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Elfamycins: inhibitors of elongation factor-Tu.

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.

SUBMITTER: Prezioso SM

PROVIDER: S-EPMC5701666 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Elfamycins: inhibitors of elongation factor-Tu.

Prezioso Samantha M SM Brown Nicole E NE Goldberg Joanna B JB

Molecular microbiology 20170809 1

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 gro ...[more]

PMID: 28710887

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