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Chemical Compound Review

Enacyloxin iia     (1S,3R,4S)-3-[ (2E,4E,6E,8E,10Z,12S,13R,14S. ..

Synonyms: AC1NRAYQ, ENX
 
 
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Disease relevance of Enacyloxin iia

 

High impact information on Enacyloxin iia

  • Thus, enacyloxin IIa can affect both EF-Tu and the ribosomal A-site directly, inducing an anomalous positioning of aa-tRNA, that inhibits the incorporation of the amino acid into the polypeptide chain [3].
  • Enacyloxin IIa, an inhibitor of protein biosynthesis that acts on elongation factor Tu and the ribosome [3].
  • Enacyloxin IIa [IC50 on poly(Phe) synthesis approximately 70 nM] is shown to affect the interaction between elongation factor (EF) Tu and GTP or GDP; in particular, the dissociation of EF-Tu-GTP is strongly retarded, causing the Kd of EF- Tu-GTP to decrease from 500 to 0.7 nM [3].
  • Enacyloxin IIa inhibits bacterial protein synthesis by hindering the release of EF-Tu.GDP from the ribosome [4].
  • Enacyloxin IIa pinpoints a binding pocket of elongation factor Tu for development of novel antibiotics [4].
 

Biological context of Enacyloxin iia

  • GTP; (ii) by enabling the release of enacyloxin IIa after GTP hydrolysis; and (iii) by reducing the affinity of EF-Tu.GDP. enacyloxin IIa for aminoacyl-tRNA at the ribosomal A-site, which then allows the release of EF-Tu.GDP.enacyloxin IIa [1].
 

Associations of Enacyloxin iia with other chemical compounds

 

Gene context of Enacyloxin iia

  • Among the mutant EF-Tus, three different resistance mechanisms can be distinguished: (i) by obstructing enacyloxin IIa binding to EF-Tu [1].

References

  1. Mutant EF-Tu species reveal novel features of the enacyloxin IIa inhibition mechanism on the ribosome. Zuurmond, A.M., Olsthoorn-Tieleman, L.N., Martien de Graaf, J., Parmeggiani, A., Kraal, B. J. Mol. Biol. (1999) [Pubmed]
  2. New polyenic antibiotics active against gram-positive and gram-negative bacteria. IV. Structural elucidation of enacyloxin IIa. Watanabe, T., Sugiyama, T., Takahashi, M., Shima, J., Yamashita, K., Izaki, K., Furihata, K., Seto, H. J. Antibiot. (1992) [Pubmed]
  3. Enacyloxin IIa, an inhibitor of protein biosynthesis that acts on elongation factor Tu and the ribosome. Cetin, R., Krab, I.M., Anborgh, P.H., Cool, R.H., Watanabe, T., Sugiyama, T., Izaki, K., Parmeggiani, A. EMBO J. (1996) [Pubmed]
  4. Enacyloxin IIa pinpoints a binding pocket of elongation factor Tu for development of novel antibiotics. Parmeggiani, A., Krab, I.M., Watanabe, T., Nielsen, R.C., Dahlberg, C., Nyborg, J., Nissen, P. J. Biol. Chem. (2006) [Pubmed]
  5. Functional role of the noncatalytic domains of elongation factor Tu in the interactions with ligands. Cetin, R., Anborgh, P.H., Cool, R.H., Parmeggiani, A. Biochemistry (1998) [Pubmed]
 
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