GMS 6552 exam with correct answers |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Most common drug target - correct answer✔✔- receptors
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Channel-linked receptors - correct answer✔✔- ion channels open when bound to ligand |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- hyperpolarization or depolarization
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- milliseconds
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- ex. nicotinic receptor, ACh receptor
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G-protein coupled receptors - correct answer✔✔- use second messenger systems to induce
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cellular effects when bound |||\\\ |||\\\ |||\\\
- seconds
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- ex. muscarinic ACh receptor
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Kinase-linked receptors - correct answer✔✔- cause protein phosphorylation inducing cellular
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effects when bound |||\\\ |||\\\
-minutes
- ex. insulin receptor
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Nuclear receptors - correct answer✔✔- induce gene transcription when bound
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- hours
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- ex. estrogen receptor
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Heterotrimeric G proteins - correct answer✔✔- receptor |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- alpha, beta, gamma - subunits
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,- amplify signal
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- induce second messenger systems
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Alpha subunit - correct answer✔✔- binds GTP converting to GDP
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GPCR ligands - correct answer✔✔- hormones
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- neurotransmitters
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- chemokines
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- ions
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- amino acids
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- peptides
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- etc.
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PKA - correct answer✔✔- protein kinase A
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- activated by cyclic AMP
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- enter nucleus and alter transcription
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Phosphorylase kinase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- breakdown glycogen
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L-type Ca Channels - correct answer✔✔- activated by PKA
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- heart contraction
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Pyruvated kinase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- activate gylcolysis
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, Hormone sensitve lipase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- cause triglyceride breakdown
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CREB - correct answer✔✔- activated by PKA
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- cause gene transcription
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Adenylate cyclase - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- cAMP as second messenger
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- activate PKA
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Phosphollipase C - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- IP3 as second messenger
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- increase Ca2+ causing contraction
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Phospholipase A2 - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- AA as secondary messanger
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- activate eicosanoids which are released as local hormones
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- activate ion channels
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Protein kinase-linked receptors - correct answer✔✔- no second messanger
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1) receptors associated with cytosolic kinases (prolactin)
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2) receptor tyrosine kinases (insulin)
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3) receptor serine/threonin kinases (TGF-b)
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Receptor tyrosine kinases - correct answer✔✔- membrane receptors that attach phosphates
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to tyrosines
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Most common drug target - correct answer✔✔- receptors
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Channel-linked receptors - correct answer✔✔- ion channels open when bound to ligand |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- hyperpolarization or depolarization
|||\\\ |||\\\ |||\\\
- milliseconds
|||\\\
- ex. nicotinic receptor, ACh receptor
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\
G-protein coupled receptors - correct answer✔✔- use second messenger systems to induce
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
cellular effects when bound |||\\\ |||\\\ |||\\\
- seconds
|||\\\
- ex. muscarinic ACh receptor
|||\\\ |||\\\ |||\\\ |||\\\
Kinase-linked receptors - correct answer✔✔- cause protein phosphorylation inducing cellular
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
effects when bound |||\\\ |||\\\
-minutes
- ex. insulin receptor
|||\\\ |||\\\ |||\\\
Nuclear receptors - correct answer✔✔- induce gene transcription when bound
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- hours
|||\\\
- ex. estrogen receptor
|||\\\ |||\\\ |||\\\
Heterotrimeric G proteins - correct answer✔✔- receptor |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- alpha, beta, gamma - subunits
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\
,- amplify signal
|||\\\ |||\\\
- induce second messenger systems
|||\\\ |||\\\ |||\\\ |||\\\
Alpha subunit - correct answer✔✔- binds GTP converting to GDP
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
GPCR ligands - correct answer✔✔- hormones
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- neurotransmitters
|||\\\
- chemokines
|||\\\
- ions
|||\\\
- amino acids
|||\\\ |||\\\
- peptides
|||\\\
- etc.
|||\\\
PKA - correct answer✔✔- protein kinase A
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- activated by cyclic AMP
|||\\\ |||\\\ |||\\\ |||\\\
- enter nucleus and alter transcription
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\
Phosphorylase kinase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- breakdown glycogen
|||\\\ |||\\\
L-type Ca Channels - correct answer✔✔- activated by PKA
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- heart contraction
|||\\\ |||\\\
Pyruvated kinase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- activate gylcolysis
|||\\\ |||\\\
, Hormone sensitve lipase - correct answer✔✔- activated by PKA |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- cause triglyceride breakdown
|||\\\ |||\\\ |||\\\
CREB - correct answer✔✔- activated by PKA
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- cause gene transcription
|||\\\ |||\\\ |||\\\
Adenylate cyclase - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- cAMP as second messenger
|||\\\ |||\\\ |||\\\ |||\\\
- activate PKA
|||\\\ |||\\\
Phosphollipase C - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- IP3 as second messenger
|||\\\ |||\\\ |||\\\ |||\\\
- increase Ca2+ causing contraction
|||\\\ |||\\\ |||\\\ |||\\\
Phospholipase A2 - correct answer✔✔- activated by GPCR |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- AA as secondary messanger
|||\\\ |||\\\ |||\\\ |||\\\
- activate eicosanoids which are released as local hormones
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
- activate ion channels
|||\\\ |||\\\ |||\\\
Protein kinase-linked receptors - correct answer✔✔- no second messanger
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
1) receptors associated with cytosolic kinases (prolactin)
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
2) receptor tyrosine kinases (insulin)
|||\\\ |||\\\ |||\\\ |||\\\
3) receptor serine/threonin kinases (TGF-b)
|||\\\ |||\\\ |||\\\ |||\\\
Receptor tyrosine kinases - correct answer✔✔- membrane receptors that attach phosphates
|||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\ |||\\\
to tyrosines
|||\\\