Darmani- Pharmacodynamics Flashcards

1
Q

is a tertiary structure on that shares interactions with nearby amino acids?

A

no. they share interactions with distant amino acids

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2
Q

what is the agent that binds to a receptor?

A

agonist

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3
Q

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?

A

antagonist

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4
Q

in G-Protein receptors, where is the binding domain and where is the phosphorylation site?

A

binding-> near the N-terminal

phosphorylation-> C-terminal

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5
Q

in intracellular receptors in the N-domain still the binding domain?

A

no the C- domain is.

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6
Q

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?

A

chaperone

it dimerizes

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7
Q

in the G-protein, what subunit inactivates it?

A

the alpha subunit inactivates the GDP

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8
Q

what cascade do G-proteins activate?

A

target enzymes-> second messengers-> protein kinases-> effectors

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9
Q

what is it called when one GPCR couples to multiple G-proteins?

A

divergence coupling

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10
Q

do GIPs active GTPas activity by inhibiting G-protein function?

A

no they exert the opposite effects

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11
Q

calcium is a known to be a second messenger. what else does it do?

A

integrates signaling systems

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12
Q

what happens if you chronically deprive a receptor of excitation?

A

the receptors will up regulate and increase density. becoming more supersensitive

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13
Q

in homologous desensitization G-P-coupled receptor kinases (GRKs) phosphorylate what? and what happens to desensitzation?

A

only phosphorylates agonist occupid receptors.
initially minimal desensitization but then there is an increase in receptor affinity by arrestins leading to maximal desensitization

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