Abstract
Since the pioneering discovery of the inhibitory effects of kirromycin on bacterial elongation factor Tu (EF-Tu) more than 25 years ago [1], a great wealth of biological data has accumulated concerning protein biosynthesis inhibitors specific for EF-Tu. With the subsequent discovery of over two dozen naturally occurring EF-Tu inhibitors belonging to four different subclasses, EF-Tu has blossomed into an appealing antimicrobial target for rational drug discovery efforts. Very recently, independent crystal structure determinations of EF-Tu in complex with two potent antibiotics, aurodox and GE2270A, have provided structural explanations for the mode of action of these two compounds, and have set the foundation for the design of inhibitors with higher bioavailability, broader spectra, and greater efficacy.
Keywords: Inhibitory Mechanisms, Antibiotics Targeting Elongation Factor Tu, thermus thermophilus, the kirromycine, pulvomycin, cyclic thiazolyls, enacyloxin lla, planobispora rosea cinnamoneus, nocardialactamdurans, streptomyces, ramocissimus
Current Protein & Peptide Science
Title: Inhibitory Mechanisms of Antibiotics Targeting Elongation Factor Tu
Volume: 3 Issue: 1
Author(s): T. Hogg, J. R. Mesters and R. Hilgenfeld
Affiliation:
Keywords: Inhibitory Mechanisms, Antibiotics Targeting Elongation Factor Tu, thermus thermophilus, the kirromycine, pulvomycin, cyclic thiazolyls, enacyloxin lla, planobispora rosea cinnamoneus, nocardialactamdurans, streptomyces, ramocissimus
Abstract: Since the pioneering discovery of the inhibitory effects of kirromycin on bacterial elongation factor Tu (EF-Tu) more than 25 years ago [1], a great wealth of biological data has accumulated concerning protein biosynthesis inhibitors specific for EF-Tu. With the subsequent discovery of over two dozen naturally occurring EF-Tu inhibitors belonging to four different subclasses, EF-Tu has blossomed into an appealing antimicrobial target for rational drug discovery efforts. Very recently, independent crystal structure determinations of EF-Tu in complex with two potent antibiotics, aurodox and GE2270A, have provided structural explanations for the mode of action of these two compounds, and have set the foundation for the design of inhibitors with higher bioavailability, broader spectra, and greater efficacy.
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Cite this article as:
Hogg T., Mesters R. J. and Hilgenfeld R., Inhibitory Mechanisms of Antibiotics Targeting Elongation Factor Tu, Current Protein & Peptide Science 2002; 3 (1) . https://dx.doi.org/10.2174/1389203023380855
DOI https://dx.doi.org/10.2174/1389203023380855 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
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