Exam (elaborations)
GMS6504 Binding Modes Exam Questions And Correct Answers
- Course
- Institution
GMS6504 Binding Modes Exam Questions And Correct Answers...
[Show more]
Content preview
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
The benefits of buying summaries with Stuvia:
Guaranteed quality through customer reviews
Stuvia customers have reviewed more than 700,000 summaries. This how you know that you are buying the best documents.
Quick and easy check-out
You can quickly pay through credit card or Stuvia-credit for the summaries. There is no membership needed.
Focus on what matters
Your fellow students write the study notes themselves, which is why the documents are always reliable and up-to-date. This ensures you quickly get to the core!
Frequently asked questions
What do I get when I buy this document?
You get a PDF, available immediately after your purchase. The purchased document is accessible anytime, anywhere and indefinitely through your profile.
Satisfaction guarantee: how does it work?
Our satisfaction guarantee ensures that you always find a study document that suits you well. You fill out a form, and our customer service team takes care of the rest.
Who am I buying these notes from?
Stuvia is a marketplace, so you are not buying this document from us, but from seller Easton. Stuvia facilitates payment to the seller.
Will I be stuck with a subscription?
No, you only buy these notes for $9.99. You're not tied to anything after your purchase.
Can Stuvia be trusted?
4.6 stars on Google & Trustpilot (+1000 reviews)
78834 documents were sold in the last 30 days
Founded in 2010, the go-to place to buy study notes for 14 years now