Advanced Receptors Flashcards
What is an orthosteric binding site?
Main ligand binding site
What is an allosteric binding site?
An allosteric modulator binding site
what does Positive affinity modulation do?
Increases the potency of currently bound ligands
What does Negative affinity modulation do?
Decreases the potency of currently bound ligands
What does Positive efficacy modulation do?
Increase the potency and efficacy of bound ligands
What does Negative efficacy modulation do?
Decrease the potency and efficacy of bound ligands
What is biased agonism
different agonists produce different responses on the one receptor
Eg.
Gprotein biased agonist produces G protein pathways in preference to B arrestin pathway
What is internalization in terms of desensitization
The process of sequestering (removing) a receptor from the surface of the cell
What is Down regulation in terms of desensitization
Reduced production or higher degradation of surface receptors
What is Receptor Inactivation in terms of desensitization
Receptor that does not promote a signal even when ligand is bound
what is signalling protein inactivation in terms of desensitization
The inactivation of signalling proteins. even when stimulated by the receptor
What is mediator exhaustion in terms of desensitization
Excessive usage of molecule down the signal pathway
Eg. increase of metabolism when there’s not much glucose around
