Elfamycins: inhibitors of elongation factor-Tu.

Mol Microbiol

Division of Pulmonology, Allergy/Immunology, Cystic Fibrosis and Sleep, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.

Published: October 2017

AI Article Synopsis

  • Elfamycins are a lesser-known group of antibiotics that interrupt the translation process by affecting EF-Tu function, primarily used in labs to study these mechanisms rather than as effective medications.* -
  • Their poor pharmacokinetic properties and solubility have limited their utility as therapies, but the increasing problem of antibiotic resistance is prompting a reevaluation of their potential.* -
  • Research efforts include discovering new natural variants and improving existing compounds, with LFF571, a modified version of GE2270 A, successfully completing phase 2 clinical trials, indicating a promising future for elfamycins in antibiotic treatment.*

Article Abstract

Elfamycins are a relatively understudied group of antibiotics that target the essential process of translation through impairment of EF-Tu function. For the most part, the utility of these compounds has been as laboratory tools for the study of EF-Tu and the ribosome, as their poor pharmacokinetic profile and solubility has prevented implementation as therapeutic agents. However, due to the slowing of the antibiotic pipeline and the rapid emergence of resistance to approved antibiotics, this group is being reconsidered. Some researchers are using screens for novel naturally produced variants, while others are making directed, systematic chemical improvements on publically disclosed compounds. As an example of the latter approach, a GE2270 A derivative, LFF571, has completed phase 2 clinical trials, thus demonstrating the potential for elfamycins to become more prominent antibiotics in the future.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5701666PMC
http://dx.doi.org/10.1111/mmi.13750DOI Listing

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