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Protein synthesis inhibitor

protein synthesis inhibitor antibiotics, protein synthesis inhibitors
A protein synthesis inhibitor is a substance that stops or slows the growth or proliferation of cells by disrupting the processes that lead directly to the generation of new proteins

While a broad interpretation of this definition could be used to describe nearly any antibiotic, in practice, it usually refers to substances that act at the ribosome level either the ribosome itself or the translation factor, taking advantages of the major differences between prokaryotic and eukaryotic ribosome structures

Contents

  • 1 Mechanism
    • 11 Earlier stages
    • 12 Initiation
    • 13 Ribosome assembly
    • 14 Aminoacyl tRNA entry
    • 15 Proofreading
    • 16 Peptidyl transfer
    • 17 Ribosomal translocation
    • 18 Termination
    • 19 Protein synthesis inhibitors of unspecified mechanism
  • 2 Binding site
  • 3 See also
  • 4 References

Mechanism

In general, protein synthesis inhibitors work at different stages of prokaryotic mRNA translation into proteins, like initiation, elongation including aminoacyl tRNA entry, proofreading, peptidyl transfer, and ribosomal translocation and termination:

Earlier stages

  • Rifamycin inhibits prokaryotic DNA transcription into mRNA by inhibiting DNA-dependent RNA polymerase by binding its beta-subunit

Initiation

  • Linezolid acts at the initiation stage, probably by preventing the formation of the initiation complex, although the mechanism is not fully understood

Ribosome assembly

  • Neomycin prevents ribosome assembly by binding to the prokaryotic 30S ribosomal subunit

Aminoacyl tRNA entry

  • Tetracyclines and Tigecycline a glycylcycline related to tetracyclines block the A site on the ribosome, preventing the binding of aminoacyl tRNAs

Proofreading

  • Aminoglycosides, among other potential mechanisms of action, interfere with the proofreading process, causing increased rate of error in synthesis with premature termination

Peptidyl transfer

  • Chloramphenicol blocks the peptidyl transfer step of elongation on the 50S ribosomal subunit in both bacteria and mitochondria
  • Macrolides as well as inhibiting ribosomal translocation and other potential mechanisms bind to the 50s ribosomal subunits, inhibiting peptidyl transfer
  • Quinupristin/dalfopristin act synergistically, with dalfopristin, enhancing the binding of quinupristin, as well as inhibiting peptidyl transfer Quinupristin binds to a nearby site on the 50S ribosomal subunit and prevents elongation of the polypeptide, as well as causing incomplete chains to be released
  • Geneticin, also called G418, inhibits the elongation step in both prokaryotic and eukaryotic ribosomes

Ribosomal translocation

  • Macrolides, clindamycin and aminoglycosides with all these three having other potential mechanisms of action as well, have evidence of inhibition of ribosomal translocation
  • Fusidic acid prevents the turnover of elongation factor G EF-G from the ribosome
  • Ricin inhibits elongation by enzymatically modifying an rRNA of the eukaryotic 60S ribosomal subunit

Termination

  • Macrolides and clindamycin both also having other potential mechanisms cause premature dissociation of the peptidyl-tRNA from the ribosome
  • Puromycin has a structure similar to that of the tyrosinyl aminoacyl-tRNA Thus, it binds to the ribosomal A site and participates in peptide bond formation, producing peptidyl-puromycin However, it does not engage in translocation and quickly dissociates from the ribosome, causing a premature termination of polypeptide synthesis
  • Streptogramins also cause premature release of the peptide chain

Protein synthesis inhibitors of unspecified mechanism

  • Retapamulin
  • Mupirocin
  • Fusidic acid

Binding site

The following antibiotics bind to the 30S subunit of the ribosome:

  • Aminoglycosides
  • Tetracyclines

The following antibiotics bind to the 50S ribosomal subunit:

  • Chloramphenicol
  • Erythromycin
  • Clindamycin
  • Linezolid an oxazolidinone
  • Telithromycin
  • Streptogramins
  • Retapamulin

See also

  • Protein biosynthesis
  • Prokaryotic translation

References

  1. ^ "Definition: protein synthesis inhibitor from Online Medical Dictionary" 
  2. ^ "7344 Antibiotics, Toxins, and Protein Engineering, Spring 2007" MIT OpenCourseWare 
  3. ^ Swaney SM, Aoki H, Ganoza MC, Shinabarger DL December 1998 "The Oxazolidinone Linezolid Inhibits Initiation of Protein Synthesis in Bacteria" Antimicrob Agents Chemother 42 12: 3251–3255 PMC 106030  PMID 9835522 
  4. ^ Skripkin E, McConnell TS, DeVito J, et al October 2008 "Rχ-01, a New Family of Oxazolidinones That Overcome Ribosome-Based Linezolid Resistance" Antimicrobial Agents and Chemotherapy 52 10: 3550–3557 doi:101128/AAC01193-07 PMC 2565890  PMID 18663023 
  5. ^ Mehta, Roopal; Champney, W Scott 2003 "Neomycin and Paromomycin Inhibit 30S Ribosomal Subunit Assembly in Staphylococcus aureus" Current Microbiology 47 3: 237–43 doi:101007/s00284-002-3945-9 PMID 14570276 
  6. ^ Slover CM, Rodvold KA, Danziger LH June 2007 "Tigecycline: a novel broad-spectrum antimicrobial" Ann Pharmacother 41 6: 965–972 doi:101345/aph1H543 PMID 17519296 Retrieved 2009-12-19 
  7. ^ a b Flavio Guzmán 2008-08-12 "Protein synthesis inhibitors: aminoglycosides mechanism of action animation Classification of agents" Pharmamotion Archived from the original on 2010-03-12 
  8. ^ a b Protein synthesis inhibitors: macrolides mechanism of action animation Classification of agents Pharmamotion Author: Gary Kaiser The Community College of Baltimore County Retrieved on July 31, 2009
  9. ^ a b c Page 212 in: Title: Hugo and Russell's pharmaceutical microbiology Authors: William Barry Hugo, Stephen P Denyer, Norman A Hodges, Sean P Gorman Edition: 7, illustrated Publisher: Wiley-Blackwell, 2004 ISBN 0-632-06467-6 Length: 481 pages
  10. ^ "Geneticin" Thermo Fisher Scientific 
  11. ^ Wisteria Lane cases --> CLINDAMYCIN University of Michigan Retrieved on July 31, 2009
  12. ^ Leonard JE, Grothaus CD, Taetle R October 1988 "Ricin binding and protein synthesis inhibition in human hematopoietic cell lines" Blood 72 4: 1357–1363 PMID 3167211 
  13. ^ Terao K, Uchiumi T, Endo Y, Ogata K June 1988 "Ricin and alpha-sarcin alter the conformation of 60S ribosomal subunits at neighboring but different sites" Eur J Biochem 174 3: 459–463 doi:101111/j1432-10331988tb14120x PMID 3391162 
  14. ^ a b Menninger JR 1995 "Mechanism of inhibition of protein synthesis by macrolide and lincosamide antibiotics" J Basic Clin Physiol Pharmacol 6 3–4: 229–250 doi:101515/JBCPP199563-4229 PMID 8852269 
  15. ^ a b Tenson T, Lovmar M, Ehrenberg M July 2003 "The mechanism of action of macrolides, lincosamides and streptogramin B reveals the nascent peptide exit path in the ribosome" J Mol Biol 330 5: 1005–1014 doi:101016/S0022-28360300662-4 PMID 12860123 
  16. ^ a b c d e f g h i Levinson, Warren 2008 Review of medical microbiology and immunology New York: McGraw-Hill Medical ISBN 978-0-07-149620-9 
  17. ^ a b Drugbankca > Showing drug card for Retapamulin DB01256 Update Date: 2009-06-23

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