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PHRM 864 > L topo/microtubule > Flashcards

L topo/microtubule Flashcards

1
Q

Cells in __ phase are most sensitive to topo 1 induced cleavage *

A

S

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2
Q

thing highlighted red under drug resistance for topo 1 inhibitors *

A

glutathione s-transferase overexpression

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3
Q

T or F:
Topotecan and Irinotecan are water soluble

A

True

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4
Q

Topotecan class

A

topo 1 inhibitor

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5
Q

Irinotecan class

A

topo 1 inhbitor

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6
Q

dose limiting toxicity thing of irinotecan (not symptom)

A

UGT1A1

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7
Q

Topoisomerase I inhibitors primarily halt cells in which phase of the cell cycle?

A. G0/G1

B. S

C. G2

D. M

A

B

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8
Q

Many compounds inhibit topo II, but only ones that produce what are cancer therapies

A

double stranded DNA breaks, (does this not just make sense for everything)

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9
Q

Main topo II inhibitor in class

A

Doxorubicin

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10
Q

Example of anthracyclines (topo II inhibitors) (just try)

A

doxorubicin
daunorubicin
epirubicin
idarubicin

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11
Q

T or F:
Since topo II inhibitors act as intercalators, they are much less toxic than other therapies

A

False, more toxicity

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12
Q

T or F:
Topo II inhibitors release free radicals that can cause dna damage

A

true, one of the more important aspects of the classs

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13
Q

what do the free radicals from topo II inhibitors do to us that is highlighted red and super important? *

A

cause cardiotoxicity since heart tissue ahs low levels of enzymes that neutralize free radicals

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14
Q

T or F:
Topo II inhibitors act during G2/M and are cell cycle dependent

A

False, they do have activity there but they are considered non-cell cycle dependent

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15
Q

What is another toxicity that doxorubicin has that isnt cardio related? (also highlighted in red) *

A

severe local tissue damage if extravasated

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16
Q

what drug is given in combo with doxorubicin to mediate toxicity (specifically cardio) *

A

dexrazoxane

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17
Q

Cardiotoxicity of doxorubicin is believed to be caused by what?

A

iron-catalyzed free radical formation

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18
Q

What class is etoposide?

A

Topo II inhibitor

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19
Q

Cell cycle stage specificity of etoposide***

A

G2

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20
Q

T or F:
Etoposide inhibits re-ligation of double strand breaks induced by topo II and intercalates like doxorubicin

A

false. it does not intercalate **

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21
Q

2 pumps that contribute to resistance of topo II inhibitors.

A

pGp and MRP

22
Q

bleomycin target(s)

A

Imidazole –
free radical
Thiazole -
intercalator

23
Q

Bleomycin has its greatest effect on cells in the __ and __ phases of the cell cycle

A

G2 and M

24
Q

dose-limiting toxicity related to bleomycin

A

pulmonary (think blow)

25
Q

bleomycin is inactivated by bleomycin aminohydrolase, which is in high concentrations everywhere but _____ and _____

A

skin and lung

26
Q

T or F:
bleomycin has rash side effects

A

true

27
Q

Prevent microtubule assembly:
A. Vinca alkaloids
B. Taxanes

A

A. Vinca alkaloids

28
Q

Prevent microtubule disassembly:
A. Vinca alkaloids
B. Taxanes

A

B. Taxanes

29
Q

T or F:
Cells treated with vinca alkaloids cannot build up any microtubules

A

True

30
Q

T or F:
taxanes stabilize microtubules

A

true

31
Q

T or F:
Taxanes stabilizing microtubules is good because we want cellular stability

A

false, dynamic instability is important for microtubules to find their chromosomes

32
Q

T or F:
vinca alkaloids destabilize microtubules

A

true

33
Q

T or F:
vinca alkaloids are small molecules that get into cells with ease

A

false, large, need specific transporter

34
Q

what do vinca alkaloids bind to?

A

tubulin

35
Q

vinca alkaloids binding to tubulin leads to no attachment of microtubules to the _______ which is called what?

A

spindles
mitotic arrest

36
Q

microtubules are critical to nerve cell axon function, therefore a toxicity of vinca alkaloids would be what?

A

peripheral neuropathy / neurotoxicity

37
Q

Vincristine 2 main things listed under toxicity

A

extravasation causes severe inflammation

neurotoxicity *

38
Q

T or F:
The neurotoxicity from vinca alkaloids is dose dependent

A

true

39
Q

Eribulin is a what inhibitor

A

microtubule polymerization inhibitor

40
Q

T or F:
Eribulin has a lower rate of toxicity than other microtubule inhibitor drugs *

A

true

41
Q

What does Paclitaxel do to microtubules?

A

stabilizes tf outta them bitches

42
Q

what do the taxane drugs end with?

A

-taxl

43
Q

what do taxanes bind to?

A

tubulin

44
Q

what is the main thing that leads to mitotic arrest when discussing taxanes?

A

stabilizing the microtubules -> block depolymerization and segregation of sister chromatids

45
Q

Paclitaxel dose limiting toxicity thing

A

myelosuppression

46
Q

what is paclitaxel linked to to increase solubility and circulation time of the drug

A

albumin

47
Q

Wtf is an epothilone (ixabepilone) and what does does it bind to / do

A

binds to tubulin
promotes tubulin polymerization and microtubule stabilization

48
Q

T or F:
Epothilones (ixabepilone) are not cross-resistant with taxanes

A

True

49
Q

T or F:
Epothilones (ixabepilone) is a poor PGP substrate

A

true

50
Q

Which of the following microtubule inhibitors block the polymerization of tubulin?

A. Paclitaxel

B. Vincristine

C. Ixabepilone

A

B

PHRM 864 (22 decks)

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