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45 Cards in this Set

  • Front
  • Back
how is cAMP synthezied?
from _____ in the presence of _____
ATP
cyclic AMP
what does Gs proteins do to adenyl cyclase?
stimulates intracellular cAMP level
what do Gi proteins do to adenyl cyclase?
inhibits intracellular cAMP level
What does cAMP activate?
PKA causing phosphorylation of multiple proteins
Can PKA directly activate cyclic nucleotide gated ion channels?
yes
how is cAMP degradaded?
by PDE (phosphodiesterase)
what is the mechanism of action of the PDE?
hydroluzes the 3' cyclic phosphate bond of the cyclin nucleotide (cAMP or cGMP), producing inactive AMP or GMP
T or F
distinct reseptor signaling pathways provide hormonal regulation by either increasing or decreasing intracellular cAMP level
T
what catalyze the production of cGMP?
guanylyl cyclase

GTP --> cGMP
what turns cGMP --> GMP
PDE
what activate soluble GC (guanyl cyclase)?
NO
what activates receptor GC?
extracellular hormones like natriuretic peptides
what are the two kinds of GC?
soluble GC and receptor GC
what does cGMP activates?
cGMP dependent protein kinase(PKG), and cyclic nucleotide-gated (CNG) ion channels
Does cGMP activate cyclic nucleotide gated ion channels?
yes
how are cyclic nucleotide gated (CNG) channel activities increased?
by direct cyclic nucleotide binding on cytosolic side
what do CNG (cyclic nucleotide-gated) ion channels do?
alters cell membrane potential
major effector in visual and olfactory sensory signaling
primarily permeable to Na+ ions
structural component of soluble GC
heterodimers (alpha,beta) that possesses a heme prosthetic group with a ferrous (Fe2+) core that associates with His 105 of the beta subunit
how does NO activate soluble GC?
by directly binding to the ferrous core, breaking the bond b/w iron and histidine 105, causing activation of the GC domain and production of cGMP
how is soluble GC terminated?
dissociation of NO from the heme prosthetic group
T or F
CO can also bind to the heme group of soluble GC and has exactly the same affect as NO
F
CO does bind to the heme group of sGC, but is far less efficacious as an activator of the GC domain. It does not break the Fe-His105 bond
cGMP-dependent protein kinase (PKG) is a member of the serine/threonine protein kinase family, what does it do?

phosphorylates multiple proteins at _____residues, altering protein activity/function.
phosphorylates multiple proteins at Ser/Thr residues, altering protein activity/function.
what do Gq proteins activate?
phospholipase C beta
what does phospholipase C beta do?
cleaves PIP producing IP3 and DAG (diacylglycerol)
what does IP3 does?
release calcium from ER
IP3 initiates release of calcium from ____
ER
what does diacylglycerol (DAG) do?
activates protein kinase C with help of calcium
when elevated calcium binds calmodulin, what's getting activated?
CaM (Ca-calmodulin) protein kinase
during amplification GPCR can activate multiple heterotrimeric G proteins, what do activated effector enzymes catalyze?
productio of multiple second messengers
what can phosphorylate multiple substrates altering their function?
2nd messenger effector (i.e. PKA)
what does Phospholipase C beta cleave?
PIP (phosphatydylnositol 4,5 bisphosphate)
what does cleaved PIP2 yield?
2 bioactive 2nd messengers, DAG and inositol triphosphate (IP3)
what 2nd messenger in vascular smooth muscle is being effected by Prazosin?
prozosin's block of alpha1adrenergic receptors inhibits vascular PLC-beta activation by Gq and the production of DAG, IP3 and Ca release. since intracellular calcium triggers contraction of cascular smooth muscle, reducing intracellular Ca2+ promotes vasodilation and effectively lowers arterial blood pressure.
what 2nd messengers are effected by common ED drugs (ie viagra) and what is their mechanism of action?
PDE
viagra is a selective inhibitor of PDE5 which is responsible for degradation of cGMP in the corpus cavernosum. when sexual stimulation causes local release of NO, sildenafil inhibition of PDE5 causes increased levels of cGMP in the corpus cavernosum resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum
viagra is a selective inhibitor of ____ which is responsible for degradation of cGMP in the corpus cavernosum. when sexual stimulation causes local release of NO, sildenafil inhibition of PDE5 causes increased levels of ____ in the corpus cavernosum resulting in smooth muscle ______ and inflow of blood to the corpus cavernosum
PDE5
cGMP
relaxation
phototransduction example
dark: high or low rate of transmitter release
Na+ channel open or close
high rate of transmitter
Na+ channel open = depolarization
phototransduction example
Light: high or low rate of transmitter release
Na+ channel open or closed
low rate
Na+ channel closed - hyperpolarization
when 1 photon hits rhodopsin, GPCR, cGMP activated.
Na+ channgel close --> hyperpolarization --> increase or decrease transmitter relase
decrease
match up the followings:
signal molecule, cyclic AMP, adenyl cyclase

1st messegner, Gprotein effector, 2nd messenger
signal molecule - 1st messenger
cAMP - 2nd messenger
adenyl cyclase - G-protein effector
In case of cholera, PKA was inhibited or activated?
activated
what does viagra inhibit?
PDE5 therefore prevents cGMP degradation
mechanism to keep cytolic Ca2+ level low:
plasma membrane CaATPase pumps and exchangers that extrude Ca2+ using _____
ATP
PDE can be considered _____
G protein effector
it hydrolyzes cyclic nucleotide
can a patient take a selective alpha 1 adrenergic receptor blocker (Gq signaling pathway) and Viagra take at the same time?
Yes
the two drugs have different mechanisms of action and are not contraindicated
can a patient take a generic nitrates for maintenance of high BP( which activates soluble GC and increases cGMP) and Viagra take at the same time?
No. both use the same mechanism of action and two together can cause severe hypotension