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Drugs & Toxins Affecting GPCR Signaling definitions

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  • GPCR
    Membrane protein that transmits signals from extracellular ligands to intracellular pathways, often activating G proteins.
  • Adenylate Cyclase
    Effector enzyme that catalyzes conversion of ATP to cAMP, amplifying cellular signals in GPCR pathways.
  • G Protein
    Intracellular signaling molecule with alpha, beta, and gamma subunits, mediating effects of activated GPCRs.
  • cAMP
    Secondary messenger produced by adenylate cyclase, relaying signals to activate downstream effectors like PKA.
  • PKA
    Protein kinase activated by cAMP, phosphorylating target proteins to regulate cellular responses.
  • Cholera Toxin
    Bacterial protein that inhibits GTPase activity of Gs, causing persistent activation of adenylate cyclase.
  • Pertussis Toxin
    Bacterial protein that blocks GDP-GTP exchange in Gi, preventing inhibition of adenylate cyclase.
  • Gs
    Stimulatory G protein alpha subunit that activates adenylate cyclase when bound to GTP.
  • Gi
    Inhibitory G protein alpha subunit that suppresses adenylate cyclase activity when active.
  • Agonist
    Structural analog that binds a receptor and mimics the effect of a natural ligand, triggering a cellular response.
  • Antagonist
    Structural analog that binds a receptor but blocks the effect of a natural ligand, preventing a response.
  • Adenosine Receptor
    GPCR that mediates effects of adenosine, such as decreased heart rate and drowsiness.
  • Caffeine
    Molecule acting as an antagonist at adenosine receptors, blocking drowsiness and increasing heart rate.
  • GDP-GTP Exchange
    Process by which G proteins switch from inactive GDP-bound to active GTP-bound states, enabling signal transmission.
  • GTPase Activity
    Intrinsic function of G proteins that hydrolyzes GTP to GDP, terminating signal transduction.