L topo/microtubule

Question 1

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

Answer 1

S

Question 2

thing highlighted red under drug resistance for topo 1 inhibitors *

Answer 2

glutathione s-transferase overexpression

Question 3

T or F:
Topotecan and Irinotecan are water soluble

Answer 3

True

Question 4

Topotecan class

Answer 4

topo 1 inhibitor

Question 5

Irinotecan class

Answer 5

topo 1 inhbitor

Question 6

dose limiting toxicity thing of irinotecan (not symptom)

Answer 6

UGT1A1

Question 7

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

A. G0/G1

B. S

C. G2

D. M

Answer 7

B

Question 8

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

Answer 8

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

Question 9

Main topo II inhibitor in class

Answer 9

Doxorubicin

Question 10

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

Answer 10

doxorubicin
daunorubicin
epirubicin
idarubicin

Question 11

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

Answer 11

False, more toxicity

Question 12

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

Answer 12

true, one of the more important aspects of the classs

Question 13

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

Answer 13

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

Question 14

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

Answer 14

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

Question 15

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

Answer 15

severe local tissue damage if extravasated

Question 16

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

Answer 16

dexrazoxane

Question 17

Cardiotoxicity of doxorubicin is believed to be caused by what?

Answer 17

iron-catalyzed free radical formation

Question 18

What class is etoposide?

Answer 18

Topo II inhibitor

Question 19

Cell cycle stage specificity of etoposide***

Answer 19

G2

Question 20

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

Answer 20

false. it does not intercalate **

Question 21

2 pumps that contribute to resistance of topo II inhibitors.

Answer 21

pGp and MRP

Question 22

bleomycin target(s)

Answer 22

Imidazole –
free radical
Thiazole -
intercalator

Question 23

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

Answer 23

G2 and M

Question 24

dose-limiting toxicity related to bleomycin

Answer 24

pulmonary (think blow)

Question 25

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

Answer 25

skin and lung

Question 26

T or F: bleomycin has rash side effects

Answer 26

true

Question 27

Prevent microtubule assembly: A. Vinca alkaloids B. Taxanes

Answer 27

A. Vinca alkaloids

Question 28

Prevent microtubule disassembly: A. Vinca alkaloids B. Taxanes

Answer 28

B. Taxanes

Question 29

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

Answer 29

True

Question 30

T or F: taxanes stabilize microtubules

Answer 30

true

Question 31

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

Answer 31

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

Question 32

T or F: vinca alkaloids destabilize microtubules

Answer 32

true

Question 33

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

Answer 33

false, large, need specific transporter

Question 34

what do vinca alkaloids bind to?

Answer 34

tubulin

Question 35

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

Answer 35

spindles mitotic arrest

Question 36

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

Answer 36

peripheral neuropathy / neurotoxicity

Question 37

Vincristine 2 main things listed under toxicity

Answer 37

extravasation causes severe inflammation neurotoxicity *

Question 38

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

Answer 38

true

Question 39

Eribulin is a what inhibitor

Answer 39

microtubule polymerization inhibitor

Question 40

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

Answer 40

true

Question 41

What does Paclitaxel do to microtubules?

Answer 41

stabilizes tf outta them bitches

Question 42

what do the taxane drugs end with?

Answer 42

-taxl

Question 43

what do taxanes bind to?

Answer 43

tubulin

Question 44

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

Answer 44

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

Question 45

Paclitaxel dose limiting toxicity thing

Answer 45

myelosuppression

Question 46

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

Answer 46

albumin

Question 47

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

Answer 47

binds to tubulin promotes tubulin polymerization and microtubule stabilization

Question 48

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

Answer 48

True

Question 49

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

Answer 49

true

Question 50

Which of the following microtubule inhibitors block the polymerization of tubulin? A. Paclitaxel B. Vincristine C. Ixabepilone

Answer 50

B