BCHM drugs Flashcards

1
Q

Azidothymidine (Zidovudine or AZT)

Structure?

A

Anti-viral Nucleoside Analogue of deoxythymidine

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

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2
Q

Azidothymidine (Zidovudine or AZT)

Target?

A

Viral reverse transcriptase

Inhibitor of viral replication

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3
Q

Acyclovir

Structure?

A

Anti-viral Nucleoside Analogue of deoxyguanosine

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

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4
Q

What is special about Acyclovir

A

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.

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5
Q

What is the target of Didanosine?

A

Viral reverse transcriptase
Inhibitor of viral replication

HIV

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6
Q

Adenosine arabinoside (Vidarabine) used for which disease?

A

Relapsed Childhood Acute Lymphoblastic Leukemia and Herpes Simplex Infections

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7
Q

Which drugs can be used for HIV?

A

Didanosine
Tenofovir
AZT

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8
Q

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

A

Inhibits Methylation once incorporated into DNA and RNA

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9
Q

Which drug do you use for TB?

A

Rifamycin (Rifampin)

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10
Q

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.

A

5-fluorouracil

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11
Q

Which drugs attach viral DNA polymerase?

A

Tenofovir and Adenosine arabinoside (Vidarabine)

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12
Q

Inhibits HUMAN DNA polymerase

A

Cytosine arabinoside (araC or Cytarabine)

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13
Q

Inhibits DNA Gyrase

A

Novobiocin, Ciprofloxacin and Nalidixic Acid

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14
Q

Which drug intercalates between adjacent G-C Bases

A

Actinomycin D (Dactinomycin)

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15
Q

What does Alpha-Amanitin Toxin inhibit?

A

RNA Polymerase II (Eukaryotes)

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16
Q

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

A

Streptomycin

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17
Q

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

A

Erythromycin

18
Q

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

A

Tetracycline

19
Q

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

A

Puromycin

Prokaryotes and Eukaryotes

20
Q

Allopurinol

A

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

21
Q

Cycloheximide prevents which part of translation?

A

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

22
Q

Diphtheria toxin inactivates…

A

It inactivates Eukaryotic EF-2, Preventing Translocation

23
Q

Which drugs blocks elongation of translation in prokaryotes?

A

Tetracycline
Erythromycin
Chloramphenicol
Puromycin

24
Q

Which drugs blocks elongation of translation in eukaryotes?

A

Cycloheximide
Puromycin
Diphtheria toxin

25
Q

Which drug blocks Eukaryotic Topoisomerase II?

A

Etoposide

26
Q

What does camptothecin block?

A

Eukaryotic Topoisomerase I

27
Q

Which complex of ETC does Rotenone inhibit?

A

Complex I

28
Q

Which complex of ETC does Antimycin A inhibit?

A

Complex III

29
Q

Which complex of ETC does Oligomycin inhibit?

A

Complex V

ATPase

30
Q

Amytal and Piericidin blocked which complex of ETC?

A

Complex I

31
Q

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

A

Complex IV

32
Q

Name 3 inhibitors of complex I

A

Rotenone
Amytal
Piercidin

33
Q

How does direct inhibitors of ETC affect:

  1. ATP synthesis
  2. ETC
  3. O2 consumption
A
  1. ATP synthesis - decrease
  2. ETC - decrease
  3. O2 consumption - decrease
34
Q

How does uncouplers of ETC affect the following?

  1. ATP synthesis
  2. ETC
  3. O2 consumption
A
  1. ATP synthesis - decrease
  2. ETC - increase
  3. O2 consumption - increase
35
Q

What type of drug is Valinomycin?

A

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

36
Q

How does 2,4-DNP disrupt ETC?

A

Uncoupler - destroys proton gradient

37
Q

Gramicidin affects ETC by…

A

forming an ionophore - uncoupler

38
Q

Name 2 drugs that inhibit ADP/ATP translocase

A

Atractyloside and

Bongkrekic acid

39
Q

Pentavalent arsenate poisoning inhibits which enzyme?

A

glyceraldehyde 3-phosphate dehydrogenase enzyme

40
Q

Flouride ions hibit which enzyme?

A

Enolase

41
Q

Trivalent arsenic compounds will block which enzymes?

A

Pyruvate dehydrogenase complex

a-ketoglutarate dehydrogenase complex

42
Q

Low thamine levels will affect which enzymes?

A

Transketolase
Pyruvate dehydrogenase complex
a-ketoglutarate dehydrogenase complex