Anticancer Drugs MOA Only Exam 1

Question 1

Polyfunctional Alkylating Agents MOA

Answer 1

form covalent bonds with macromolecules in DNA molecule to cause DNA damage

Question 2

Antimetabolites MOA

Answer 2

inhibit DNA and/or RNA synthesis by either binding to the catalytic site of the enzyme or binding to an allosteric regulatory site

Question 3

Methotrexate MOA

Answer 3

inhibit purine synthesis and THF (in normal and cancer cells) by binding to dihydrofolate reductase

Question 4

Leucovorin MOA

Answer 4

establish high concentration in normal cells

• decrease influx of methotrexate
• increase efflux of methotrexate
• restore DNA and purine synthesis by being converted into N5, N10-Methylenetetrahydrofolate

Question 5

Glucarpidase MOA

Answer 5

decrease plasma levels by converting Methotrexate to inactive metabolites

Question 6

Mercaptopurine MOA

Answer 6

compete with inosinate (IMP) to inhibit the conversion of AMP and GMP (without, the cell cannot make DNA)

Question 7

Fluorouracil MOA

Answer 7

• 5-FUTP = inhibit RNA synthesis

- 5-FdUMP = inhibit DNA synthesis by inhibiting thymidylate synthase

Question 8

Uridine Triacetate (Triphosphate) MOA

Answer 8

compete with 5-FUTP and win against UTP to restore RNA synthesis

Question 9

Vinca Alkaloids MOA

Answer 9

bind to tubules, causing depolymerization of microtubules, resulting in mitotic arrest in M phase

Question 10

Epipodophyllotoxins MOA

Answer 10

inhibit topoisomerase II and cause DNA damage (strand breakage) to arrest the cell in S-G2 phase which inhibits mitosis

Question 11

Camptothecins MOA

Answer 11

inhibit topoisomerase I, resulting in DNA damage

Question 12

Taxanes MOA

Answer 12

bind to microtubule and cause polymerization of microtubles and leads to cell arrest in G2-M phase.

Question 13

Anthracyclines MOA

Answer 13

• inhibit topoisomerase II
• high affinity binding to DNA through intercalation (insertion between DNA bases and bind noncovalently to inhibit DNA synthesis)
• bind to cellular membranes to alter function and permeability
• generation of free radicals and oxygen free radicals using iron

Question 14

Mitomycin MOA

Answer 14

• bifunctional alkylating drug that binds to two DNA strands (crosslink) to damage DNA

Question 15

Bleomycin MOA

Answer 15

• form iron-bleomycin-DNA complex. bleomycin is oxidized and forms oxygen free radicals to cause double and single strand breaks, causing cell arrest in G2 phase