L7 Antimetabolites Flashcards
Which of the following drugs targets Her2?
A. Sirolimus
B. Alectinib
C. Vemurafinib
D. Tucatinib
D
Which of the following drugs targets a kinase that is produced by formation of the Philadelphia chromosome?
A. Alectinib
B. Gefitinib
C. Imatinib
D. binimetinib
C
Which compound below is not a covalent kinase inhibitor?
A. Gefitinib B. Osimertinib C. Afatinib D. Acalabrutinib
A
Which type of kinase inhibitor can bind in the ATP binding site and stabilize the inactive confirmation of a kinase?
A. Type I B. Type II C. Type III D. Type IV
B
T or F:
Antimetabolites are typically analogs of naturally occurring metabolites
true
T or F:
most antimetabolites require biotransformation to a nucleotide analog to be active
true
what are the 2 ways pyrimidine analogs can interfere with metabolism?
interfere with pyrimidine synthesis
inhibit DNA polymerase
what is the fluorinated uracil analog?
5-fluorouracil (5-FU)
what is the significance of 5-FU being converted into fDUMP or fUTP?
5-FU has a short half life in plasma, the others get into the cell and persist
in the presence of folates, __________ _________ synthesizes thymidine monophosphate (TMP) from dUMP ***
thymidylate synthase
T or F:
upregulation of thymidylate synthase contributes to 5-FU resistance
True
what is the enzyme that breaks down 5-FU?
dihydropyrimidine dehydrogenase (DPD)
what is the “rescue” for 5-FU overdose?
thymidine
what is the connection between 5-FU and leucovorate?
leucovorate is a folate cofactor that is converted to tetrahydrofolate in cells, higher levels of tetrahydrofolate increases the efficacy of 5-FU
what do the cytosine analogs primarily inhibit?
DNA synthesis
what class is cytarabine?
cytosine analog
Cytarabine gets converted to ______ intracellularly
Ara-CTP
what is Ara-CTP
the thing cytarabine gets converted into, it is a competitive inhibitor of DNA polymerase alpha
what converts cytarabine into non-toxic uracil arabinoside?
cytidine deaminase
T or F:
Increased levels of cytidine deaminase in the CNS makes Ara-C highly toxic
False, decreased levels
what class is gemcitabine
cytosine analog
T or F:
Cytarabine is more potent than the other cytosine analog Gemcitabine
false, gem is more
what does tetrahydrouridine inhibit?
cytidine deaminase (CDA)
T or F:
Cytarabine is inactivated by cytidine deaminase
True
Tetrahydrouridine is given with _____ to increase efficacy and decrease resistance
cytarabine
Nucleoside analog:
A. 5-FU
B. Cytarabine
A. 5-FU
6-MP is a _____ analog
purine
6-MP inhibits multiple enzymes in the __________________________ pathway
de novo purine biosynthesis
T or F:
6-MP blocks the synthesis of purine nucleotides
true
6-MP is inactivated by what?
thiopurine methyl transferase (TPMT)
what common drug has an interaction with 6-MP that is definitely on the exam
allopurinol
why is there a bad drug reaction between 6-MP and allopurinol
xanthine oxidase breaks down 6-MP, allopurinol is a xanthine oxidase inhibitor
T or F:
allopurinol blocks the breakdown of both purine analogs, 6-MP and 6-TG
false, just 6-MP
Which drug primarily interferes with purine biosynthesis?
A. 5-Fluorouracil
B. Capecitabine
C. 6-Mercaptopurine
D. Cytosine arabinoside
C
make some folic acid flashcards because im brain dead and not getting the slide rn
okay later bro
stopped at slide 39
