answers A+ rated
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
-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)
Receptor tyrosine kinase pathway - correct answer ✔✔- ligand binds > IRS proteins > PI-3 Kinase >
PKD/Akt < PDK1/2
PKB/Akt - correct answer ✔✔- activated by PI-3 Kinase & PDK1/2