Related Experiment Video
Updated: Jul 16, 2026
10:13
Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
G-protein-coupled receptor signalling through protein networks
1Department of Infectology, The Scripps Research Institute, Jupiter, FL 33458, USA. strosber@scripps.edu
Biochemical Society Transactions
|January 11, 2007
Summary
This review covers G-protein-coupled receptors (GPCRs), crucial drug targets, detailing their structure, function, and protein interactions. It highlights research on beta-adrenoceptors, muscarinic acetylcholine, melatonin, and angiotensin receptors.
Area of Science:
- Pharmacology and Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- G-protein-coupled receptors (GPCRs) represent a vast superfamily of cell surface receptors.
- They are implicated in numerous physiological processes and are primary targets for a significant portion of marketed drugs.
- Understanding GPCR structure and function is critical for developing new therapeutics.
Purpose of the Study:
- To provide a comprehensive overview of GPCRs, including their structure, function, and interactions with associated proteins.
- To highlight key research findings in the field of GPCRs over the last 30 years.
- To exemplify GPCR research using specific examples such as beta-adrenoceptors, muscarinic acetylcholine, melatonin, and angiotensin receptors.
Main Methods:
- Review of scientific literature and research findings.
- Synthesis of data on GPCR structure and function.
- Case studies focusing on specific receptor families.
Main Results:
- Detailed discussion of GPCR structural motifs and functional mechanisms.
- Elucidation of the diverse roles of GPCRs in cellular signaling.
- Examples illustrating the complexity of GPCR interactions with signaling partners.
Conclusions:
- GPCRs are fundamental to cellular communication and disease pathways.
- Continued research into GPCRs offers significant potential for novel drug development.
- The presented examples underscore the therapeutic importance and research diversity within the GPCR field.
More Related Videos
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
08:16Detection of G Protein-coupled Receptor Expression in Mouse Vagal Afferent Neurons using Multiplex In Situ Hybridization
Published on: September 20, 2021
Related Concept Videos
01:21G-protein Coupled Receptors
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.
01:21G-protein Coupled Receptors
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.
01:30Assembly of Signaling Complexes
Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
01:15G Protein-coupled Receptors
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...
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...
01:15G Protein-coupled Receptors
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...
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...
01:30Transducer Mechanism: G Protein–Coupled Receptors
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, 7TM, or...
GPCRs are also called heptahelical, 7TM, or...