Drugs

Question 1

cisplatin

Answer 1

base alkylating agent; damages DNA of cancer cells to prevent replication/transcription

Question 2

actinomycin D

Answer 2

naturally-occurring chemotherapy; “intercalates” into DNA (inserts ring that stacks with DNA bases) to alter structure; interferes with DNA replication and transcription

Question 3

doxorubicin

Answer 3

interferes with DNA replication (similar to actinomycin D)

Question 4

etoposide and camptothecin

Answer 4

chemotherapeutics that target topoisomerase (topoisomerase breaks DNA backbone to “relax” supercoiled DNA and these drugs leave DNA breaks that can’t be repaired)

Question 5

puromycin

Answer 5

mimics “acceptor” 3’ end of tRNA, binds in ribosome as it is translating, preventing completion of translation

Question 6

Tamoxifen acts as an antagonist to ________

Answer 6

estrogen

Question 7

Tamoxifen prevents the recruitment of ______ cofactors

Answer 7

HAT

Question 8

aspirin

Answer 8

(anti-inflammatory) blocks phosphorylation of IkB so NK-kB can’t be exposed and can’t get into nucleus to signal inflammation

Question 9

cyclosporine

Answer 9

(immunosuppressant) inhibits calcineurin activation so NF-ATc can’t be dephosphorylated and activate immune response

Question 10

alpha amanitin

Answer 10

non-competitive inhibitor of RNA Pol II; binds bridge helix (upper and lower jaws of RNA Pol), blocks RNA chain elongation by preventing translocation

Question 11

rifamipicin

Answer 11

binds bacterial RNA polymerase and blocks RNA exit channel; prevents growth of RNA because growing RNA chain has nowhere to go

Question 12

rapamycin

Answer 12

inhibits eukaryotic cap-dependent translation by affecting 4E-BP so initiation complex doesn’t form; main target of mTOR; used in cancer treatment

Question 13

warfarin

Answer 13

prevents carboxylation of glutamate residues and acts as anticoagulant (blood thinner)

Question 14

gleevec

Answer 14

tyrosine kinase inhibitor; leukemia treatment that competitively binds a kinase so substrate is not phosphorylated; tumor can’t proliferate

Question 15

velecade/ bortezomib

Answer 15

inhibits a proteasome that degrades good proteins (treats multiple myeloma)

Question 16

aminoglycosides

Answer 16

streptomycin

Question 17

tetracyclines

Answer 17

tetracyclines

Question 18

macrolides

Answer 18

erythromycin

Question 19

other antibiotics that bind at RNA exit channel

Answer 19

chloramphenicol

Question 20

Ritonavir is a ________ inhibitor and inhibits _________

Answer 20

competitive, HIV protease