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Protien synthesis inhibitors by dr.elza

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Protiensynthesis inhibitors

Publié dans : Santé & Médecine
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Protien synthesis inhibitors by dr.elza

  1. 1. Dr.Elza Joy Munjely JR-I Depmt. Of Pharmacology Govt. Medical College,Kottayam.
  2. 2. 2 INTRODUCTION TO PROTEIN SYNTHESIS • Protein synthesis inhibitor - substance that stops or slows the growth or proliferation of bacterial cells by disrupting the processes of generation of new proteins by targeting the bacterial ribosome. • Act at the ribosome level • Take advantage of the major differences between prokaryotic and eukaryotic ribosome. • Work at different stages of mRNA translation like initiation, elongation, and termination.
  3. 3. 3 PROKARYOTIC AND EUKARYOTIC RIBOSOMES
  4. 4. PROTEIN SYNTHESIS
  5. 5. PROCESS OF TRANSLATION
  6. 6. 30 S 50S P-Site A-Site INITIATION COMPLEX m-RNA
  7. 7. A4 P-Site A-Site A3 A2 A1 TRANSPEPTIDATION
  8. 8. A4 P-Site A-Site A3 A2 A1
  9. 9. A4 A3 A2 A1
  10. 10. A4 A3 A2 A1 A 5 TRANSLOCATION
  11. 11. A4 A3 A2 A1 A 5 TRANSLOCATION
  12. 12. A4 A3 A2 A1 A 5 A 6
  13. 13. MOA OF AMINOGLYCOSIDES & SPECTINOMYCIN  Penetrate bacterial cell wall through porin channels by passive diffusion  Betalactams facilitate passive diffusion of aminoglycosides-SYNERGISTIC ACTION Bind to 30S ribosomal subunit Improper formation of initiation complex Misreading of mRNA
  14. 14. 30 S 50S P-Site A-Site IMPROPER FORMATION OF INITIATION COMPLEX & MISREADING OF mRNA m-RNA AMINOGLYCOSIDES &SPECTINOMYCIN
  15. 15. MOA OF LINEZOLID  Binds to 50S ribosomal subunit near the interface with 30S subunit.  Prevents the formation of ribosomal complex.
  16. 16. 50S P-Site A-Site LINEZOLID INHIBITION OF RIBOSOMAL COMPLEX FORMATION
  17. 17. MOA OF TETRACYCLINES  Drug enter into cytoplasm by:  Energy dependent tetracycline active transport system – Gram positive bacteria  Passive diffusion through porin channels – Gram negative bacteria  Binds to 30Ssubunit of the ribosome  & inhibits the binding of aminoacyl tRNA to the A site.
  18. 18. A4 P-Site A-Site A3 A2 A1 TETRACYCLINES PREVENTS BINDING OF AMINOACYL tRNA TO A SITE
  19. 19. MOA OF CHLORAMPHENICOL  Binds to 50S subunit of the ribosome  Inhibits peptide bond formation.
  20. 20. A4 P-Site A-Site A3 A2 A1 TRANSPEPTIDATION INHIBITED CHLORAMPHENICOL
  21. 21. MOA OF MACROLIDES ,CLINDAMYCIN &STREPTOGRAMINS  Reversibly binds to P site of 50 S ribosome  Thus inhibits translocation
  22. 22. A4 A3 A2 A1 P-Site A-Site MACROLIDES , CLINDAMYCIN & STREPTOGRAMINS TRANSLOCATION INHIBITED
  23. 23. MOA OF MUPIROCIN  Binds to isoleucyl tRNA synthetase  Prevents incorporation of isoleucine into bacterial protiens
  24. 24. THANK YOU

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