Anti-Cancer

Question 1

Methotrexate

Answer 1

Anti-metabolite, antiFOLATE
Competitively and reversibly inhibits DHFR enzyme (tetrahydrofolate synthesis)
- 100X > affinity than folic acid
- inhibits synthesis of DNA, RNA and proteins

Question 2

Fluorouracil (5-FU)

Answer 2

Anti-metabolite, [Pyrimidine Analog]
Thymidylate synthase (dUMP > dTMP) inhibitor
Blocks formation of T, needed for DNA rep.
Toxicity: myelosuppression, mucositis

Question 3

6-Mercaptopurine (6-MP)

Answer 3

[Purine Analog]
Inhibits conversion of IMP to AMP and GMP (XMP) via SAMP
- decreases purine availability for DNA synthesis

Question 4

Gleevec

Answer 4

[Tyrosine Kinase Inhibitor]
Binds to growth factor proteins and inhibits phosphorylation cascade.
Prevents activation of Ras and other growth activating signals

Question 5

Cyclophosphamide

Answer 5

[Alkylating Agent]
Pro-drug converted to its active form in the liver
- Nitrogen mustard (forms DNA cross links) alkylating agent
Ex: Cytoxan, Neosar

Question 6

Vincristine, Vinblastine

Answer 6

[Mitotic Spindle Poison]
Binds tubulin diners inhibiting microtubule formation
Arrests mitosis in metaphase

Question 7

Doxorubicin

Answer 7

interacts with DNA by intercalation, keeps topoisomerase II bound to the DNA chain
inhibits macromolecule biosynthesis
prevents resealing of dsDNA chain
generates free radicals: heart problems

Question 8

microRNAs

Answer 8

Bind mRNA and target it for degradation or to repress translation of DNA into RNA
very broad spectrum tx; used for gene therapy

Question 9

Oral Complications of Anti-Cancer Tx

Answer 9

Stomatitis/Mucositis
Immunosuppression&raquo_space; infections
Neurotoxicity (esp differentiated quiescent cells)