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145 Cards in this Set

  • Front
  • Back
what are two biogenic amines
epinepherine
norepinephrine
what are the binding properties of receptors
saturability
affinity
specificity
what is Ka equal to
1/Kd (association constant)
is a specific binding curve able to be to show saturablilty
yes
is a non specific binding curve able to show saturabiliy
no
what is a scatcher plot
enable us to plot binding ina linear form to get the total # of binding site/the dissassocition constant
In a scatcher plot what corresponds to the Y and X intercepts
Y=bound/free (hormones)
X=Bmax (R+RL)
what are 5 ways that signal transmission is accompilished
gene activation
opening of ion channels by linked receptr
enzymatic activity
ligand-stimulated autophosporylation
activation of a specific G protein
how does a gated ion channel work
opens or closes in response to intracellular or extracellular signal ligand concentration or membrane potential
what is an example of a receptor enzyme
protein tyrosine kinase
how does receptor enzymes work
ligand binds to the extracellular domain and stimulates intracellular enzymatic activity
what is the general process of how a serpentine receptor works
ligand binds receptor
receptor activates intracellular GTP-binding protein (G)
G regulates and enzyme that generates second messengers
what are 3 ways that desensitization is accomplished
1. reduction in receptor #
2. localization of receptors at the cell sur
3. efficiency of the signal transmission

generally all specific for agonists
what is adaptation
the ability of signal systems to adjust to response to different levels of signals
how does an agonist inhibit a signal response
by blocking the binding of the agonist
T or F receptor activation triggers a feedback circuit that shuts off the receptor or removes it from the cell surface
T
T or F signal amplification is and aspect of signaling systems
T
what is integration (cross talk)
signals can oppose each other or reinforce each other. this can take place at multiple steps
what are four ways that ion channels are regulated
ligand gated channels
voltage-gated channels
mechanically gated channels
covanlent modification
what causes cystic fibrosis
the CL- channels have been mutated which affect the ability of them to be regulated by covalent modification
what type of transport is involved in channels
passive transport.

all the regulation of the channels disscussed work by passive diffusion down their electrochemical gradients
what ions does acetylcholine dependent gated protein allow
Ca+, Na+ or K+
in acetylcholine-dependent opening of gated proteins what happens when acetylcholine binds
a rotation of bound alpha helices to place polar aspect in the interior of the protein to facilitate Ca+, Na+ or K+
what is tertodotoxin
a neuro toxin that targets ion channels from japanese puffer fish
targets voltage-gated Na+channels
what is saxitoxin
a neuro toxin that targets ion channels
from red tide
targets voltage-gated Na+ channels
what is Alpha-bungarotoxin
a neuro toxin that targets ion channels
venom from a banded krait snake that inhibits the nicotinic acetylcholine receptor
dendrotoxin
a neuro toxin that targets ion channels from mamba snakes that block neuronal voltage dependent K+ channels
what do spider venom toxins inhibit
calcium channels or sodium potassium channels
what are conotoxins
a neuro toxin that targets ion channels from cone snails, most selective of all inhibitors, can select for voltage sensitive sodium, calcium or potassium channels and ligand-gated channels

these are being studied as starting materials for new drugs
what are three channel specific drugs
local anesthetics, anticonvulsants, and antiarrhythmics
what is the most common type of enzyme activity found intrinsic to a transmembrane receptor
Protein Tyrosine Kinase
what types of signaling use PTK's
growth factors
insulin
cytokines (interferons and interleukins)
are receptors for PTK's single pass transmembrane proteins or multiple pass
single pass with ligand binding domain in the extracellular surface
what is unusual about the insulin receptor binding and protein tyrosine kinases domains
once the insulin ligand binds two dimers (heterodimers) for a tetrameric complex via disulfide bonds
what a kinase insert region
an important site for autophosphorylation and protein-protein interacitons
in receptor tyrosine kinases where are the aminoterminal and carboxytermial domains located
aminoterminal=extracellular
carboxyterminal=intracellular
what type of site is created by autophosphorylation
phosphotyrosine site for binding of the SH2 protein
autophosphorylation can take place in two spots what are they
cytoplamic domain (growth factors/insulin)
the PTK receptor (cytokine receptor)
what differs among effector proteins
the differ in the the SH2 structure which effect which specific tyrosine phosphate sites it reacts with
recruitment of effector proteins propogates the GF signal by which two ways
1. facillatating the binding of the effector protein to the its binding partner

2. facilitating phosphorylation of tyrosine with its accompanied activation of PTK
what two hormones regulate cell proliferation
insulin
growth factor
what is a Ras protein
a monomeric guanyl nuclotide-binding protein (G-protein) that activate the MAP kinase cascade which changes gene expression
in the major proliferative response involves what protein
the ras protein
what is SOS
a guanine-nucleotide exchange factor for Ras (in ras this stimulate the exchange of GDP for GTP (active))
between what two proteins does phosporylated tyrosine bind
Grb2 and SH2
what is the most common type of enzyme activity found intrinsic to a transmembrane receptor
Protein Tyrosine Kinase
what types of signaling use PTK's
growth factors
insulin
cytokines (interferons and interleukins)
are receptors for PTK's single pass transmembrane proteins or multiple pass
single pass with ligand binding domain in the extracellular surface
what is unusual about the insulin receptor binding and protein tyrosine kinases domains
once the insulin ligand binds two dimers (heterodimers) for a tetrameric complex via disulfide bonds
what a kinase insert region
an important site for autophosphorylation and protein-protein interacitons
in receptor tyrosine kinases where are the aminoterminal and carboxytermial domains located
aminoterminal=extracellular
carboxyterminal=intracellular
what type of site is created by autophosphorylation
phosphotyrosine site for binding of the SH2 protein
autophosphorylation can take place in two spots what are they
cytoplamic domain (growth factors/insulin)
the PTK receptor (cytokine receptor)
what differs among effector proteins
the differ in the the SH2 structure which effect which specific tyrosine phosphate sites it reacts with
recruitment of effector proteins propogates the GF signal by which two ways
1. facillatating the binding of the effector protein to the its binding partner

2. facilitating phosphorylation of tyrosine with its accompanied activation of PTK
what two hormones regulate cell proliferation
insulin
growth factor
what is a Ras protein
a monomeric guanyl nuclotide-binding protein (G-protein) that activate the MAP kinase cascade which changes gene expression
in the major proliferative response involves what protein
the ras protein
what is SOS
a guanine-nucleotide exchange factor for Ras (in ras this stimulate the exchange of GDP for GTP (active))
between what two proteins does phosporylated tyrosine bind
Grb2 (and SH2 containing adaptor protein)

SOS
what does and activated Ras do
it binds and activates Raf-1

Ser/Thr selective protein kinase
what does Raf-1 do
it activates MEK
what does MEK do
it activates ERK
what does ERK do
it phosoporylates proteins such as important transcription factors like pp90(kinase that phosporylates S6)
how is Ras's function in cancer patients
highly mutated
how is phosphatidylinositol 3-kinase activated
2 ways
growth factor receptors

IRS-1
what does PI3-K generate
3,4,5 phosphatidylinositol PIP3 from PIP2
what is a Plekstrin homology domain (PH domain0
a region of protein that binds phosphoinositides and Beta/gamma units of G proteins as well protein kinase C
where does PIP3 interact with proteins
the PH domain
what is attacked to the PIP3
PKB protein kinase B
what does PTEN do and one what molecule does it act
terminates the signaling pathway
acts on PIP3 to change it back to PIP
what is central to insulins effects on metabolism
PI3/PKB pathway
what C is targeted by the PI-3K
C3
phosphorylation here changes PIP2 to PIP3
what does PDK-1 do
phosporylates the PKB that is attached to PIP3
does what does activated PKB activate
GSK3

phosporylated form is the inactive form
the active form causes inhibition
what does and activated Ras do
it binds and activates Raf-1

Ser/Thr selective protein kinase
what does Raf-1 do
it activates MEK
what does MEK do
it activates ERK
what does ERK do
it phosoporylates proteins such as important transcription factors like pp90(kinase that phosporylates S6)
how is Ras's function in cancer patients
highly mutated
how is phosphatidylinositol 3-kinase activated
2 ways
growth factor receptors

IRS-1
what does PI3-K generate
3,4,5 phosphatidylinositol PIP3 from PIP2
what is a Plekstrin homology domain (PH domain0
a region of protein that binds phosphoinositides and Beta/gamma units of G proteins as well protein kinase C
where does PIP3 interact with proteins
the PH domain
what is attacked to the PIP3
PKB protein kinase B
what does PTEN do and one what molecule does it act
terminates the signaling pathway
acts on PIP3 to change it back to PIP
what is central to insulins effects on metabolism
PI3/PKB pathway
what C is targeted by the PI-3K
C3
phosphorylation here changes PIP2 to PIP3
what does PDK-1 do
phosporylates the PKB that is attached to PIP3
does what does activated PKB activate
GSK3

phosporylated form is the inactive form
the active for phophorylates glycogens synthase to inactive form
what does active GSK3 phosphorylate
Glycogen syntase

when this is phosphorylated it is inactive
what molecule stimulates GLUT4 to the plasma membrane
PKB
what is herceptin
a monoclonal antibody against Her2
what is Her2 involved in
breast cancer
what is Gleevec
drug that selects against tyrosine kinases in leukemia patients and GI tumors
what two drugs have been approved for use in colon rectal cancers
Erbitux
Avastin
how are JAK activated
by trans autophosphorylation
what happens when cytokines bind to receptors that have little cytoplamic domains
triggers a stepwise association with the subunits B1 and B2 to the receptor
what comes along with the Beta 1 and 2 subunits
JAK molecule
what does JAK do?
stimulates tyrosine phosphorylation of components of STAT transcription factors
what is STAT
transcription factors that JAK acts on, which are then translocated to the nucleus for gene regulation
what happens to STAT after phosphorylation but before it enters the nucleus
becomes dimerized
what does cholera toxin effect
the G protein
what does the G protein do
activates adenylyl cyclase
what does adenylyl cyclase do
catalyzes the reaction of ATP to Camp
what are the 3 fates of Camp
1. exported out of the cell
2. changed to 5'-AMP (cyclic amp phosphoidesterase)
3. changes PKA to an active form
what does active PKA do
phosphorylates ser/threonine resisdues in many structure in the cell
what characterizes a G protein
the alpha subunit
what do methyl xanthines do
they inhibit cyclic amp phosphodiesterases
T or F the cyclic AMP response pathway is not reversable at all
F

reversable at all levels
what is the purpose of having multiple steps in the cyclic AMp pathway
allows for amplification and cross talk with other pathways
what is the response to TSH
thyroid hormone synthesis and secretion
what is the response to ACTH
cortisol synthesis and secretion
what is the response to LH
progesterone secretion
what is the response to adrenaline in the muscle
glycogen breakdown
what is the response to adrenaline in the heart
increase in heart rate and force of contraction
what is the response to adrenaline, ACTH, glucagon, TSH in fat
triacylglyceride breakdown
what is the response to glucagon
glycogen breakdown
what is the response to PTH
bone resorption
what is the response to vasopression
water resorption
what does inderal and propranalol do
beta blockers (antagonist that prevent binding of adrenaline)
what are Beta blockers such as inderal and propranalol used for
treatment of hypertension, migraines and some cardiac problems

some performers use them for stage fright
what has a higer affinity value for B-catecholamine receptor antagonist or agonists
antagonist is way higher
what stimulates the exchange of GDP for GTP in a G protein
binding of the ligand to the receptor
what happens to the trimeric G protein when GTP is bound
GTP causes a dissassociation of the A subunit
the A subunit bound with GTP is the active G protein
what causes the hydrolyzation of GTP on the Alpha sub unit of the G protein
intrinsic GTPase of the Alpha subunit
what is the subunit that the cholera toxin targets in the G protein
the alpha subunit which specifically attacks the intrinsic GTPase so the signal stay on!
what happens in the intestines when cholera toxin has done its worst
Camp dependent activation of CL- channels leads to secretion of sodium and water
how does C-amp activate PKA
by disinhibition of the R subunits blocking the PKA binding sites
why does PKA have two sites for binding
two site will give a stepper response curve
what are some important agonist in the Phosphotidyllinositol turnover signaling pathway
acetylcholine
histamine
vasopression
angiotensin
platlet-derived growth factor
what activates the Phosphotidylinositol turnover signaling pathway
hormone receptor complex that activates phospholipase C
what does phospholipase C do
takes phosphotidlinositol 4,5 bisphosphate and adds H2o and separates them to yeild
diacylglycerol
inositol 1,4,5-triphosphate
what directly activates phospholipase C
activated G protein
activated growth factor receptor
what activates protein kinase C
diacylglycerol
what causes a release of Ca+ from the ER in the turnover signaling pathway
inositol 1,4,5 triphosphate
after PLC cleaves off diacylglycerol and IP3 what is the destination of these two molecules
diacylglycerol=stays in the membrane
IP3= is soluble and head to the nucleus
what further degrades diacylglycerol in the the turnover pathway
phospholipases A1/A2
what is an alternative to further degredation of diacylglycerol besides the Phospholipase A1/A2
conversion to phosphatidic acid by phosphorylation
what molecule is able to mimic diacylglycerol in the activation of protein kinase C
Phorbol ester tumor promoters

these are metabollically stable
what bond does Phospholipase A1 cleave in phosphotidylinositol
the bond ester bond at carbon 1 right next to the fatty acid chain
what bond does Phospholipase A2 cleave in phosphotidylinositol
the bond ester bond at carbon 2 right next to the fatty acid chain
what bond does Phospholipase C cleave in phosphotidylinositol
the bond phosphodiester bond at carbon 3 right inbetween the O and P
what bond does Phospholipase D cleave
the bond in between the P and the O on the side of the head group
when C2 is esterified with arachidonic acid in phophatidylinositol the molecule becomes a precursor for what
Eicosanoids