Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

12.1K
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...
12.1K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

2.0K
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,...
2.0K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

119.3K
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

6.0K
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...
6.0K
G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

4.6K
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

1.2K
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...
1.2K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Zonated mechanosensing by PIEZO1 controls liver regeneration.

Science (New York, N.Y.)·2026
Same author

Neurotensin receptor 2 agonism attenuates adverse cardiac remodeling in preclinical models.

Science translational medicine·2026
Same author

Endothelial soluble APP/APLP2 promote heart repair through KIT-mediated angiogenesis.

Science advances·2026
Same author

Activation of TREK-1 and TREK-2 Two-Pore Domain Potassium Channels by the K<sub>v</sub>4 Channel Modulator, NS5806.

Pharmacology research & perspectives·2026
Same author

Methodological guidelines for P2X receptor assays and data interpretation.

Cell death & disease·2026
Same author

Ginger Bioactives as Multi-Target Therapeutics: Mechanisms, Delivery Innovation, and Human Health Impact.

Nutrients·2026
Same journal

Tangeretin ameliorates sepsis-induced neurocognitive impairment in adult male mice by suppressing Akt-driven glycolytic reprogramming and neuroinflammation.

British journal of pharmacology·2026
Same journal

The discovery and development of ensifentrine: A novel inhaled dual PDE3/4 inhibitor having 'bifunctional' bronchodilator and anti-inflammatory activity.

British journal of pharmacology·2026
Same journal

Glucagon-like peptide-1 improves vascular endothelial dysfunction in hypertensive mice via CREB-driven transcriptional regulation of long non-coding RNA 155383.

British journal of pharmacology·2026
Same journal

The chemokine receptor-like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling.

British journal of pharmacology·2026
Same journal

Peripheral targets for neuropathic pain.

British journal of pharmacology·2026
Same journal

Therapeutic potential of liver X receptor agonist GW3965 in preserving myelin integrity following traumatic brain injury.

British journal of pharmacology·2026
See all related articles

Related Experiment Video

Updated: Jul 7, 2025

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

16.4K

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors.

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
Summary
This summary is machine-generated.

The Concise Guide to Pharmacology 2023/24 offers a tabular overview of drug targets and their interactions. This biennial publication provides a citable record of pharmacology data, including G protein-coupled receptors and other key targets.

More Related Videos

Parallel Interrogation of &#946;-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
09:03

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Published on: March 10, 2020

12.3K
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

8.9K

Related Experiment Videos

Last Updated: Jul 7, 2025

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

16.4K
Parallel Interrogation of &#946;-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
09:03

Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay

Published on: March 10, 2020

12.3K
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

8.9K

Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biochemistry

Background:

  • The Concise Guide to Pharmacology is a biennial publication series.
  • It summarizes key properties of drug targets and their interactions.
  • The 2023/24 edition is the sixth in this series.

Purpose of the Study:

  • To provide a concise, tabular overview of approximately 1800 drug targets and 6000 interactions.
  • To offer a permanent, citable, point-in-time record of pharmacological data.
  • To link to an open-access knowledgebase for more detailed information.

Main Methods:

  • Data compilation and summarization in a tabular format.
  • Inclusion of selective pharmacology data where available.
  • Organization of targets into six major categories: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes, and transporters.

Main Results:

  • Presents information on ~1800 drug targets and ~6000 ligand interactions.
  • Emphasizes selective pharmacology and provides links to the Guide to Pharmacology knowledgebase.
  • Includes nomenclature guidance, summary information on pharmacological tools, key references, and further reading suggestions.

Conclusions:

  • The Concise Guide to Pharmacology 2023/24 serves as a valuable, up-to-date resource for researchers.
  • It provides official IUPHAR classification and nomenclature for human drug targets.
  • The publication supersedes previous editions and offers a stable reference point for pharmacological data.