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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 Receptors01:15

G Protein-coupled Receptors

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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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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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IP3/DAG Signaling Pathway01:11

IP3/DAG Signaling Pathway

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Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the  phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and...
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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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Updated: May 4, 2026

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors GPCRs
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Intercellular Lipid Mediators and GPCR Drug Discovery.

Dong-Soon Im1

  • 1Molecular Inflammation Research Center for Aging Intervention (MRCA) and College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea.

Biomolecules & Therapeutics
|January 10, 2014
PubMed
Summary

G-protein-coupled receptors (GPCRs) are key drug targets. New research explores lipid mediators and their GPCRs for novel drug discovery, focusing on lysophospholipids and fatty acids.

Keywords:
Drug discoveryFatty acidGPCRLipidLipid mediatorLysophospholipid

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Area of Science:

  • Pharmacology
  • Cell Biology
  • Biochemistry

Background:

  • G-protein-coupled receptors (GPCRs) are the largest receptor superfamily, crucial for cellular signaling and homeostasis.
  • GPCRs represent significant targets for therapeutic intervention due to their physiological importance.
  • Recent technological advancements facilitate the identification of novel GPCR ligands and functions.

Purpose of the Study:

  • To review the discovery of intercellular lipid mediators and their cognate GPCRs.
  • To highlight the drug discovery potential of lipid-mediated signaling pathways.
  • To discuss emerging lipid mediators and their roles in drug development.

Main Methods:

  • Literature review of recent research on lipid mediators and GPCRs.
  • Analysis of drug discovery efforts targeting lipid GPCRs.
  • Identification and categorization of various lipid classes acting on GPCRs.

Main Results:

  • Intercellular lipid mediators, including lysophosphatidic acid and sphingosine 1-phosphate, have yielded successful drugs like fingolimod (FTY-720).
  • Numerous lipid GPCRs for lysophospholipids (e.g., lysophosphatidylserine, lysophosphatidylinositol, lysophosphatidylcholine) and free fatty acids have been identified.
  • The review encompasses a broad range of lipid mediators and their associated GPCRs relevant to drug development.

Conclusions:

  • Lipid GPCRs represent a promising area for novel drug discovery.
  • Further exploration of lipid mediators and their signaling pathways can lead to new therapeutic agents.
  • Targeting lipid GPCRs offers a viable strategy for developing treatments for various physiological conditions.