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45 Cards in this Set

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What are the chromosomal abnormalities associated with the philadelphia chromosome? and what does it cause?
Chr. 9 & 22
chronic myeloid leukemia
How do you treat CML?
interferon
What does imatinib do?
inhibitor of the BCR-Abl tyrosine kinase encoded by the philadelphia chromosome. Receptor assumes inactive conformation --> inactivation of kinase
Where does warfarin act?
the S enantiomer is 4x more potent than the R. Interacts with vitamin K epoxide reductase.
Describe induced fit
binding of a drug to its receptor changes its conformation
Describe the structure of nACHR
5 subunits
two alpha subunits that allow for ACh binding
What do local anesthetics do?
block the conductance of Na ions in neurons that transmit pain info
What do benzodiazepines do?
bind to GABA_A receptors and increase the conductance of Cl ions --> hyperpolarization
Describe the structure of a G-protein coupled receptor
7-transmembrane regions
1 polypeptide chain
each transmembrane region has a single alpha heli.
How does the G-protien coupled receptor look during the resting state? (on the cytoplasmic side of things)
noncovalently linked to a G protein made of alpha and beta-gamma subunits
Describe G protein dissciation
alpha subunit switches GDP for GTP.
a-GTP dissociates from the betagamma subunit
- a, or bg diffuse along the inner leaflet of the plasma membrane to interact with different effectors
How does the signaling stop?
inherent GTPase activity of the alpha subunit causes hydorlysis of GTP to GDP
What does G_s do?
- activates adenylyl cyclase
- activates Ca2+ channels
What does G_i do?
- inhibits adenylyl cyclase
- activates K+ channels
What does G_q do?
- activates phospholipase C
WHat does G_o do?
Inhibits Ca2+ channels (opposite of G_s)
B_1 adrenergic receptors
Control RH
B_2 adrenergic receptors
relax smooth muscle
B_3 adrenergic receptors
mobilize energy by fat cells
Where does the B1 receptor act?
1. SA node
2. Cardiac muscle
3. Adipose tissue
Where does the B2 receptor act?
1. bronchial and smooth m
2. GI smooth m
3. Uterus
4. Bladder
5. Liver
6. Pancreas
Where does the B3 receptor act?
Adipose tissue
What do tyrosine kinase receptors do?
phosphorylate tyrosine residues on the cytoplasmic tail of the receptor
--> recruits and tyrosine phosphoryltation of amny cytosolic signaling molecules
Name a famous tyrosine kinase receptor
Insulin
Where does insulin bind?
to the alpha subunits
What happens once the beta subunits in the insulin receptor transphosphorylate?
insulin receptor substrate (IRS) proteins are recruited
What are some main roles of tyrosine kinase receptors?
growth and differentiation
Describe tyrosine kinase-associated receptors
like tyrosine-kinase receptors, except they rely on nonreceptor kinases to phosphorylate target proteins
To what family to receptor serine/threonin kinases belong to?
TGF-beta receptor superfamily
Why ar eserine/threonin kinase receptors important
regulated cell grown and differentiation
- implicated in cancer progression
Describe Receptor Gyanylyl cyclases
have no G proteins. Ligand binding stimulates intrinsic receptor guanylyl cyclase activity
GTP --> cGMP
Name an important member of the receptor Guanylyl cyclase family
B-type natriuretic peptide
(secreted by ventricles in response to volume overload)
How do antimitotic vinca alkaloids act?
Diffuse through cellular membrane and target tubulin monomers to prevent polymerization
Arrests cells in metaphase
Define tachyphylaxis
drugs show diminishing effects over time
(receptor and cell become desensitized to drug)`
Define homologous desensitization
actions of agonists at only one class of receptors are lessened
Define heterologous desensitization
effects of agonists on a number of classes of receptors are coordinately diminished
how do you get heterologous desensitization?
drug-induced alteration in a common point of convergence in the mechanisms of action of the involved receptors
(e.g. a shared effector molecule)
How do you get receptor inactivation?
phosphorylation of the receptor completely blocks the signaling activity of the receptor
Define receptor downregulation
continual stimulation cuases endocytosis and sequestration of receptors.
Name one 'drug' that does not act with one of the four basic receptor types
mannitol. directly changes the osmolarity of the nephron
give a nother 'drug' that is unique
antacids. neutralize stomach pH
What does pravastatin do?
reduces cholesterol levels
Define K_d in terms of ligand concentration
the concentration of ligand at which 50% of all the available receptors are bound
What is a graded dose response relationship?
describes the effect of variosu doses of a drug on an individual
What is a quantal dose response relationship?
describes the effect of various doses of a drug on a population of individuals