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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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Molecular Models02:00

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Physical models representing molecular architectures of chemical compounds play essential roles in understanding chemistry. The use of molecular models makes it easier to visualize the structures and shapes of atoms and molecules.
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Cooperative Allosteric Transitions01:58

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Cooperative allosteric transitions can occur in multimeric proteins, where each subunit of the protein has its own ligand-binding site. When a ligand binds to any of these subunits, it triggers a conformational change that affects the binding sites in the other subunits; this can change the affinity of the other sites for their respective ligands. The ability of the protein to change the shape of its binding site is attributed to the presence of a mix of flexible and stable segments in the...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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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Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

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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,...
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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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Related Experiment Video

Updated: May 6, 2026

Strategic Screening and Characterization of the Visual GPCR-mini-G Protein Signaling Complex for Successful Crystallization
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Structure-based molecular modeling approaches to GPCR oligomerization.

Agnieszka A Kaczor1, Jana Selent, Antti Poso

  • 1Department of Pharmaceutical Chemistry, School of Pharmacy, University of Eastern Finland, Kuopio, Finland; Department of Chemical Technology of Pharmaceutical Substances with Computer Modeling Lab, Faculty of Pharmacy with Division of Medical Analytics, Medical University of Lublin, Lublin, Poland.

Methods in Cell Biology
|October 23, 2013
PubMed
Summary
This summary is machine-generated.

Targeting G-protein-coupled receptor (GPCR) complexes offers new drug discovery avenues. This chapter details structure-based modeling methods like protein-protein docking for studying GPCR dimerization and interactions.

Keywords:
ElectrostaticsG-protein-coupled receptorsMolecular dynamicsNormal mode analysisProtein–protein docking

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Computational Biology

Background:

  • Traditional drug design targets single G-protein-coupled receptors (GPCRs) at orthosteric sites.
  • GPCR dimerization and oligomerization are critical for drug design, offering novel therapeutic targets.
  • Understanding GPCR complex dynamics is key for developing selective drugs targeting receptor interactions.

Purpose of the Study:

  • To provide a comprehensive overview of structure-based molecular modeling techniques for studying GPCR dimerization.
  • To highlight the importance of GPCR oligomerization in drug discovery.
  • To describe methods for analyzing receptor-receptor interactions and identifying potential drug binding sites.

Main Methods:

  • Protein-protein docking simulations to predict GPCR complex formation.
  • Molecular dynamics and normal mode analysis to investigate dynamic processes of dimerization.
  • Electrostatics studies to understand interaction forces driving GPCR association.
  • Experimental techniques like Förster resonance energy transfer (FRET) and Bioluminescence resonance energy transfer (BRET) complement computational approaches.

Main Results:

  • Structure-based modeling provides insights into the mechanisms and dynamics of GPCR oligomerization.
  • Identification of specific regions involved in receptor-receptor interactions.
  • Potential for designing small molecules that modulate GPCR complex formation and function.

Conclusions:

  • GPCR dimerization and oligomerization represent a promising area for novel drug discovery.
  • Structure-based molecular modeling is essential for elucidating GPCR complex dynamics.
  • Targeting GPCR complexes offers a new paradigm for developing selective therapeutics.