Lecture 9 Signaling - BergTymoczkoStryer Biochemistry...

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Biochemistry Sixth Edition Chapter 14: Signal-Transduction Pathways Copyright  ©  2007 by W. H. Freeman and Company   Berg • Tymoczko • Stryer
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Three signal transduction pathways
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Principles of signal transduction Release of the primary messenger Reception Interaction of the primary messenger with receptors Relay of the signal: generation of second messengers activation of protein kinase cascades Response Activation or inhibition of effector proteins that directly alter the physiological response Signal termination Specificity/selectivity Affinity
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Second messengers Characteristics : Intracellular mcls Concentration changes in response to signaling events Signal amplification
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Signaling: seven transmembrane helix receptors and heterotrimeric G proteins
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hormones, neurotransmitters odorants photons Approx. 33% of therapeutic drugs target receptors of this class
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Structure of 7TM receptors Pass through the membrane 7 times Also called serpentine receptors Rhodopsin : 7TM receptor plays an essential role in vision first member of the family to a structure determined
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Ligand binding to 7TM receptors leads to activation of heterotrimeric G proteins G protein: binds guanine nucleotides Also, hetero tri meric G-protein: α , β and γ subunits G α ACTIVE 7TM receptors = G-protein coupled receptors (GPCRs)
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The surface of G α that binds βγ also binds adenylate cyclase =
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G proteins transmit a signal when bound to GTP and are silent when bound to GDP
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