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h. Introduction to Signaling and G-Protein-Coupled Receptors
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Intracellular receptors use small {{c1::hydrophobic}} molecules as ligands
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Cell surface receptors have {{c1::hydrophilic}} molecules as ligands
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Signaling pathways that produce altered protein function are {{c1::fast}} in speed
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Signaling pathways that produce altered protein synthesis are {{c1::slow}} in speed
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A {{c1::protein kinase}} covalently adds a phosphate from ATP to the signaling protein
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A protein {{c1::phosphatase}} removes a phosphate group from a signaling molecule
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GTP-binding proteins are {{c1::activated}} when bound GDP is exchanged for GTP
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G-proteins are {{c1::inactivated}} by GTPase activity that hydrolyzes bound GTP to GDP
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GPCR stands for {{c1::G-protein coupled receptor}}
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{{c1::GPCRs}} are {{c2::integral}} membrane proteins comprised of a single peptide forming {{c3::7}} membrane-spanning alpha helices
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In the intracellular domain of GPCRs, {{c1::Ser/Thr}} residues are {{c2::phosphorylated}} in response to ligand binding
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GPCRs activate {{c1::heterotrimeric}} G-proteins (which is different from Ran-GTP and Rab-GTP which need GAP and GEF)
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{{c1::Agonists}} are compounds that stimulate signal transduction
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{{c1::Antagonists}} are compounds that inhibit signal transduction and bind to {{c1::antagonist}} binding sites that are structurally {{c1::distinct}}…
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Explain the basic process for activation of heterotrimeric g-protein by GPCRs:
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Heterotrimeric G-proteins are associated with the membrane via {{c1::lipid}} modifications
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GPCRs regulate signaling pathways that control intracellular levels of {{c1::cAMP (which is formed by adenylyl cyclase and activates PKA (cAMP-de…
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The {{c1::alpha}} subunit of {{c2::Gs}} protein is responsible for activating {{c3::adenylyl cyclase}} which in turn is responsible for…
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{{c1::Phosphodiesterase}} deactivates PKA by converting cAMP to AMP which means that cAMP can no longer bind to PKA and activate the enzyme
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{{c1::Adenylyl Cyclase}} is activated by alpha Gs and produces cAMP
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The alpha subunit of Gi inactivates {{c1::adenylyl cyclase}}
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{{c1::Gs}} is locked in the active state by cholera toxin
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{{c1::Gi}} activation is prevented by pertussis toxin
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PKA is responsible for what 2 steps in glucagon regulation?
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What role does Protein Kinase A (PKA) play in transcriptional responses?
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In GPCR calcium signaling the activated {{c1::beta-gamma}} subunit of the {{c2::Gq}} protein activates {{c3::Phospholipase C}}, which {…
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Protein kinase C must bind the {{c1::diacylglycerol}} and {{c2::calcium}} in order to be activated
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The activation of {{c2::PKC}} by diacylglycerol and Calcium stimulates gene expression by activating the transcription factor {{c1::NF-(kappa)B}}
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{{c1::Calmodulin}} is a {{c2::calcium}} binding protein that is abundant and activates various other enzymes
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GPCRs can be inactivated by {{c1::phosphorylation}} which causes {{c2::arrestin}} to bind, and prevent interactions with GTP
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What are 2 methods by which GPCRs can be directly inactivated?
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