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Related Concept Videos

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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GPCR Desensitization01:12

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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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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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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.
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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Microbial Biosensors01:17

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Microbial biosensors are analytical devices that utilize living microbes to detect specific substances through measurable signals. These devices consist of two main components: biosensing organisms and signal-transducing elements. Biosensing organisms, such as Escherichia coli or Saccharomyces cerevisiae, are typically housed in multiwell plates connected to transducers, enabling rapid, real-time detection of target analytes.Signal Generation MechanismWhen a target analyte—such as...
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Direct interrogation of context-dependent GPCR activity with a universal biosensor platform.

Remi Janicot1, Marcin Maziarz1, Jong-Chan Park1

  • 1Department of Biochemistry & Cell Biology, Chobanian & Avedisian School of Medicine, Boston University, Boston, MA 02118, USA.

Cell
|February 27, 2024
PubMed
Summary

Researchers developed a new biosensor platform to measure G protein-coupled receptor (GPCR) activity in cells. This tool offers high fidelity insights into GPCR signaling, aiding drug discovery and understanding cellular responses.

Keywords:
BRETG proteinGPCRGTPaseantipsychoticsbiased signalingbiosensordrug discoveryfibrosisneurotrasnmitter

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Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are a major class of drug targets.
  • Current tools lack the precision to study GPCRs in physiological settings.
  • Understanding GPCR behavior is crucial for developing new therapeutics.

Purpose of the Study:

  • To create a scalable platform for measuring GPCR activity.
  • To enable high-fidelity assessment of G-protein activation by any GPCR.
  • To investigate GPCR signaling in endogenous and primary cells.

Main Methods:

  • Development of compact ONE vector G-protein Optical (ONE-GO) biosensor constructs.
  • Characterization of numerous GPCRs across diverse cell types, including primary cardiovascular cells and neurons.
  • Application of the platform to study GPCRs in disease-relevant conditions.

Main Results:

  • Revealed insights into the molecular basis of GPCR G-protein coupling selectivity.
  • Determined pharmacogenomic profiles of antipsychotics on natural GPCR variants.
  • Identified cell-type-specific and disease-state-dependent G-protein subtype signaling bias by endogenous GPCRs.

Conclusions:

  • The open-source ONE-GO platform provides broad accessibility for studying context-dependent GPCR activity.
  • This tool facilitates a deeper understanding of GPCR function in health and disease.
  • Enables direct interrogation of GPCR signaling in physiologically relevant systems.