Protien synthesis inhibitors by dr.elza

Protiensynthesis inhibitors

1. PROTIEN SYNTHESIS INHIBITORS Dr.Elza Joy Munjely JR-I Depmt . Of Pharmacology Govt. Medical College,Kottayam .

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 PROKARYOTIC AND EUKARYOTIC RIBOSOMES

4. PROTEIN SYNTHESIS

5. PROCESS OF TRANSLATION

6. 30 S 50S P-Site A-Site INITIATION COMPLEX m-RNA

7. A4 P-Site A-Site A3 A2 A1 TRANSPEPTIDATION

8. A4 P-Site A-Site A3 A2 A1

9. A4 A3 A2 A1

10. A4 A3 A2 A1 A5 TRANSLOCATION

11. A4 A3 A2 A1 A5 TRANSLOCATION

12. A4 A3 A2 A1 A5 A6

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. 30 S 50S P-Site A-Site IMPROPER FORMATION OF INITIATION COMPLEX & MISREADING OF mRNA m-RNA AMINOGLYCOSIDES &SPECTINOMYCIN

15. MOA OF LINEZOLID Binds to 50S ribosomal subunit near the interface with 30S subunit. Prevents the formation of ribosomal complex.

16. 50S P-Site A-Site LINEZOLID INHIBITION OF RIBOSOMAL COMPLEX FORMATION

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. A4 P-Site A-Site A3 A2 A1 TETRACYCLINES PREVENTS BINDING OF AMINOACYL tRNA TO A SITE

19. MOA OF CHLORAMPHENICOL Binds to 50S subunit of the ribosome Inhibits peptide bond formation.

20. A4 P-Site A-Site A3 A2 A1 TRANSPEPTIDATION INHIBITED CHLORAMPHENICOL

21. MOA OF MACROLIDES ,CLINDAMYCIN &STREPTOGRAMINS Reversibly binds to P site of 50 S ribosome Thus inhibits translocation

22. A4 A3 A2 A1 P-Site A-Site MACROLIDES , CLINDAMYCIN & STREPTOGRAMINS TRANSLOCATION INHIBITED

23. MOA OF MUPIROCIN Binds to isoleucyl tRNA synthetase Prevents incorporation of isoleucine into bacterial protiens

24. THANK YOU