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44 Cards in this Set

  • Front
  • Back
where is the site for G protein interaction on GPCR's?
at the intracellular C-terminus and C3 loop
where are the ligands recognized in GPCR's?
at the 3D pocket made by the extracellular N-terminus and loop domains
what is wrong in familial male precocious disease?
autosomal dominant
aspartate to glycine in H6 of LH GPCR
always active
what is wrong in thyroid adenoma?
hyperthyroidism
two mutations in third cytoplasmic loop, aspartic acid to glycine and alanine to isoleucine
independent activation
how are subfamilies of G proteins categorized?
by amino acid sequence of G alpha subunit
how many subunits do G proteins have
3
alpha, beta and gamma
what are the actions of the G alpha subunit?
binds to activating sequence of GPCR
binds and hydrolyzes GTP to GDP
what turns off the G protein signaling pathway?
GTPase activity of the G alpha subunit
GTP to GDP
effect of cholera toxin on G protein?
inhibits GTPase, persistent activation
effect of pertussis toxin on G protein?
blocks the interaction of subunit with receptor
what cytosolic proteins contain SH2 domains?
PI3-kinase
PLC-gamma
GTPase-activating protein
what is the ligand for soluble guanylyl cyclases?
NO
what is the ligand for membrane-bound guanylyl cyclases?
ANF
what site binds ligands in the hormone receptor?
C-terminus
what site controls gene transcription in the hormone receptor?
N-terminus
what do non-hormone receptors do?
respond to lipid levels in the cell
examples of steroid hormone receptors?
sex hormone receptor
glucocorticoid receptor
vitamin D receptor
thyroid hormone receptor
retinoid receptor
examples of non-hormone receptors?
PPARgamma
LXR
SXR
how do non-hormone receptors monitor lipid levels?
control transcription of genes for cytochrome P450(inactivate lipids), intracellular lipid binding proteins(buffer and transport), and ATP binding cassette transporters( transport)
what cytosolic proteins contain SH2 domains?
PI3-kinase
PLC-gamma
GTPase-activating protein
what is the ligand for soluble guanylyl cyclases?
NO
what is the ligand for membrane-bound guanylyl cyclases?
ANF
what site binds ligands in the hormone receptor?
C-terminus
what site controls gene transcription in the hormone receptor?
N-terminus
what do non-hormone receptors do?
respond to lipid levels in the cell
examples of steroid hormone receptors?
sex hormone receptor
glucocorticoid receptor
vitamin D receptor
thyroid hormone receptor
retinoid receptor
examples of non-hormone receptors?
PPARgamma
LXR
SXR
how do non-hormone receptors monitor lipid levels?
control transcription of genes for cytochrome P450(inactivate lipids), intracellular lipid binding proteins(buffer and transport), and ATP binding cassette transporters( transport)
what segment of the voltage channel recognizes the ion?
P segment
where is the voltage sensor located?
cytosolic side
where are the recognition sites in ligand gated channels?
alpha subunits between alpha gamma and alpha delta
what do glucose carriers not transport?
sucrose and lactose(disaccharides)
what is the initial step of K+ transport into the cell?
dephosphorylation
where are Ca2+ ATPases located?
plasma membrane and ER
what transporters are driven by the Na+ gradient?
Na+-glucose symporter
Ca/Na antiporter
what is a common competitive antagonist for ligand-gated acetylcholine receptors?
curare
what is the mechanism of local anesthetic?
binding to phe and tyr residues of the Na channel in S6 of the fourth subunit
how do anti-arrhythmics function?
block open channels, reduce excitability
how do anti-epileptics work?
block inactivated channels, slows recovery rate, limits repetitive firing
what is used in heart failure?
cardiac glycosides(digitoxin)
bind to and block the Na/K ATPase
increase intracellular Ca
increase contraction
what is cochicine used for?
killing abnormally rapidly dividing cells by binding to tubulin and preventing microtubule formation
what is taxol used for?
binds to and stabilizes microtubules arresting cells in mitosis
what are benzimidazole derivatives used for?
binding to parasitic tubulin
what is cochicine used to treat?
gouty arthritis
inhibits leukocyte migration and release of inflammatory mediators