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45 Cards in this Set
- Front
- Back
how is cAMP synthezied?
from _____ in the presence of _____ |
ATP
cyclic AMP |
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what does Gs proteins do to adenyl cyclase?
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stimulates intracellular cAMP level
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what do Gi proteins do to adenyl cyclase?
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inhibits intracellular cAMP level
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What does cAMP activate?
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PKA causing phosphorylation of multiple proteins
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Can PKA directly activate cyclic nucleotide gated ion channels?
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yes
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how is cAMP degradaded?
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by PDE (phosphodiesterase)
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what is the mechanism of action of the PDE?
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hydroluzes the 3' cyclic phosphate bond of the cyclin nucleotide (cAMP or cGMP), producing inactive AMP or GMP
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T or F
distinct reseptor signaling pathways provide hormonal regulation by either increasing or decreasing intracellular cAMP level |
T
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what catalyze the production of cGMP?
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guanylyl cyclase
GTP --> cGMP |
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what turns cGMP --> GMP
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PDE
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what activate soluble GC (guanyl cyclase)?
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NO
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what activates receptor GC?
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extracellular hormones like natriuretic peptides
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what are the two kinds of GC?
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soluble GC and receptor GC
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what does cGMP activates?
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cGMP dependent protein kinase(PKG), and cyclic nucleotide-gated (CNG) ion channels
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Does cGMP activate cyclic nucleotide gated ion channels?
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yes
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how are cyclic nucleotide gated (CNG) channel activities increased?
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by direct cyclic nucleotide binding on cytosolic side
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what do CNG (cyclic nucleotide-gated) ion channels do?
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alters cell membrane potential
major effector in visual and olfactory sensory signaling primarily permeable to Na+ ions |
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structural component of soluble GC
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heterodimers (alpha,beta) that possesses a heme prosthetic group with a ferrous (Fe2+) core that associates with His 105 of the beta subunit
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how does NO activate soluble GC?
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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
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how is soluble GC terminated?
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dissociation of NO from the heme prosthetic group
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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 |
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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.
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what do Gq proteins activate?
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phospholipase C beta
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what does phospholipase C beta do?
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cleaves PIP producing IP3 and DAG (diacylglycerol)
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what does IP3 does?
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release calcium from ER
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IP3 initiates release of calcium from ____
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ER
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what does diacylglycerol (DAG) do?
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activates protein kinase C with help of calcium
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when elevated calcium binds calmodulin, what's getting activated?
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CaM (Ca-calmodulin) protein kinase
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during amplification GPCR can activate multiple heterotrimeric G proteins, what do activated effector enzymes catalyze?
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productio of multiple second messengers
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what can phosphorylate multiple substrates altering their function?
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2nd messenger effector (i.e. PKA)
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what does Phospholipase C beta cleave?
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PIP (phosphatydylnositol 4,5 bisphosphate)
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what does cleaved PIP2 yield?
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2 bioactive 2nd messengers, DAG and inositol triphosphate (IP3)
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what 2nd messenger in vascular smooth muscle is being effected by Prazosin?
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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.
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what 2nd messengers are effected by common ED drugs (ie viagra) and what is their mechanism of action?
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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 |
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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
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PDE5
cGMP relaxation |
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phototransduction example
dark: high or low rate of transmitter release Na+ channel open or close |
high rate of transmitter
Na+ channel open = depolarization |
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phototransduction example
Light: high or low rate of transmitter release Na+ channel open or closed |
low rate
Na+ channel closed - hyperpolarization |
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when 1 photon hits rhodopsin, GPCR, cGMP activated.
Na+ channgel close --> hyperpolarization --> increase or decrease transmitter relase |
decrease
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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 |
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In case of cholera, PKA was inhibited or activated?
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activated
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what does viagra inhibit?
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PDE5 therefore prevents cGMP degradation
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mechanism to keep cytolic Ca2+ level low:
plasma membrane CaATPase pumps and exchangers that extrude Ca2+ using _____ |
ATP
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PDE can be considered _____
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G protein effector
it hydrolyzes cyclic nucleotide |
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can a patient take a selective alpha 1 adrenergic receptor blocker (Gq signaling pathway) and Viagra take at the same time?
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Yes
the two drugs have different mechanisms of action and are not contraindicated |
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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?
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No. both use the same mechanism of action and two together can cause severe hypotension
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