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相关概念视频

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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相关实验视频

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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在不同的骨细胞中GPCRs的功能

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
概括

G蛋白结合受体 (GPCR) 是骨疾病的关键点. 这篇评论详细介绍了骨细胞中的GPCR,并提供了骨质疏松症和关节炎等骨疾病的新疗法.

关键词:
一个GPCR美国冠状细胞骨质细胞骨质细胞

更多相关视频

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

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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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相关实验视频

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

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科学领域:

  • 骨生物学和药理学
  • 细胞和分子医学

背景情况:

  • G蛋白结合受体 (GPCR) 在调节骨细胞功能和骨平衡方面发挥着至关重要的作用.
  • GPCR信号的失调与各种骨疾病有关,突出显示了它们的治疗潜力.

研究的目的:

  • 在不同类型的骨细胞中系统地审查和编目GPCR表达和功能.
  • 阐明GPCRs为骨健康协调细胞可塑性的分子机制.
  • 为推进骨相关疾病的GPCR向治疗提供框架.

主要方法:

  • 在介质干细胞,骨质细胞,骨细胞,巨细胞,骨质细胞和骨质细胞中的GPCR表达和功能作用的系统审查.
  • 包括cAMP/PKA,PLC-β/IP3和NF-κB在内的正规信号通路的整合.
  • 对GPCR参与骨平衡和疾病发病的分析.

主要成果:

  • 在不同的骨细胞系中编目了GPCR的特定数量及其功能 (例如,在MSC中12个,在骨质细胞/骨细胞中21个,在巨细胞/骨细胞中23个,在骨质细胞中31个).
  • 通过集成的信号轴,证明了GPCR如何动态调节细胞可塑性.
  • 鉴定出GPCRs是矩阵矿化,机械转导,炎症性骨质再吸收和内分泌骨化的关键调节剂.

结论:

  • GPCRs是骨平衡的中央调节剂,在骨细胞类型中具有不同的表达模式和功能.
  • 了解GPCR信号提供了开发骨疾病新疗法的基础.
  • 偏向性激应和全调节等精确策略为骨质疏松症,关节炎和再生医学的临床转化提供了有希望的途径.