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Related Concept Videos

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.
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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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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...
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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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Updated: Oct 20, 2025

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors.

Stephen Ph Alexander1, Arthur Christopoulos2, Anthony P Davenport3

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

British Journal of Pharmacology
|September 16, 2021
PubMed
Summary

The Concise Guide to Pharmacology 2021/22 offers a comprehensive overview of nearly 1900 human drug targets, emphasizing selective pharmacology. This biennial publication provides a citable record of drug target properties and ligands.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • The Concise Guide to Pharmacology is a biennial publication series.
  • It serves as a reference for human drug targets and their properties.

Purpose of the Study:

  • To provide a concise overview of key properties for approximately 1900 human drug targets.
  • To emphasize selective pharmacology and link to a detailed online knowledgebase.
  • To offer a permanent, citable record of pharmacological information.

Main Methods:

  • Compilation of data on drug targets, including G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes, and transporters.
  • Presentation of information in a tabular format with nomenclature guidance.
  • Inclusion of information on pharmacological tools, references, and further reading suggestions.

Main Results:

  • Overview of nearly 1900 human drug targets with a focus on selective pharmacology.
  • Detailed information on target and ligand properties available via www.guidetopharmacology.org.
  • The guide is divided into six major pharmacological target classes.

Conclusions:

  • The Concise Guide to Pharmacology 2021/22 provides an updated, citable snapshot of drug target information.
  • It facilitates comparison of related targets and supersedes previous editions.
  • Official IUPHAR classification and nomenclature are provided for human drug targets.