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Related Concept Videos

Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

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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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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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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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GPCR Desensitization01:12

GPCR Desensitization

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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...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

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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...
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Related Experiment Video

Updated: Sep 29, 2025

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay
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G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer Assay

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Common coupling map advances GPCR-G protein selectivity.

Alexander S Hauser1, Charlotte Avet2, Claire Normand3

  • 1Department of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.

Elife
|March 18, 2022
PubMed
Summary
This summary is machine-generated.

This study integrates multiple datasets to create a comprehensive map of receptor-G protein signaling. It reveals novel couplings and provides insights into G protein selectivity for drug design.

Keywords:
G proteinGPCRcomputational biologyhumanpharmacologysignal transductionsystems biology

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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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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Area of Science:

  • Pharmacology
  • Cellular Biology
  • Biochemistry

Background:

  • G protein-coupled receptors (GPCRs) mediate responses for many hormones and drugs.
  • Existing databases and datasets on GPCR-G protein interactions vary in scope and findings.
  • Understanding GPCR-G protein coupling is crucial for cellular signaling and drug development.

Purpose of the Study:

  • To develop a unified G protein coupling map by integrating existing literature and large-scale datasets.
  • To identify novel GPCR-G protein interactions and analyze their selectivity and promiscuity.
  • To compare G protein co-expression and co-coupling patterns with their phylogenetic relationships.

Main Methods:

  • Integrated data from the Guide to Pharmacology database and two recent large-scale datasets.
  • Developed a common coupling map to identify conserved and novel GPCR-G protein interactions.
  • Analyzed GPCR and G protein selectivity, promiscuity, co-coupling, and co-expression patterns.

Main Results:

  • A comprehensive map of known and novel GPCR-G protein couplings was generated.
  • Insights into the selectivity and promiscuity of GPCRs and G proteins were uncovered.
  • Comparisons between G protein co-coupling/co-expression and phylogenetic families were performed.

Conclusions:

  • The integrated coupling map advances understanding of GPCR-G protein signaling.
  • Insights into selectivity can guide the development of safer drugs targeting G protein signaling bias.
  • This work provides a foundation for future research in receptor pharmacology and cellular signaling.