Drugs- Get Them Here

Question 1

Warfarin- What enzyme does it inhibit? What process is prevented? What is it used for?

Answer 1

Inhibits gamma-glutamyl carboxylase. Prevents the carboxylation of glutamate which is important in clotting factors, thus blood thinner.

Question 2

Vornistat

Answer 2

HDAC inhibitor. Prevents HDAC from silencing tumor suppressor genes, thus cancer drug.

Question 3

Gleevac

Answer 3

bcr-abl Tyrosine kinase inhibitor. Prevents dephosphorylation of tyrosine residue by competitive binding inhibiting cell proliferation. Cancer drug for Chronic Myeligenous Leukemia (CMC).

Question 4

Bortezomib

Answer 4

Protesome inhibitor. Prevents degradation of apoptotic factors. Treats multiple myeloma.

Question 5

alpha-amanitin

Answer 5

RNA polymerase II inhibitor. Binds to bridge helix (alpha helix btwn upper and lower “jaw” of enzyme) and prevents translocation of Pol II on promotor.

Question 6

Rifampicin

Answer 6

RNA polymerase II inhibitor. Blocks RNA exit channel located within beta-subunit of Pol II.

Question 7

AZT

Answer 7

Inhibitor of HIV Reverse Transcriptase

Question 8

Acyclovir

Answer 8

inhibits Viral DNA polymerase, used for Herpes Simplex Virus, and Varicella Zoster Virus

Question 9

Quinolones

Answer 9

Inhibits bacterial DNA gyrase, a topoisomerase

Question 10

Puromicin

Answer 10

An antibiotic that mimics the “acceptor” 3’ end of a tRNA that is charged with an amino acid.

Puromycin can bind in the ribosome as it is translating and covalently attach to a growing polypeptide chain,
preventing the completion of translation.

Question 11

Streptomycin

Answer 11

inhibits 30s subunit; affects initiation and elongation

Question 12

Erythromycin, and Choloramphenicol

Answer 12

inhibits 50s subunit; affects peptidyl transferase

Question 13

Tetracyclin

Answer 13

inhibits A site, affect binding of aminoacyl tRNA

Question 14

Rapamycin

Answer 14

inhibit mTor; inhibit phosphorylation of 4E-BP

Question 15

DDI

Answer 15

Inhibitor of HIV Reverse Transcriptase

Question 16

What does eIF2 kinase do?

Answer 16

It phosphorylates inactive nucleases, making them active to degrade viral mRNA

Question 17

Cyclosporin and Fk506

Answer 17

immunosuppressants that inhibit calcineurin, which inhibits NFAT from entering the nucleus and activating immune response

Question 18

Aspirin

Answer 18

anti-inflammatory agent. Inhibits phosphorylation and degredation of Inhibitor kappa B, thus preventing NF-kappa B from entering the nucleus and transcribing genes for inflammatory response

Question 19

Cisplatin

Answer 19

an alkylating agent that forms DNA adducts that disrupt DNA replication in rapidly dividing cells

Question 20

Actinomycin D

Answer 20

antibiotic that intercalates with DNA to interfere with DNA replication

Question 21

Aminoglycosides

Answer 21

cause premature termination of polypeptide synthesis at ribosome

Question 22

Microlides

Answer 22

inhibit translation in bacteria by inhibiting PTC function