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相关概念视频

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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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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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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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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.
119.3K
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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G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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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...
4.6K
Pharmacodynamics: Overview and Principles01:21

Pharmacodynamics: Overview and Principles

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Pharmacodynamics is a scientific field that delves into drugs' intricate biochemical, cellular, and physiological effects on the human body. The study of pharmacodynamics helps us understand how drugs interact with the body and elicit various responses.
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or...
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相关实验视频

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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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简要的药理学指南2023/24:G蛋白结合受体

Stephen P H Alexander1, Arthur Christopoulos2, Anthony P Davenport3

  • 1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

British journal of pharmacology
|December 20, 2023
PubMed
概括

药理学简要指南2023/24提供药物点及其相互作用的表格概述. 这两年一次的出版物提供了可引用的药理学数据记录,包括G蛋白结合受体和其他关键标.

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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 Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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科学领域:

  • 药理学 药理学是指药理学的学科.
  • 药物发现 药物发现 药物发现
  • 生物化学 生物化学

背景情况:

  • 药理学简要指南是一系列两年一次的出版物.
  • 它总结了药物点及其相互作用的关键特性.
  • 2023/24年版是本系列的第六个.

研究的目的:

  • 为大约1800个药物标和6000个相互作用提供简洁,表格式的概述.
  • 提供药理学数据的永久,可引用,及时记录.
  • 链接到开放式知识库以获取更详细的信息.

主要方法:

  • 在表格格式中编译和总结数据.
  • 包括可用的选择性药理学数据.
  • 目标的组织分为六大类:G蛋白结合受体,离子通道,核激素受体,催化受体,酶和输送器.

主要成果:

  • 介绍了约1800种药物标和约6000种连接体相互作用的信息.
  • 强调选择性药理学,并提供链接到药理学指南知识库.
  • 包括命名指南,关于药理工具的摘要信息,关键参考文献和进一步阅读建议.

结论:

  • 药理学简要指南2023/24为研究人员提供了宝贵的,最新的资源.
  • 它为人类药物标提供了IUPHAR官方的分类和命名法.
  • 该出版物取代了以前的版本,并为药理学数据提供了一个稳定的参考点.