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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

13.7K
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

2.6K
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,...
2.6K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

121.9K
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.
121.9K
The Two-State Receptor Model01:29

The Two-State Receptor Model

2.5K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
2.5K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

7.8K
Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...
7.8K
GPCR Desensitization01:12

GPCR Desensitization

6.6K
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...
6.6K

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Updated: Sep 24, 2025

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

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G-Protein coupled receptors: structure and function in drug discovery.

Chiemela S Odoemelam1, Benita Percival1, Helen Wallis1

  • 1Nottingham Trent University 50 Shakespeare St Nottingham NG1 4FQ UK philippe.wilson@ntu.ac.uk.

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|May 6, 2022
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Summary

This review covers computational advances in G-protein coupled receptor (GPCR) pharmacology and drug discovery. It details GPCR families, signaling, and the role of dielectric constants in protein environments.

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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Area of Science:

  • Biochemistry
  • Pharmacology
  • Computational Biology

Background:

  • G-protein coupled receptors (GPCRs) form a large superfamily crucial for physiological functions and drug development.
  • GPCRs exhibit conserved structural features like seven transmembrane domains, but vary in residue conservation.
  • Understanding GPCRs is vital for developing novel therapeutics targeting various diseases.

Purpose of the Study:

  • To provide an accessible review of computational advances in GPCR pharmacology.
  • To detail progress in GPCR drug discovery methodologies.
  • To offer an overview of GPCR families, signaling, and binding properties.

Main Methods:

  • Review of existing literature on computational approaches in GPCR research.
  • Analysis of structural and functional differences across GPCR families (A-C).
  • Discussion of GPCR signaling mechanisms, allosteric binding, and cooperativity.

Main Results:

  • Highlights computational tools and strategies enhancing GPCR drug discovery.
  • Explains structural variations and their impact on GPCR function.
  • Discusses the influence of protein dielectric constants on ligand binding and signaling.

Conclusions:

  • Computational methods are pivotal for advancing GPCR pharmacology and drug discovery.
  • A comprehensive understanding of GPCR structure-function relationships aids in targeted drug design.
  • Further research into GPCRs, including environmental effects, can unlock new therapeutic avenues.