Protein Synthesis Inhibitors (General) Flashcards

1
Q

Drugs tha selectively inhibit bacterial protein synthesis:

A
  1. Chloramphenicol
  2. Tetracyclines
  3. Macrolides
  4. Clindamycin
  5. Streptogramins
  6. Linezolid
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2
Q

do microorganisms and mamalian cells have the same process of protein synthesis?

A

NOPE

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3
Q

what kind of ribosomes does bacteria have?

A

70S

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4
Q

What kind of ribososme does mamalian cells have?

A

80S

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5
Q

What are the basis for selective toxicity against microorganisms without causing major effects on mamalian cells?

A

Differences in:
- Ribosomal subunits
- Chemical composition
- Functional specificities of component nucleic acids and proteins

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6
Q

Broad spectrum protein synthesis inhibitors

A
  • Chloramphenicol
  • Tetracyclines
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7
Q

Moderate spectrum protein synthesis inihibitors

A
  • Macrolides
  • Ketolides
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8
Q

Narrow spectrum protein synthesis inhibitors

A
  • Lincosamide
  • Streptogramins
  • Linezolid
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9
Q

first inhibitors of bacterial protein synthesis
to be discovered

A
  • Chloramphenicol
  • Tetracyclines
  • Aminoglycosides
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9
Q

an older macrolide antibiotic, has
a narrower spectrum of action but continues to be active against several important pathogens

A

Erythromycin

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10
Q

semisynthetic macrolides, have some distinctive properties compared with erythromycin

A
  • Azithromycin
  • Clarithromycin
  • Clindamycin
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11
Q

Newer inhibitors ofmicrobial protein synthesis, have activity against certain bacteria that have developed resistance to older antibiotics.

A
  • streptogramins
  • linezolid
  • telithromycin
  • tigecycline (tetracycline analog)
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11
Q

The binding site of most of the antibiotics reviewed in this chapter are on the ____ ribosonal subunit except tetracyclines

A

50s

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12
Q

The binding site of tetracyclines are on the ____ ribosomal subunit

A

30S

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13
Q

transpeptidation is catalyzed by what enzyme

A

peptidyl transferase

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14
Q

inhibits transpeptidation by blocking the binding of the aminoacyl moiety of the charged transfer RNA (tRNA) to the acceptor site of the mRNA complex.

A

Chloramphenicol

15
Q

Most of the antibiotics reviewed in this chapter are bacteriostatic inhibitors of protein synthesis acting at the ribosomal level except:

A
  • streptogramins
  • oxazolidinones
  • pleuromutilins
16
Q

They bind to the 50S ribosomal subunit, constricting the
exit channel on the ribosome through which nascent polypeptides are extruded. In addition, tRNA synthetase activity is inhibited, leading to a decrease in free tRNA within the cell.

A

Streptogramins

17
Q

binds to the unique site in the 50s ribosome, inhibiting initiation by blocking formation of the tRNA-ribosome-mRNA ternary complex

A

Linezolid

18
Q

bind to the 30S ribosomal subunit preventing
binding of amino acid-charged tRNA to the acceptor site of the
ribosome-mRNA complex.

A

Tetracyclines

19
Q

can inhibit the functions of
mitochondrial ribosomes, which contain 70S ribosomal RNA.

A

Chloramphenicol

20
Q

have little effect on mammalian protein synthesis because an active efflux mechanism prevents their intracellular
accumulation.

A

Tetracyclines

21
Q

Steps in bacterial protein synthesis:

A
  1. tRNA carrying amino acid 6 binds to acceptor site of ribosome
  2. The peptidyl tRNA at the donor site with amino acid 1-5 binding to the amino acid 6 (transpeptidation)
  3. The uncharged tRNA at the donor site is released
  4. The new six amino acid chain with its tRNA shifts to the peptidyl site