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