Signal Transduction II Flashcards
ligand gated ion channels
found on electrically excitable cells
when receptor is open, ions enter/ exit along electrochemical gradients
FAST response
GABA receptor
inhibitory transmitter
opens Cl- channels, HYPERPOLARIZATION-> muscle relax
PAMs
bind to sites other than GABA, enhance GABA dependent activity of receptor
nicotinic acethycholinergic receptor
Ach binds to cause conformational changes
forms pore that allows Na+ to enter-> DEPOLARIZATION
ligand degraded by acetylcholinesterases and signal terminated
alpha subunit of G-protein coupled receptors
binds to GTP/GDP
when bound to GTP=ON
G alpha S
stimulates adenylyl cyclase and increases cAMP production
G alpha I
inhibits adenylyl cyclase and decreases cAMP production
G alpha Q
activates phospholipase C and stimulates IP3 and DAG production
PIP2 will activate
DAG and IP3 (G alpha Q pathway)
IP3 will bind to calcium channel, released calcium will help DAG activate PKC
calmodulin
Ca2+ binds to calcium responsive proteins
undergoes conformational change to interact w other signaling proteins
heart muscle ach signaling
potassium outflow-> decreased muscle contraction
skeletal muscle
influx of sodium-> increase muscle contraction
alpha subunit g-protein termination
inactivates itself via GTP hydrolysis
desensitization
GPCR desensitize themselves by activating GRKs
-GRKs phosphorylate intracellular domains of GPCR
-arrestin binds to phosphorylated residues on GPCR-> blocks binding and prevents from becoming reactivated
wnt protein
ligan
frizzled
receptor
beta-catenin
when activated, binds to TF to promote transcription of genes
helps regulate development and growth
when Wnt not bound
APC and GSK-3 phosphoylates beta-catenin and degrades it
no signaling, no transcription
when Wnt bound
Wnt binds to frizzled, inactivates APC and GSK-3 complex
saves beta-catenin from degradation, translocate into nucleus and binds to TF
SHH
ligand
PTCH
receptor
SHH not bound
PTCH associated with GPCR (SMO)
keeps in inactive state
SHH bound
PTCH and SMO dissociate
active state
-turns on signaling cascade that leads to increased gene expression through TF (GL11)
—important during embryogenesis
notch signaling
signaling for organogenesis/ neurogenesis
-binding of notch to its ligand on neighbor cell
-delta notch complex internalized by delta possessing cell
-conformational change occurs in cytoplasmic domain of notch
-cleaved domain tranlocates into nucleus