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Related Concept Videos

GPCR Desensitization01:12

GPCR Desensitization

6.1K
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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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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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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2.4K
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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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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Updated: May 1, 2026

Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors GPCRs
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Construction of Model Lipid Membranes Incorporating G-protein Coupled Receptors GPCRs

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Towards selective lysophospholipid GPCR modulators.

Julia K Archbold1, Jennifer L Martin1, Matthew J Sweet2

  • 1Division of Chemistry and Structural Biology, The University of Queensland, Institute for Molecular Bioscience, St Lucia, Brisbane, QLD 4072, Australia.

Trends in Pharmacological Sciences
|April 22, 2014
PubMed
Summary
This summary is machine-generated.

Researchers aim to determine the structure of non-endothelial differentiation gene (Edg) G-protein-coupled receptors (GPCRs). This structural insight is crucial for developing targeted drugs for cancer, inflammation, and neurological disorders.

Keywords:
G-protein-coupled receptors (GPCRs)GPCR structureendothelial-derived growth factor (Edg)lysophosphatidic acid (LPA)sphingosine 1-phosphate (S1P)

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A Pipeline to Investigate the Structures and Signaling Pathways of Sphingosine 1-Phosphate Receptors
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Area of Science:

  • Biochemistry
  • Pharmacology
  • Structural Biology

Background:

  • G-protein-coupled receptors (GPCRs) recognizing lysophospholipids (LPLs) are classified into endothelial differentiation gene (Edg) and non-Edg families.
  • Understanding of non-Edg GPCRs is limited due to recent discovery and lack of selective drugs.
  • Structure-based drug design targeting allosteric sites offers potential for selective LPL GPCR modulators.

Purpose of the Study:

  • To obtain a representative structure of a non-Edg GPCR.
  • To facilitate structure-based drug design for novel LPL GPCRs.
  • To enable the development of selective modulators for non-Edg receptors.

Main Methods:

  • Structure determination of non-Edg GPCRs.
  • Comparative analysis with known Edg GPCR structures (e.g., S1PR1).
  • Development of selective pharmacological tools.

Main Results:

  • Currently, only one Edg GPCR (S1PR1) structure is available, showing low sequence identity (<20%) with non-Edg GPCRs.
  • A pressing need exists for a representative non-Edg GPCR structure.
  • Selective modulators for non-Edg receptors are yet to be developed.

Conclusions:

  • A representative structure of a non-Edg GPCR is essential for advancing structure-based drug design.
  • Elucidating non-Edg GPCR structures will aid in understanding their biological roles.
  • Targeting non-Edg GPCRs holds therapeutic potential for cancer, inflammation, and neuropsychiatric disorders.