Drugs

Question 1

Rifampin

Answer 1

Inhibit initiation of transcription by inhibiting the formation of phosphodiester bond in prokaryotes

Question 2

Alpha-amanitin

Answer 2

Block RNA pol II

Question 3

Actinomycin D

Answer 3

Intercalating DNA strands

Inhibits both DNA replication and transcription in prok and euk

Question 4

Courmarin, novobiocin

Quinolones, nalidixic, ciprofloxacin

Answer 4

Inhibit bac gyrase

Question 5

Diphtheria-Toxin A

Answer 5

Transfer ADP-ribose to host cells EF-2
Inhibit translocation thus no protein synthesis
Add nicotinamide to reverse rxn, get EF-2 out

Question 6

Streptomycin

Answer 6

Binds to 30S subunit, prevent binding of fMet-tRNA to P site

Inhibit initiation of translation and assembly of full ribosome

Question 7

Tetracycline

Answer 7

Interact with 30S
Prevent binding or aminoacyl-tRNA to A site
Block elongation
Selectively concentrated by bacteria

Question 8

Erythromycin

Answer 8

Bind irreversibly to 50S
Block translocation by EF-G
Prevent elongation

Question 9

Chloramphenicol

Answer 9

Binds to 50S and inhibits peptidyl transferase
Prevents elongation
Mainly prok, but may inhibit mitochondrial ribosomes

Question 10

Cycloheximide

Answer 10

Inhibit peptidyl transferase in 60S
Onlu nuclear tl, not mito tl, in euk
Only research not for human

Question 11

Puromycin

Answer 11

Ribosome cannot break amide bond to release tRNA
Inhibits elongation and cause premature chain termination
In both euk and prok, not in clinic

Question 12

Statin, lovastatin = mevinolin

Answer 12

Competitive inhibitor of HMG-CoA reductase

Reduce blood cholesterol

Question 13

Organophosphates like DFP

Answer 13

Irreversibly inhibit acetylcholinesterase, which degrades Ach to cholin and acetate

Question 14

Penicillin

Answer 14

Irreversibly inhibits bac glycoprotein transpeptidase, a serine protease, which breaks bac cell wall

Question 15

Aspirin

Answer 15

Irreversibly inhibit COX-1 & -2
Covalent acetylation of ser along the wall of a tunnel inside the enzyme
Block formation of thromboxanes
Prevent platelet aggregation, improve vascular health

Question 16

Suicide inhibitors

Answer 16

Allopurinol activated by xanthine oxidase and irreversibly bind to this same enzyme

Question 17

Cholera

Answer 17

Ribosylates Gs alpha, no longer hydrolyze GTP, permanently active
Elevated cytosolic cAMP activate PKA and Ca2+ > stimulate Cl- secretion into lumen > Na+ and water follows > diarrhea

Question 18

Pertussis

Answer 18

Whooping cough, paralyses the cilia of mammalian respiratory epithelium

Toxin is hexamer: 2 S4, S1-S5

Ribosylates Gi alpha

Question 19

Atenolol

Answer 19

Beta-blocker, regulate tachycardia

Question 20

Azidothymidine = AZT

Answer 20

Lack 3’OH
DeoxyT analog
Inhibit RT, treat HIV

Question 21

Didanosine = ddl

Answer 21

Lack 3’ OH
DeoxyA analog
Inhibit RT, treat HIV

Question 22

Acyclovir

Answer 22

DeoxyG analog
Open ring structure than sugar
Inhibit viral DNA Pol
Treat Herpes virus

Question 23

Tenofovir

Answer 23

DeoxyA analog

Inhibit RT, treat HIV

Question 24

Arabinooside (both C and A)

Answer 24

Planar structure
Inhibit DNA Pol
Anti-cancer

Question 25

5-aza-2’deoxycytidine

5-azacytidine

Answer 25

Inhibit DNA methylation

Question 26

5-fluorouracil

Answer 26

Inhibit synthesis of thymine

Question 27

Azathioprine

Answer 27

Suppress transplant rejection

Question 28

Alluporinol

Answer 28

Treat gout

Question 29

Adenosine (Adenocard) IV

Answer 29

Treat supraventricular tachycardia

Question 30

Camptothecin

Answer 30

Inhibit Topo I

Question 31

Etoposide

Answer 31

Inhibit Topo II