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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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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.
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GPCRs Regulate Adenylyl Cylase Activity01:09

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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

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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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Secondary Messengers in Hormone Action01:26

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Water-soluble hormones cannot cross the plasma membrane, so they rely on protein receptors that span the membrane to trigger intracellular signaling pathways. These pathways then activate second messengers inside the cell, including cAMP or calcium ions.
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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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A Paradigm for Peptide Hormone-GPCR Analyses.

Fred Naider1, Jeffrey M Becker2

  • 1Department of Chemistry, College of Staten Island, CUNY, 2800 Victory Blvd, Staten Island, NY 10314, USA.

Molecules (Basel, Switzerland)
|September 23, 2020
PubMed
Summary
This summary is machine-generated.

Researchers studied yeast G protein-coupled receptors (GPCRs) and their peptide ligands, revealing key interactions and structures. This work provides deep insights into GPCR-peptide binding dynamics without needing crystal structures.

Keywords:
G protein-coupled receptorsSaccharomyces cerevisiaechemical crosslinkingfluorescence screeningnuclear magnetic resonancepeptide analogspeptide pheromonephotoactivated crosslinkingreceptor mutationreceptor-ligand interaction

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Structural Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface proteins involved in numerous physiological processes.
  • Understanding peptide-GPCR interactions is vital for drug discovery and understanding cellular signaling.
  • The yeast Saccharomyces cerevisiae provides a powerful model system for studying fundamental receptor biology.

Purpose of the Study:

  • To review 35 years of research on the yeast Ste2p receptor and its ligand, the α-factor peptide.
  • To elucidate the structure-function relationships of Ste2p and its interaction with α-factor.
  • To explore GPCR-peptide binding mechanisms using a combination of biochemical and genetic approaches.

Main Methods:

  • Nuclear magnetic resonance (NMR) spectroscopy of Ste2p transmembrane domains.
  • Fluorescence assays for agonist and antagonist binding.
  • Biochemical crosslinking of peptide analogs to Ste2p.
  • Analysis of receptor mutant phenotypes.
  • Utilizing Saccharomyces cerevisiae as a model system.

Main Results:

  • Identified the ligand-binding domain within Ste2p.
  • Characterized functional assemblies of transmembrane domains (TMs).
  • Discovered novel ligand analogs and gained insights into bound α-factor structure.
  • Unraveled the structures and functions of various Ste2p domains (N-terminus, TMs, loops, C-terminus).
  • Revealed residue interactions specific to the active receptor state and ligand-induced dimerization.

Conclusions:

  • Comprehensive insights into GPCR-peptide interactions can be achieved without crystal structures.
  • Specific residue interactions and conformational dynamics are critical for Ste2p activation.
  • The study provides a detailed understanding of GPCR activation mechanisms and ligand binding.
  • This research lays the groundwork for further investigations into GPCR signaling pathways.