BCHM drugs

Question 1

Azidothymidine (Zidovudine or AZT)

Structure?

Answer 1

Anti-viral Nucleoside Analogue of deoxythymidine

No 3’ OH Group due to N=N=N group at 3’ position

Question 2

Azidothymidine (Zidovudine or AZT)

Target?

Answer 2

Viral reverse transcriptase

Inhibitor of viral replication

Question 3

Acyclovir

Structure?

Answer 3

Anti-viral Nucleoside Analogue of deoxyguanosine

No 3’ OH Group due to broken ring structure of pentose sugar

Question 4

What is special about Acyclovir

Answer 4

First phosphorylation by viral thymidine kinase (specificity b/c only infected cells possess viral kinase), last two phosphorylations by host cellular kinase. Causes chain termination once incorporated to DNA.

Question 5

What is the target of Didanosine?

Answer 5

Viral reverse transcriptase
Inhibitor of viral replication

HIV

Question 6

Adenosine arabinoside (Vidarabine) used for which disease?

Answer 6

Relapsed Childhood Acute Lymphoblastic Leukemia and Herpes Simplex Infections

Question 7

Which drugs can be used for HIV?

Answer 7

Didanosine
Tenofovir
AZT

Question 8

How does 5-aza-2’-deoxycytidine (Decitabine) – 5-azacytidine work?

Answer 8

Inhibits Methylation once incorporated into DNA and RNA

Question 9

Which drug do you use for TB?

Answer 9

Rifamycin (Rifampin)

Question 10

In cells, which drug is converted to FdUMP which inhibits thymidylate kinase, and thus inhibiting synthesis of thymine nucleotides that are required for DNA synthesis.

Answer 10

5-fluorouracil

Question 11

Which drugs attach viral DNA polymerase?

Answer 11

Tenofovir and Adenosine arabinoside (Vidarabine)

Question 12

Inhibits HUMAN DNA polymerase

Answer 12

Cytosine arabinoside (araC or Cytarabine)

Question 13

Inhibits DNA Gyrase

Answer 13

Novobiocin, Ciprofloxacin and Nalidixic Acid

Question 14

Which drug intercalates between adjacent G-C Bases

Answer 14

Actinomycin D (Dactinomycin)

Question 15

What does Alpha-Amanitin Toxin inhibit?

Answer 15

RNA Polymerase II (Eukaryotes)

Question 16

Which drug binds to 30s ribosomal subunit of prokaryotes and distorts structure, preventing initiation of translation?

Answer 16

Streptomycin

Question 17

Which drug binds to 50S subunit of complete 70S ribosome and blocks translocation?

Answer 17

Erythromycin

Question 18

Interacts with 30S subunit of complete 70S ribosome and blocks access of A site

Answer 18

Tetracycline

Question 19

Blocks Elongation after it forms peptide bond with growing protein chain, causing peptide to fall out of P site and premature translation termination

Answer 19

Puromycin

Prokaryotes and Eukaryotes

Question 20

Allopurinol

Answer 20

Inhibits xanthine oxidase, thus lowering the conversion of purine bases to uric acid end products.

Question 21

Cycloheximide prevents which part of translation?

Answer 21

Prevents elongation of translation by inhibiting Eukaryotic peptidyl-transferase (peptide bond formation).

Question 22

Diphtheria toxin inactivates…

Answer 22

It inactivates Eukaryotic EF-2, Preventing Translocation

Question 23

Which drugs blocks elongation of translation in prokaryotes?

Answer 23

Tetracycline
Erythromycin
Chloramphenicol
Puromycin

Question 24

Which drugs blocks elongation of translation in eukaryotes?

Answer 24

Cycloheximide
Puromycin
Diphtheria toxin

Question 25

Which drug blocks Eukaryotic Topoisomerase II?

Answer 25

Etoposide

Question 26

What does camptothecin block?

Answer 26

Eukaryotic Topoisomerase I

Question 27

Which complex of ETC does Rotenone inhibit?

Answer 27

Complex I

Question 28

Which complex of ETC does Antimycin A inhibit?

Answer 28

Complex III

Question 29

Which complex of ETC does Oligomycin inhibit?

Answer 29

Complex V | ATPase

Question 30

Amytal and Piericidin blocked which complex of ETC?

Answer 30

Complex I

Question 31

CO, azide, Hydrogen sulphide (H2S) and Cyanide (CN-) blocked which complex of ETC?

Answer 31

Complex IV

Question 32

Name 3 inhibitors of complex I

Answer 32

Rotenone Amytal Piercidin

Question 33

How does direct inhibitors of ETC affect: 1. ATP synthesis 2. ETC 3. O2 consumption

Answer 33

1. ATP synthesis - decrease 2. ETC - decrease 3. O2 consumption - decrease

Question 34

How does uncouplers of ETC affect the following? 1. ATP synthesis 2. ETC 3. O2 consumption

Answer 34

1. ATP synthesis - decrease 2. ETC - increase 3. O2 consumption - increase

Question 35

What type of drug is Valinomycin?

Answer 35

Uncoupler of ETC. It's a mobile carrier of K+.

Question 36

How does 2,4-DNP disrupt ETC?

Answer 36

Uncoupler - destroys proton gradient

Question 37

Gramicidin affects ETC by...

Answer 37

forming an ionophore - uncoupler

Question 38

Name 2 drugs that inhibit ADP/ATP translocase

Answer 38

Atractyloside and | Bongkrekic acid

Question 39

Pentavalent arsenate poisoning inhibits which enzyme?

Answer 39

glyceraldehyde 3-phosphate dehydrogenase enzyme

Question 40

Flouride ions hibit which enzyme?

Answer 40

Enolase

Question 41

Trivalent arsenic compounds will block which enzymes?

Answer 41

Pyruvate dehydrogenase complex | a-ketoglutarate dehydrogenase complex

Question 42

Low thamine levels will affect which enzymes?

Answer 42

Transketolase Pyruvate dehydrogenase complex a-ketoglutarate dehydrogenase complex