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32 Cards in this Set
- Front
- Back
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What are the 5 different transmembrane signaling?
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1. Lipid soluble ligand, 2. janus kinase, 3. tyrosine kinase, 4. ligand-gated channel, 5. G-protein coupled receptor
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What are 2 examples of lipid-soluble ligands?
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1. Steroids, 2. thyroid hormones (normally hormones that regulate gene expression)
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What are the characteristics of lipid-soluble ligands?
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1. Lag time in response,2. effect persist even after agonist is removed
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Which signaling cascade utilizes receptors in the nucleus?
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Intracellular receptors for lipid soluble ligands
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What blocks the lipid-soluble-ligand blinding domain location?
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Hsp90 blocks - DNA binding domain
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What are examples of tyrosine kinase signaling?
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Insulin and trophic hormones(EGF, TGF, aka growth factors)
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What are the characteristics of tyrosine kinase signaling?
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Subject to down regulation -> ↓ total available cell surface receptors and a corresponding decline in response
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What signaling cascade utilizes self-cross - phosphorlyation
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Tyrosine kinase signaling
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What are examples of Janus kinase signaling?
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Cytokines = Erythropoietin + interferon), utilizes Jak + stat complexes
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What transmembrane signaling use Jak + stat complex?
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Jauns kinase signaling
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What are the endogenous ligands affecting Gs protein? Pathway effect?
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Endogenous ligand = catecholamines(B1), histamine (H2); pathway = ↑ adenylyl cyclase -> ↑ cAMP
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What are the endogenous ligands affecting Gi protein? Pathway effect?
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Endogenous ligand = acetylcholine (M2, M4), adrenergic amines (alpha-2); pathway = ↓ adenylyl cyclase -> ↓ cAMP -> ↓ HR
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What are the endogenous ligands affecting Golf protein? Pathway effect?
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Endogenous ligand = odorants (olfactory epithelium); pathway = ↑ adenlyl cyclase -> ↑ cAMP
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What are the endogenous ligands affecting Gq protein? Pathway effect?
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Endogenous ligand = acetylcholine (M1, M3, M5), catecholamines (alpha-1), Histamine (H1); pathway = ↑ phospholipase C -> ↑ IP3, DAG, cytoplasmic Ca2_
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What are the endogenous ligands affecting Gt protein? Pathway effect?
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Endogenous ligand = photons (rhodopsin and color opsin); pathway = phosphodiesterase -> ↓ cGMP
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What is the function of desensitization?
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Built-in over flow check to prevent excessive stimulation of a receptor systems
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Downregulation
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Irreversible
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Desentisization
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reversible
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What are examples of ligand-gated ion channels
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5HT, acetylcholine, and GABA signal via ion channels
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What are the characteristics of ligand-gated ion channels?
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1. Fast onset of action, 2. short action time
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What transmembrane receptors allows passage of ions?
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Ligand-gated ion channels
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What is an example of G-protein coupled receptor
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Second messenger systems = cAMP(EPI), cGMP, Ca2+, IP3
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What are the characteristics of G-protein coupled receptor
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1. Signal amplification, 2. spare receptors
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What transmembrane signaling normally binds GDP -> GTP?
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G-protein coupled receptors
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Which receptor regulation utilizes coated pits and lysosomes?
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Down regulation - ie EGF receptor are completely removed to prevent excessive activation
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Which receptor regulation mechanism has its intracellular tail bound by beta-arr?
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desensitization
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What is the target second messenger system in sildenafil?
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cGMP -> vascular smooth muscles and intestinal mucosa
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What are examples of durgs that bind to cGMP second messenger systems?
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1. Nitroglycerin, 2. bethanechol, 3. bradykinin, 4. histamine
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What drugs bind to IP3, DAG, and Ca2+ second messenger systems?
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1. Norepinephrine, 2. terazosin, 3. verapamil
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What is an example of reversible phosphorylation?
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Nitroglycerine -> protein kinase G (PKG)
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What is the MOA for reversible phosphorylation?
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Addition of phosphate group (PO4) to an organic molecule or a protein by a kinase
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What is an example of flexible regulation?
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Epi on cardiac muscle (constriction), vs epi on bronchial smooth muscle (dilation)(phospholambam -> produce more influx of Ca2+)
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