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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

14.8K
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

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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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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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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

127.8K
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.
127.8K
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...
7.1K
Activation and Inactivation of G Proteins01:22

Activation and Inactivation of G Proteins

8.5K
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: Nov 9, 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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Coevolution underlies GPCR-G protein selectivity and functionality.

Min Jae Seo1, Joongyu Heo2, Kyunghui Kim2

  • 1Department of Brain and Cognitive Sciences, DGIST, 333 Techno jungang-daero, Daegu, 42988, Republic of Korea.

Scientific Reports
|April 13, 2021
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) and G proteins interact selectively. Coevolutionary analysis revealed conserved residues in GPCRs and G proteins, clarifying their molecular functions and interaction mechanisms.

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Last Updated: Nov 9, 2025

G Protein-selective GPCR Conformations Measured Using FRET Sensors in a Live Cell Suspension Fluorometer 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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Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
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Area of Science:

  • Molecular Biology
  • Biochemistry
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial drug targets regulating physiological processes.
  • G proteins act as downstream signaling molecules for GPCRs, initiating cellular responses.
  • The precise mechanisms governing GPCR-G protein selectivity remain incompletely understood.

Purpose of the Study:

  • To investigate the molecular basis of selectivity between GPCRs and G proteins.
  • To identify conserved and coevolved residues within GPCRs and G proteins.
  • To elucidate the role of these residues in GPCR-G protein interactions.

Main Methods:

  • Utilized statistical coupling analysis, a coevolutionary tool.
  • Analyzed model GPCRs, including 5-hydroxytryptamine receptors (HTR) and dopamine receptors (DAR).
  • Examined conserved and coevolved residues in Gα proteins.

Main Results:

  • Identified common conserved and coevolved residues in HTR and DAR.
  • Found conserved and coevolved residues within Gα proteins.
  • Discovered specific coevolving pairs critical for GPCR-G protein selectivity.
  • Linked coevolved residues to protein molecular functions.

Conclusions:

  • The study provides insights into functional residues of GPCRs and Gα proteins.
  • Coevolutionary analysis illuminates the molecular mechanisms of GPCR-G protein selectivity.
  • Findings contribute to a deeper understanding of drug target interactions.