Protein Synthesis Inhibitors (General) Flashcards
Drugs tha selectively inhibit bacterial protein synthesis:
- Chloramphenicol
- Tetracyclines
- Macrolides
- Clindamycin
- Streptogramins
- Linezolid
do microorganisms and mamalian cells have the same process of protein synthesis?
NOPE
what kind of ribosomes does bacteria have?
70S
What kind of ribososme does mamalian cells have?
80S
What are the basis for selective toxicity against microorganisms without causing major effects on mamalian cells?
Differences in:
- Ribosomal subunits
- Chemical composition
- Functional specificities of component nucleic acids and proteins
Broad spectrum protein synthesis inhibitors
- Chloramphenicol
- Tetracyclines
Moderate spectrum protein synthesis inihibitors
- Macrolides
- Ketolides
Narrow spectrum protein synthesis inhibitors
- Lincosamide
- Streptogramins
- Linezolid
first inhibitors of bacterial protein synthesis
to be discovered
- Chloramphenicol
- Tetracyclines
- Aminoglycosides
an older macrolide antibiotic, has
a narrower spectrum of action but continues to be active against several important pathogens
Erythromycin
semisynthetic macrolides, have some distinctive properties compared with erythromycin
- Azithromycin
- Clarithromycin
- Clindamycin
Newer inhibitors ofmicrobial protein synthesis, have activity against certain bacteria that have developed resistance to older antibiotics.
- streptogramins
- linezolid
- telithromycin
- tigecycline (tetracycline analog)
The binding site of most of the antibiotics reviewed in this chapter are on the ____ ribosonal subunit except tetracyclines
50s
The binding site of tetracyclines are on the ____ ribosomal subunit
30S
transpeptidation is catalyzed by what enzyme
peptidyl transferase
inhibits transpeptidation by blocking the binding of the aminoacyl moiety of the charged transfer RNA (tRNA) to the acceptor site of the mRNA complex.
Chloramphenicol
Most of the antibiotics reviewed in this chapter are bacteriostatic inhibitors of protein synthesis acting at the ribosomal level except:
- streptogramins
- oxazolidinones
- pleuromutilins
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.
Streptogramins
binds to the unique site in the 50s ribosome, inhibiting initiation by blocking formation of the tRNA-ribosome-mRNA ternary complex
Linezolid
bind to the 30S ribosomal subunit preventing
binding of amino acid-charged tRNA to the acceptor site of the
ribosome-mRNA complex.
Tetracyclines
can inhibit the functions of
mitochondrial ribosomes, which contain 70S ribosomal RNA.
Chloramphenicol
have little effect on mammalian protein synthesis because an active efflux mechanism prevents their intracellular
accumulation.
Tetracyclines
Steps in bacterial protein synthesis:
- tRNA carrying amino acid 6 binds to acceptor site of ribosome
- The peptidyl tRNA at the donor site with amino acid 1-5 binding to the amino acid 6 (transpeptidation)
- The uncharged tRNA at the donor site is released
- The new six amino acid chain with its tRNA shifts to the peptidyl site