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Updated: May 28, 2026
10:13
Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
Diversity and modularity of G protein-coupled receptor structures
Vsevolod Katritch1, Vadim Cherezov, Raymond C Stevens
1Department of Molecular Biology, The Scripps Research Institute, La Jolla, CA 92037, USA.
Trends in Pharmacological Sciences
|October 29, 2011
Summary
G protein-coupled receptors (GPCRs) are key cell membrane proteins. Their diverse structures, revealed by recent crystal data, offer new insights into drug discovery and signaling mechanisms.
Area of Science:
- Biochemistry
- Structural Biology
- Pharmacology
Background:
- G protein-coupled receptors (GPCRs) are the largest family of cell membrane proteins.
- They share a common signal transduction mechanism but exhibit significant diversity in ligand binding and function.
Purpose of the Study:
- To review common structural features of GPCRs.
- To outline the structural diversity across the GPCR superfamily.
- To discuss the impact of structural data on drug discovery.
Main Methods:
- Review of available crystal structures for various GPCRs (e.g., rhodopsin, adrenergic, adenosine, chemokine, dopamine, histamine receptors).
- Analysis of structural features in both inactive and activated states.
- Comparative analysis across different homology levels.
Main Results:
- Crystal structures are available for key GPCRs in different conformational states.
- A modularity is observed between extracellular ligand-binding and intracellular signaling regions.
- Structural data reveals significant diversity within the GPCR superfamily.
Conclusions:
- The expanding repertoire of GPCR structures provides a framework for further research.
- Structural insights are crucial for understanding GPCR biology and therapeutic mechanisms.
- This structural knowledge aids in charting a roadmap for future drug discovery efforts targeting GPCRs.
Related Concept Videos
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...
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,...