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What are the 5 mechanisms for signaling?
- 1- Intracellular receptors for lipid-soluble agents
- 2- Ligand-Regulated transmembrane enzymes
- 3- Cytokine Receptors
- 4- Ligand-gated ion channels
- 5- G-proteins & second messengers
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What receptor type do these drugs work on:
nitric oxide, corticosteroids, sex horomones, thyroid horomone, vitamin D
Intracellular receptors for lipid-soluble agents
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What receptor type do these drugs work on:
insulin, EGF (epidermal growth factor), PDGF (platelet-derived growth factor), TFG-beta (transforming growth factor-beta)
Ligand-regulated transmembrane enzymes (including RTKs)
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Specific inhibitors of growth factor-activated _______ ________ _______ are effective therapeutic agents in treating cancer.
receptor tyrosine kinases
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True or false, cytokine receptors do NOT have intrinsic kinase activity.
True
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What receptor type do these drugs work on:
acetylcholine, serotonin, gamma-aminobutyric acid (GABA), excitatory amino acids
Ligand-gated Ion Channels
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What receptor type do these drugs work on:
catecholamines, histamine, vasopressin, glucagon, FSH, LH, thyrotropin, PTH
G-Protein Receptor
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Which enzyme domains are invovled with ligand-regulated transmembrane enzymes? (3)
- 1- protein tyrosine kinase
- 2- serine kinase
- 3- guanylyl cyclase
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Activated tyrosine kinases phosphorylate _______ residues on different target signal proteins.
tyrosine
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What type of protein is bound non-covalently to cytokine receptors?
a tyrosine kinase from the JAK kinase family
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What are STATs?
signal transducers and activators of transcription
they regulate gene expression
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cAMP is degraded to 5'-AMP via what?
PDE (phosphodiesterases)
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_______ _______ are important targets for drug discovery.
Protein kinases
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Specific inhibitors of protein kinases are used in ________ _________
cancer chemotherapy
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