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    GPCR

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    anaeshkl
    GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

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    GPCR

    Uploaded by

    anaeshkl
    248 views2 pages
    GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

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    GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as DOC, PDF, TXT or read online from Scribd
    Download as doc, pdf, or txt
    248 views2 pages

    GPCR

    Uploaded by

    anaeshkl
    GPCRs, also known as seven transmembrane receptors, are a protein family that senses molecules outside the cell and activates intracellular signal transduction pathways to ultimately produce cellular responses. They are classified into six classes based on sequence homology and function. GPCRs play wide physiological roles including vision, smell, behavior regulation, immune function, and the autonomic nervous system. They have a structure of seven transmembrane helices and activate signaling pathways by undergoing a conformational change upon ligand binding that activates an associated G protein. GPCR signaling can be regulated through both homologous and heterologous mechanisms involving phosphorylation and arrestin binding.

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    GPCR

    ~ aka 7 tranmembrane receptors/heptahelical receptors/ 7 transmembrane domain receptors/ G


    Protein Linked Receptors

    protein family of TM receptors that sense molecules outside cell and activate inside signal
    transduction pathways and ultimately cellular responses

    Ligand that bind include:


    Light sensitive compounds
    Odours
    Pheromones
    Hormones
    Neurotransmitters

    Classification

    6 classes based on sequence homology and functional similarity


    Class A to Class F
    GRAFS (glutamate, Rhodopsin, Adhesion, Frizzled/Taste2, Secretin)

    Physiological roles
    - wide variety
    - visual sense; rhodopsin
    - smell: odorant/pheromones
    - behavioral and mood regulation: serotonin, dopa, GABA, glutamate
    - immune system activity and inflammation: histamine receptors
    - autonomic nervous system

    Structure

    - 7 TM helices
    - extracellular parts of receptor can be glycosylated: extracellular loops contain 2 highly
    conserved cysteine reidues that form disulphide bonds

    Mechanism
    - activated by ligand
    - conformational change  activation of G protein ( depending on type of G protein)

    Ligands
    - examples
    - 3 types of ligands: agonist, inverse agonist, neutral antagonist
    Conformational change
    - ligand recognized, receptor shifts conformation and mechanically activates G protein
    - G protein detaches from receptor
    - GPCR can then activate other G protein or switch to inactive state
    - GPCR exist in conformational equilibrium between active and inactive state
    - Activated G protein are bound to GTP
    - G protein cycle activated

    GPCR signaling without G protein

    Receptor Regulation
    - 2 forms: homologous and heterologous
    - homologous- activated GPCR is downregulated
    - heterologous- activated GPCR causes downregulation of a different GPCR ( via
    phosphorylation of intracellular receptor domain by Protein kinase)

    By CAMP- dependent PK by GPCR Kinases


    - activated PK A phosphorylate GPCR - phosphorylate only active GPCR

    - 2 consequences
    translocation
    GPCR embedded in
    Dephosphorylation will bring
    back to surface

    Arrestin-linking
    Prevent from binding to G
    protein

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