Protein Synthesis-Translation_Inhibitors.doc:

 

General:

 

 

Kusugamycin

PK

Inhibits chain initiation by displacing f.met.tRNA from the ribosome.

Mutation causes resistance, which is due to the lack of methylation of 16s rRNA at specific position, thus F.met.tRNA is released from the ribosomal surface.

 

Streptomycin:

PK and EK

Binds to 30S ribosome and misincorporates aminoacyl tRNAs.  It can act on EK ribosome and misreads the codons and can inhibit chain initiation.

Mutation in s12 riboprotein can cause resistance, how?

 

Tetracycline

PK

Inhibits aminoacyl tRNA to bind to 30s ribosome.

 

Mutation in 23s rRNA causes resistance

 

Kirromycin:

PK

Kirromycin: inhibits chain translocation, by blocking the release of EF-Tu-GDP and there is no recycling of the factor.

Mutation in 23s rRNA causes resistance

 

Puromycin

PK

Incorporates the antibiotic into A site and forms a peptide bond with the peptidyl-tRNA found in P site and terminates chain synthesis prematurely.  Puromycin structure resembles a tRNA.

 

Erythromycin

PK

Prevents peptidyl bond transfer and translocation

Mutation in 23s rRNA makes it resistant to the antibiotic.

 

Chloramphenicol

PK, mitochondria, chloroplast

Affects PK and mitochondria and chloroplasts, it binds to 50s ribosomes inhibits peptidyl transfer.

Mutation in one of the 50s riboprotein makes it resistant.

 

Fusidic acid

EK

Prevents translocation, prevents the release of eEF-G-GDP from 60s ribosome.

 

 

Thieostrepton

PK

 Inhibits translocation, binds to 23srRNA and inhibits GTPase activity.

 

 

Cycloheximide

EK

Inhibits peptidyl transferase on 60s ribosome.

 

 

Neomycin

EK

Acts at multiple sites inhibits translocation in EK.

 

Hygromycin

EK

Inhibits translocation.

 

 

 

 

 

 

Eukaryotic Specific Translation Inhibitors:

 

 

Inhibitor

Action

Interferon,                                                                                      

NAF, M7GP,                                                                                  

Spectinomycin,                                                                              

Anri nitrile carboxylic acid,                       

Edeine                     

Inhibit chain initiation,

 

Same         

 

Same

 

Same

Ricin

                                                                                                         

Alpha saracin                                                                                

Tetracycline                                                                                   

Puromycin                                                                                     

 

 

Inhibit tRNA binding,

 

 

Same,

 

Same,

 

Early termination

Amicitin

                                                                       

Anisomycin                                                                                    

Sparsomycin                                                                                  

 

 

Inhibit peptide bond formation,

 

Same,

 

Same

                                                                                                         

CHI                                                                                                  

Neomycin                                                                                       

Emetine                                                                                          

Diphtheria toxin                                                                            

 

 

Prevent translocation,

 

Same,

 

Same,

 

Same,

 

Same,

Erythromycin                                              

 

Hygromycin                                                                                  

 

 

Inhibits translocation on 60s,

Inhibits translocation