Term
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Definition
Dissociation Constant. It's equal to ([receptor][hormone])/[receptor-hormone] where 1/2 of the receptors are bound by hormone. (or where the concentration of [H] = [H-R] |
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Term
Steroid Hormone
How reach receptor? Where?
R-H binds what?
Function?
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Definition
Diffuse across Plasma Membrane.
Binds receptor in cytoplasm.
H-R binds response elements in promoter & enhancers of genes.
Get transcription. |
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Term
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Definition
thyroid hormones
retinoic acid (Vit A)
Calcitriol (Vit B)
steroid hormones |
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Term
Nicotinic Acetylcholine receptor.
where found.
function? |
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Definition
Neuromuscular Junction
Ion channel |
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Term
Ligand Gated Ion Channel
fast / slow effect?
open / closed at rest?
2 types? |
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Definition
Fast effects of NT's
Closed @ rest
open when NT binds
2 types - Na channel - depolarize membrane
Cl & K channel hyperpolarize membrane |
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Term
Gaba A receptor.
where?
function? |
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Definition
in brain
chloride channel (inhibitor) |
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Term
synthesis of cyclic AMP
degradation? |
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Definition
ATP - acdenylate cyclase -> cyclic AMP (cleave 2 phosphate groups & attach oxygen of last one to the #3 carbon on ribose sugar.
Degraded by cyclic AMP phosphodiesterase to AMP. |
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Term
G-Protein
binding site?
subunits?
function? |
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Definition
Guanine binding site
3 subunits α, β & γ (last two are membrane bound)
α subunit function to activate adenylyl cyclase. |
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Term
cyclic AMP signal cascade |
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Definition
cyclic AMP activate PKA by attaching to regulatory subunits to dissociate from PKA.
activated PKA catalytic subunit activates CREB by phosphorylation
(CREB - cyclic AMP response binding element)
CREB = transcription factor |
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Term
mechanism of inhibiting adenylate cyclase |
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Definition
G-Protein has a different αi-subunit that inhibits adenylate cyclase |
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Term
cAMP action on liver
hormone? |
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Definition
hormone = glucagon
glycogen breakdown |
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Term
cAMP action in adipose tissue.
hormone?
what receptor? |
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Definition
hormone = epinephrine
on β-receptor
cause Fat breakdown |
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Term
cAMP action on bronchial & vascular smooth muscle
hormone?
receptor?
action? |
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Definition
relaxation
β-receptor
epinephrine |
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Term
cAMP action on thyroid gland
hormone?
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Definition
proliferation / hormone synthesis
TSH = hormone |
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Term
cAMP action on adrenal cortex
hormone? |
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Definition
proliferation / hormone synthesis
ACTH |
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Term
cAMP action on melanocytes
hormone? |
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Definition
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Term
cAMP action on intestine
hormone |
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Definition
Diarrhea
pancreatic polypeptide |
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Term
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Definition
water retention
vasopressin |
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Term
inhibition of cAMP in intestine cause?
hormone? |
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Definition
constipation
opioid peptides |
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Term
inhibition of cAMP in brain response?
3 diff hormones? |
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Definition
opioid peptides - analgesia
epinephrine (α-2 receptor) hypotension
dopamine - euphoria |
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Term
inhibition of cAMP on pituitary gland response?
hormone?
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Definition
inhibition of growth hormone GH excretion
somatostatin |
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Term
inhibition of cAMP on melanocytes response?
hormone? |
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Definition
inhibition of melanin synthesis
melatonin |
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Term
Pseudohypoparathyroidism
normal PTH function
cause of disease?
symptoms? |
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Definition
PTH normally raises blood Ca level by raising cAMP
disease caused by mutation in PTH receptor
pt has hypocalcemia, tetany |
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Term
Toxic thyroid nodules
3 causes? |
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Definition
hyperthyroidism
tumors in thyroid gland - overproduction of hormones.
caused by either mutation in TSH receptor. (TSH is the thyroid stimulating hormone from pituitary gland)
or a mutated Gs protein that keeps G-protein active by blocking the GTPase activity |
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Term
Cholera Toxin
effect in intestines?
also pertussis toxin in respiratory tract. |
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Definition
bacterial infection in intestine
it enters cells, modify α-subunit of Gs protein thus no more GTPase activity leaving it in permanently active state. |
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Term
mechanism of DAG (diacylglycerol) & IP3 as second msngrs |
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Definition
signal -> G-protein linked receptor
activated G-protein α-subunit activate phospholipaseC
this cleaves IP3 from diacylglycerol
IP3 trigger Ca release from ER |
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Term
smooth muscle contraction mech |
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Definition
Ca add to Calmodulin
which active MLC-Kinase (myosin light chain) by phosphorilation
get contraction. |
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Term
3 ways to elevate cytoplasmic Ca |
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Definition
hormones acting on G-protein & IP3
ligand-gated Ca channel (NMDA receptor in brain)
voltage-gated channel |
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Term
3 intracellular Ca receptors |
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Definition
protein kinase C
calmodulin
troponin C |
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Term
calcium action & hormone in pancreas |
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Definition
acetylcholine - enzyme secretion |
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Term
calcium action & hormone in mast cells |
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Definition
antigens - histamine secretion |
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Term
calcium action & hormone in bronchial smooth muscle |
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Definition
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Term
calcium action & 3 hormones in vascular smooth muscle |
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Definition
epinephrine (a1 receptors) - contraction vasopressin & angiotensin (IP3 system) - contraction |
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Term
calcium action & hormone in liver |
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Definition
vasopressin - glycogen breakdown |
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Term
calcium action & hormone in platelets |
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Definition
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Term
calcium action & hormone in endothelial cells |
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Definition
bradykinnin/histamine/Ach - NO synthesis |
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Term
cGMP affect in smooth muscle, 2 hormones |
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Definition
ANF (atrial natriuretic factor) & Nitric Oxide (NO) relaxes muscle. |
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Term
PDE5 inhibitor mech in smooth muscle |
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Definition
inhibit cGMP-specific phosphodiesterase - used in Viagra |
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Term
ANF (atrial natrouretic factor), it's receptor type? what's it's function? |
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Definition
receptor = ligand-activated guanylate cyclase. It makes cGMP which stimulates Protein kinase C which phosphorylates proteins |
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Term
when is ANF released by the heart? what two organ systems does it work on? |
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Definition
released when BP is to high cuz too much Na around. Kidney - incr Na excretion Relax bloodvessels & vascular smooth muscles |
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Term
2 methods of regulating guanylate cyclase |
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Definition
1. membrane bound guanylate cyclase is activated by hormones 2. cytoplasmic guanylate cyclase is activated by nictric oxide (NO) |
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Term
Affect of Ca in endothelial cells |
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Definition
initiate Argenine to donate a nitrogen to make NO NO diffuse through to smooth muscle & cause conversion of GTP to cGMP and get relaxation |
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Term
affect of Ca in vascular smooth muscle |
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Definition
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Term
growth factor receptors
mechanism? |
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Definition
receptor oligomerizes
receptor autophophorylates
signal protein w/ SH2 domain bind
signal protein -> activated allosterically
or tyrosine -> phosphorylated |
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Term
insulin receptor
similar to what receptor?
what 2 differences to that receptor? |
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Definition
similar to growth factor receptors
diff: unstimulated receptor is a disulfide-bonded tetramer
most effects are mediated by IRS1 & 2
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Term
growth factor receptor activation of IP3 system
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Definition
Phospholipase C-γ catalize PIP3 to IP3
IP3 -> Ca release from ER |
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Term
growth factor receptor activation of protein kinase B |
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Definition
autophosporylated receptor activates
Phosphoionositide-3-kinase (lipid kinase) convert PIP2 to PIP3
which activates PKB (protein kinase B or AKT) |
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Term
growth factor receptor activating MAP kinases |
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Definition
autophosphorylated receptor
activate RAS (a small G-protein)
which initiate phosphorylation cascade
which activates MAP kinase (mitogen-activated protein kinase) |
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Term
desensitization of beta-adrenergic receptors |
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Definition
receptor phosphorylated by BARK/PKA thus becomes inactive
arrestin binds it
gets pulled in from cell membrane to go to lysosome
BARK = (β-adrenergic receptor kinase)
PKA = Protein kinase A |
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