Most common drug target - answer-- receptors
Channel-linked receptors - answer-- ion channels open when bound to ligand
- hyperpolarization or depolarization
- milliseconds
- ex. nicotinic receptor, ACh receptor
G-protein coupled receptors - answer-- use second messenger systems to induce ...
Channel-linked receptors - answer-- ion channels open when bound to ligand
- hyperpolarization or depolarization
- milliseconds
- ex. nicotinic receptor, ACh receptor
G-protein coupled receptors - answer-- use second messenger systems to
induce cellular effects when bound
- seconds
- ex. muscarinic ACh receptor
Kinase-linked receptors - answer-- cause protein phosphorylation inducing
cellular effects when bound
-minutes
- ex. insulin receptor
PKA - answer-- protein kinase A
- activated by cyclic AMP
- enter nucleus and alter transcription
Phosphorylase kinase - answer-- activated by PKA
- breakdown glycogen
, L-type Ca Channels - answer-- activated by PKA
- heart contraction
Pyruvated kinase - answer-- activated by PKA
- activate gylcolysis
Hormone sensitve lipase - answer-- activated by PKA
- cause triglyceride breakdown
CREB - answer-- activated by PKA
- cause gene transcription
Adenylate cyclase - answer-- activated by GPCR
- cAMP as second messenger
- activate PKA
Phosphollipase C - answer-- activated by GPCR
- IP3 as second messenger
- increase Ca2+ causing contraction
Phospholipase A2 - answer-- activated by GPCR
- AA as secondary messanger
- activate eicosanoids which are released as local hormones
- activate ion channels
Protein kinase-linked receptors - 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 - answer-- membrane receptors that attach
phosphates to tyrosines
-two types
1) single transmembrane spanning protiens that dimerize when ligand binds
(EGF receptor, PDGF receptor)
2) Covalently linked dimers (insulin receptor, IGF-1 receptor)
PKB/Akt - answer-- activated by PI-3 Kinase & PDK1/2
- induces multiple pathways
- GSK-3 (stimulates glucose synthesis or protein synthesis)
- 6PF2K (stimulates glycolysis)
- GLUT4 (stimulates glucose transport)
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