨細胞の種類によって異なる発現パターンと機能を有する.
  • GPCRシグナル伝達を理解することは,骨疾患の新たな治療戦略の開発のための基盤を提供します.
  • バイアスアゴニズムやアロステリック調節などの精度戦略は,骨粗鬆症,関節炎,再生医療における臨床翻訳のための有望な経路を提供します.