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IP 1 EXAM 2 > Biochemistry and Pharmacology > Flashcards

Biochemistry and Pharmacology Flashcards

1
Q

ligand

A

small molecule that influences receptor activity by binding directly to receptor protein at a specific site

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2
Q

constitutive

A

receptor activity that occurs in the absence of agonist binding

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3
Q

partial agonist

A

activate receptor, but are unable to produce the full effect of the endogenous ligand

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4
Q

antagonist

A

binds to receptor and prevents the endogenous ligand from activating the receptor

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5
Q

inverse agonist

A

ligands that abolish all activity

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6
Q

allosteric

A

binding site other than active site

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7
Q

selectivity

A

degree to which drug discriminates

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8
Q

specificity

A

degree to which receptor discriminates

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9
Q

activation energy

A

energy needed to overcome in order to progress in chemical reaction

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10
Q

transition state

A

unstable species that is intermediate between substrate and product

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11
Q

protein structure

A

tertiary structure with folds form binding sites

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12
Q

effect of changing conformation

A

distort site so that ligands no longer bind efficiently

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13
Q

active site

A

site at which ligand can activate the receptor to transmit a signal or inhibit the receptor to stop signal

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14
Q

transmembrane receptors

A

embedded in lipid bilayer of plasma membrane
cell-surface receptor
do not need to become internalized by cell

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15
Q

intracellular receptors

A

in cytoplasm or nucleus, or in membrane of extracellular compartment
must first get into cell

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16
Q

extracellular receptors

A

soluble, move freely about the body

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17
Q

endogenous

A

produced naturally

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18
Q

exogenous

A

produced outside of the body

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19
Q

Observations of receptor concept

A
  1. Receptor affinity determines dose of drug needed to produce effect, and the number of receptors defines maximal effect
  2. Receptors determine selectivity of a drug
  3. Receptors mediate pharmacologic actions of drug as agonist or antagonist
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20
Q

receptor occupancy

A

number of receptors bound to a ligand at any given time

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21
Q

competitive binding

A

drug competes with endogenous ligand for binding to a receptor

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22
Q

noncompetitive binding

A

ex. allosteric binding

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23
Q

irreversible binding

A

appears to be noncompetitive

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24
Q

association constant K

A

ratio of concentration of complex to the product of concentrations of the unbound drug and receptor

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25
Q

Low K

A

more dissociation

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26
Q

High K

A

more binding

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27
Q

High Kd

A

more dissociation

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28
Q

Low Kd

A

more binding

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29
Q

Kd

A

[D][R]

[DR]

30
Q

K

A

[DR]

[D][R]

31
Q

Kd or dissociation constant

A

ease with which drug dissociates from receptor binding site

32
Q

low Kd

A

high affinity to receptor

33
Q

receptor desensitization

A

tolerance to a drug occurs as a result of a decreased receptor response

34
Q

ways that receptors become desensitized

A

internalization

reversible covalent modification

35
Q

down regulation

A

hydrolyzed within lysosome

36
Q

up-regulation

A

promotes greater sensitivity to drugs or endogenous ligands that activate a receptor signaling pathway

37
Q

four general types of receptor pathways

A

G-protein coupled receptor
ion channel receptor
receptor tyrosine kinase
nuclear receptor

38
Q

GPCRs common mechanism

A

activate guanine nucleotide-binding proteins (G proteins)

39
Q

nucleotides are the building blocks of

A

RNA and DNA

40
Q

When GPCRs bind to agonist, stimulate G proteins to produce and bind what?

A 
guanosine diphosphate (GDP)
bind GTP
41
Q

Which form are G proteins active?

A

GTP-bound form

42
Q

Most G protein effectors are:

A

enzymes that produce soluble second messenger that carries on the signal initatied by GPCRs

43
Q

Some GPCRs are negatively coupled to adenylyl cyclase

A

activation of receptor turns on an inhibitory G protein that blocks adenylyl cyclase and decreases cAMP formation

44
Q

positively coupled

A

turn on stimulatory G protein and produce more cAMP

45
Q

ion channels

A

transmembrane, gated so conformational changes in receptor protein can open or close channel

46
Q

ligand vs. voltage

A

respond to binding of endogenous ligand vs. changes in membrane potential

47
Q

refractory period

A

time for resting potential of membrane to be restored, cannot be stimulated to open

48
Q

Receptor Tyrosine Kinases

A

transmembrane, regulatory receptors as well as enzymes

49
Q

kinase

A

enzyme facilitates transfer of single phospate from ATP to tyrosine amino acid residue

50
Q

autophosphorylation

A

RTKs attach phosphates to themselves

51
Q

nuclear receptors

A

intracellular receptors

52
Q

ex. of nuclear receptors

A

steroid receptors

53
Q

therapeutically important effects of nuclear receptor drugs and hormones

A

Produce effects only after lag period

Effects may continue for days

54
Q

Drug classes that interact with Adrenergic Receptor

A 
Autonomic
Alpha adrenergic agonists
Alpha adrenergic antagonists
Beta adrenergic agonists
Beta adrenergic antagonists
55
Q

Drug classes that interact with Cholinergic Receptor

A

Autonomic drugs
Cholinergic agonists
Cholinergic antagonists
Neuromuscular blockers

56
Q

Drug classes that interact with Dopaminergic

A

Dopamine agonists

Dopamine antagonist

57
Q

Drug classes that interact with Serotonergic

A

Serotonin agonists

Serotonin antagonists

58
Q

Drug classes that interact with Histaminic

A

Antihistamines

59
Q

Drug classes that interact with Opioid

A

Opioid agonists and antagonists

60
Q

Michaelis constant Km

A

concentration of substrate necessary to achieve half of maximal velocity

61
Q

two main types of cofactors that participate in enzymatic reactions:

A

Coenzymes

Prosthetic groups

62
Q

coenzymes

A

held loosely by enzyme and may be released easily

63
Q

prosthetic groups

A

tightly (covalently bound) cofactors

64
Q

Drug enzyme interactions

A 
competitive (drug blocks substrate access)
non competitive (lower activation energy by binding to allosteric site)
65
Q

competitive inhibitors shift plot of reaction velocity

A

increase Km; Vmax same

66
Q

noncompetitive and irreversible effect on Vmax

A

change apparent Vmax; not affect Km

67
Q

six major classes of enzymes

A 
oxidoreductases
transfereases
hydrolases
lyases
isomerases
ligases
68
Q

oxidoreductase

A

oxidize substrates by transferring an electron to an electron accepting cofactor

69
Q

example of oxidoreductase

A

ALDH - chemical oxidation of acetaldehyde to acetic acid after consuming alcohol

70
Q

transferases

A

transfer of phosphate group from ATP to amino acid residue by kinases

71
Q

hydrolases

A

split larger molecules into smaller ones, using a molecule of H2O

IP 1 EXAM 2 (3 decks)

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