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