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    G Protein Coupled Receptor (GPCR) Adenylyl Cyclase: Ligand Binding

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    Panda Dao
    This document summarizes a G protein-coupled receptor (GPCR) signaling pathway. Upon ligand binding, the GPCR activates a heterotrimeric G protein composed of α, β, and γ subunits. The Gα subunit exchanges GDP for GTP and dissociates from the Gβγ subunits. The Gα subunit activates adenylyl cyclase, increasing cyclic AMP (cAMP) levels. cAMP activates protein kinase A and other downstream effectors. The Gβγ subunits can also directly activate or inhibit various effector proteins.

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    G Protein Coupled Receptor (GPCR) Adenylyl Cyclase: Ligand Binding

    Uploaded by

    Panda Dao
    36 views3 pages
    This document summarizes a G protein-coupled receptor (GPCR) signaling pathway. Upon ligand binding, the GPCR activates a heterotrimeric G protein composed of α, β, and γ subunits. The Gα subunit exchanges GDP for GTP and dissociates from the Gβγ subunits. The Gα subunit activates adenylyl cyclase, increasing cyclic AMP (cAMP) levels. cAMP activates protein kinase A and other downstream effectors. The Gβγ subunits can also directly activate or inhibit various effector proteins.

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    Zusatzmaterial G-Proteine

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    This document summarizes a G protein-coupled receptor (GPCR) signaling pathway. Upon ligand binding, the GPCR activates a heterotrimeric G protein composed of α, β, and γ subunits. The Gα subunit exchanges GDP for GTP and dissociates from the Gβγ subunits. The Gα subunit activates adenylyl cyclase, increasing cyclic AMP (cAMP) levels. cAMP activates protein kinase A and other downstream effectors. The Gβγ subunits can also directly activate or inhibit various effector proteins.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    36 views3 pages

    G Protein Coupled Receptor (GPCR) Adenylyl Cyclase: Ligand Binding

    Uploaded by

    Panda Dao
    This document summarizes a G protein-coupled receptor (GPCR) signaling pathway. Upon ligand binding, the GPCR activates a heterotrimeric G protein composed of α, β, and γ subunits. The Gα subunit exchanges GDP for GTP and dissociates from the Gβγ subunits. The Gα subunit activates adenylyl cyclase, increasing cyclic AMP (cAMP) levels. cAMP activates protein kinase A and other downstream effectors. The Gβγ subunits can also directly activate or inhibit various effector proteins.

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    G Protein coupled

    Receptor (GPCR)
    Adenylyl
    Ligand
    cyclase
    binding

    NH3+
    M1 M2

    outer
    6 1 2 3 4 5 6 1 2 3 4 5 6
    membrane
    leaflets
    1 4
    inner
    γ GTP α
    γ α GDP after C1a
    ATP
    β ligand binding ATP
    COO- β C2a

    β/γ subunit Trimeric NH3+


    COO- PPi
    G Protein
    2Pi
    cAMP
    β/γ subunits modify:
    • phospholipase A (act.) GTP GeP cAMP activates:
    • protein kinase C (act.) • cyclic AMP dependent protein kinases (e.g. protein kinase A)
    • calcium channels (inh.) • phosphodiesterases
    • Ras exchange factor (act.) • ions channels
    • adenylyl cyclase II, IV (act.) GDP GeP • exchange proteins directly activated by cAMP (EPAC)
    • adenylyl cyclase I, III, V, VI, VII (inh.) • cGMP phosphodiesterases adenylyl cyclases
    • G protein coupled receptor kinases (GCRK) (act.) • formate-hydrolase transcription activator (GAF) proteins
    M1 M2

    1 2 3 4 5 6 1 2 3 4 5 6

    GTP α C1a
    C2a
    ATP ATP

    NH3+
    COO- PPi
    2Pi cAMP
    cAMP

    R1 R2

    C1 C2
    P
    CRE
    PKAi P

    CREB = cAMP response element-binding protein PKAa ATP ADP


    CRE = cAMP response element sequence P
    PKAa/i = protein kinase A (active/inactive) Energy metabolism regulation CREB CREB-P
    äußeres

    Membran
    leaflets

    inneres

    C=O C=O C=O C=O C=O C=O C=O C=O


    O O O O O O O O
    ATP ADP 1,2 Diacylglycerin
    CH2 CH CH2 ATP ADP CH2 CH CH2 CH2 CH CH2 CH2 CH CH2 (DAG)
    O O O Phospho- OH
    P=O PI-5 kinase P=O
    lipase C
    O P=O PI-4 kinase O O
    OH OH P H2O
    O6 5 O6 5 O6 5 P P
    Inositol

    6 5
    OH 1 OH 4 1 OH 4
    1 4 OH HO OH HO
    OH HO 1 OH 4
    OH 2 3 P 2 P OH HO
    2 3 3
    2 3 P
    Phosphatidyl- PI 4 phosphat PI 4,5 bisphosphat
    (PIP2) PI 1,4,5 tris-
    Inositol (PI) (PIP)
    phosphat
    (IP3)

    Phospholipase C kann entweder


    durch die aktivierte Gαq oder
    durch die β/γ Untereinheit
    aktiviert werden.

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