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GMS6504 Binding Modes Exam Questions And Correct Answers
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GMS6504 Binding Modes Exam Questions AndCorrect Answers
orthosteric antagonist
-antagonist that binds to the SAME location as the agonist
antagonist properties
-saturable = if you add enough antagonist eventually you get to the point where adding
no more antagonist causes extra antagonism (limit to how much inhibition you can
achieve)
-surmountable = add enough agonist, you can overcome antagonist (reach 100%
response)
antagonist binding assay
-incubate receptor with KNOWN agonist = traceable
-wash out excess agonist
-add antagonist
antagonist response assay
-obtain dose response for agonist
-repeat in presence of increasing antagonist concentrations
dose ratio
-measure of how much effect antagonist has on response
pA2
-concentration of antagonist required to give a dose ratio of 2
-allows us to compare antagonists
A more potent antagonist will have a ___________ pA2
-LOWER
schild analysis
, -draw conclusions about antagonist interaction with receptor
inverse agonists
-binds to agonist binding site and decreases response (constitutive activity)
-response decreased over time
partial agonists
-bind to and partial stimulate receptors
-more effective with high receptor density?
non-competitive antagonists
-bind irreversibly to receptors
-as more antagonist added, graph shifts down and 100% response no longer reached
allosteric modulation
-antagonist binds to a different site than the agonist
-causes conformational change
-changes affinity of agonist for the protein
-allosteric site is below
T/F: allosteric antagonists tend to have fewer side effects than orthosteric antagonists
True
reduced side effects
-orthosteric antagonists bind the agonist binding site
-many endogenous receptors for each endogenous ligand = evolutionarily similar binding
sites and antagonist inhibits multiple enzymes
-allosteric modulators bind to more unique sites
-can potentiate natural responses (i.e Alzheimer's)
control of conformation
-receptors are constantly changing shape
-allosteric modulator acts like a doorstop to keep in one particular conformation =
whichever conformation the modulator binds to strongly
Incomplete inhibition
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