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Related Concept Videos

G Protein-coupled Receptors01:15

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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 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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Immunoglobulin-like cell adhesion molecules or Ig-CAMs are a versatile group of cell surface glycoproteins belonging to the immunoglobulin protein superfamily. Ig-CAMs possess the characteristic immunoglobulin protein domains and other domains such as the fibronectin type III domain. The Ig domains are glycosylated to varying degrees in different Ig-CAMs.
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A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
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Adhesion GPCRs in immunology.

Saskia Nijmeijer1, Henry F Vischer1, Rob Leurs1

  • 1Vrije Universiteit Amsterdam, Department of Medicinal Chemistry, O|2 Building, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.

Biochemical Pharmacology
|May 2, 2016
PubMed
Summary

Adhesion GPCRs (aGPCRs) are key cell surface receptors involved in immune responses. Their unique structure suggests potential as novel drug targets for modulating immune cell function.

Keywords:
AdhesionGPCRImmunologyLeucocytesSignallingaGPCR

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Area of Science:

  • Cell biology
  • Immunology
  • Biochemistry

Background:

  • Adhesion GPCRs (aGPCRs) are a subfamily of G protein-coupled receptors.
  • They possess a bipartite structure with large extracellular domains for cell adhesion and transmembrane domains for signaling.
  • aGPCRs are implicated in immune processes like phagocytosis and leukocyte migration.

Purpose of the Study:

  • To explore the potential of aGPCRs as drug targets for immune modulation.
  • To highlight the challenges in aGPCR research, including unknown ligands and pathways.

Main Methods:

  • Literature review and analysis of existing research on aGPCRs.
  • Focus on the structural and functional characteristics of aGPCRs in the context of immunity.

Main Results:

  • aGPCRs integrate cell adhesion with intracellular signaling pathways.
  • Specific aGPCRs, such as ADGRB1 and ADGRE family members, are linked to immune cell functions.
  • Research is limited by the lack of identified endogenous ligands and signaling mechanisms.

Conclusions:

  • aGPCRs represent promising targets for developing novel immunomodulatory drugs.
  • Further research is needed to elucidate their specific ligands and signaling pathways to fully exploit their therapeutic potential.