Darmani- Pharmacodynamics Flashcards
is a tertiary structure on that shares interactions with nearby amino acids?
no. they share interactions with distant amino acids
what is the agent that binds to a receptor?
agonist
if the allosteric site is bound by an agent and does not have an effect, what kind of agent is bound by the allosteric site?
antagonist
in G-Protein receptors, where is the binding domain and where is the phosphorylation site?
binding-> near the N-terminal
phosphorylation-> C-terminal
in intracellular receptors in the N-domain still the binding domain?
no the C- domain is.
during intracellular receptor binding a steroid is bound and brought into the cell. what carries the steroid to the nucleus? and what happens to the receptor in the nucleus?
chaperone
it dimerizes
in the G-protein, what subunit inactivates it?
the alpha subunit inactivates the GDP
what cascade do G-proteins activate?
target enzymes-> second messengers-> protein kinases-> effectors
what is it called when one GPCR couples to multiple G-proteins?
divergence coupling
do GIPs active GTPas activity by inhibiting G-protein function?
no they exert the opposite effects
calcium is a known to be a second messenger. what else does it do?
integrates signaling systems
what happens if you chronically deprive a receptor of excitation?
the receptors will up regulate and increase density. becoming more supersensitive
in homologous desensitization G-P-coupled receptor kinases (GRKs) phosphorylate what? and what happens to desensitzation?
only phosphorylates agonist occupid receptors.
initially minimal desensitization but then there is an increase in receptor affinity by arrestins leading to maximal desensitization