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Related Concept Videos

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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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 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.
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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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Because the DNA segments are cut and reorganized in a direction-specific manner, site-specific recombination has emerged as an efficient genetic engineering technique. Flippase and Cyclization recombinases or Flp and Cre, respectively, are two members of the tyrosine recombinase family derived from bacteriophages, that are used to mediate site-specific DNA insertions, deletions, and targeted expression of proteins in mammalian cell lines.
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
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DREADD: a chemogenetic GPCR signaling platform.

Hu Zhu1, Bryan L Roth2

  • 1Department of Pharmacology, University of North Carolina Chapel Hill Medical School, Chapel Hill, NC (Drs Zhu and Roth).

The International Journal of Neuropsychopharmacology
|December 19, 2014
PubMed
Summary
This summary is machine-generated.

Designer receptors exclusively activated by designer drugs (DREADDs) precisely control major G protein-coupled receptor signaling pathways. This technology offers potential applications in drug discovery, gene therapy, and tissue engineering.

Keywords:
GPCRsGsDchemogeneticshM3DqhM4Di

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • G protein-coupled receptors (GPCRs) are crucial cell surface receptors involved in numerous physiological processes.
  • Precise control over GPCR signaling pathways is essential for understanding cellular mechanisms and developing targeted therapies.

Purpose of the Study:

  • To introduce engineered GPCRs, known as DREADDs (designer receptors exclusively activated by designer drugs).
  • To highlight recent advancements in DREADD technology.
  • To discuss the potential applications of DREADDs in drug discovery, gene therapy, and tissue engineering.

Main Methods:

  • Development of a family of engineered GPCRs (DREADDs).
  • Demonstration of precise control over three major GPCR signaling pathways: Gq, Gi, and Gs.
  • Application of DREADD technology in various in vivo studies.

Main Results:

  • DREADDs enable highly specific activation or inhibition of GPCR signaling pathways.
  • The technology has been successfully validated in diverse in vivo experimental models.
  • Recent advances have expanded the capabilities and applications of DREADD technology.

Conclusions:

  • DREADD technology provides a powerful tool for precise manipulation of GPCR signaling.
  • This technology holds significant promise for advancing drug discovery and therapeutic strategies.
  • Further development of DREADDs could revolutionize gene therapy and tissue engineering approaches.