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相关概念视频

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

16.5K
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...
16.5K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

4.0K
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,...
4.0K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

131.5K
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.
131.5K
GPCR Desensitization01:12

GPCR Desensitization

7.9K
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...
7.9K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

3.9K
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:
3.9K
The Two-State Receptor Model01:29

The Two-State Receptor Model

3.0K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
3.0K

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相关实验视频

Updated: Jan 15, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
14:28

Peptide-based Identification of Functional Motifs and their Binding Partners

Published on: June 30, 2013

12.9K

国家特定的体设计针对G蛋白结合受体.

Yang Xue1, Hong Wang2, Jun Li1

  • 1Baidu Inc. NLP, Shenzhen 518000, China.

Journal of chemical information and modeling
|October 11, 2025
PubMed
概括

我们为G蛋白结合受体 (GPCRs) 开发了一种州特定的酸设计管道. 这种方法有效地产生针对GPCRs的向抗体或抗体,改善药物发现.

更多相关视频

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
11:49

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

Published on: July 28, 2014

41.6K

相关实验视频

Last Updated: Jan 15, 2026

Peptide-based Identification of Functional Motifs and their Binding Partners
14:28

Peptide-based Identification of Functional Motifs and their Binding Partners

Published on: June 30, 2013

12.9K
Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
16:16

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
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Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay

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科学领域:

  • 药理学 药理学是指药理学的学科.
  • 结构生物学 结构生物学
  • 药物发现 药物发现 药物发现

背景情况:

  • G蛋白结合受体 (GPCRs) 是关键的药物点,参与许多生理过程.
  • 由于较高的亲和力,选择性和强度,对GPCR向小分子具有优势.
  • GPCR的构造状态 (活性/无活性) 决定了连接体相互作用,需要特定状态的设计策略.

研究的目的:

  • 为GPCRs开发一个高效的,国家特定的类设计管道.
  • 为了能够根据GPCR结构状态量身定制的激素或抗剂的设计.
  • 通过识别特定GPCR标的新来验证管道.

主要方法:

  • 为GPCRs开发了一个国家特定的类设计框架.
  • 利用GPCR活跃和非活跃的构造状态来定制的设计.
  • 采用针对GPCR-复合体优化的特定状态折叠模型来选择高潜力.

主要成果:

  • 成功设计并确定了阿佩林受体 (APJR) 和生长激素分泌受体 (GHSR) 的激素和抗剂.
  • 鉴定出一种具有竞争力的抑制剂对于类似葡萄糖-1受体 (GLP-1R).
  • 证明了州特定设计管道在产生功能性的有效性.

结论:

  • 开发的管道为针对GPCRs的州特定体设计提供了一个有效的策略.
  • 这种方法有助于发现具有提高特异性和功效的新型疗法.
  • 这些发现为各种GPCR开发基于的药物开发开辟了新的途径.