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Detalle de: A Simple Structural-Based Approach to Prevent Aminoglycoside Inactivation by Bacterial Defense Proteins. Conformational Restriction Provides Effective Protection against Neomycin-B Nucleotidylation by ANT4

Title A Simple Structural-Based Approach to Prevent Aminoglycoside Inactivation by Bacterial Defense Proteins. Conformational Restriction Provides Effective Protection against Neomycin-B Nucleotidylation by ANT4
Abstract

Herein, we describe how the conformational differences exhibited by aminoglycosides in the binding pockets of the ribosome and those enzymes involved in bacterial resistance can be exploited in the design of new antibiotic derivatives with improved activity in resistant strains. The simple modification shown in the figure, leading to the conformationally restricted 5, provides an effective protection against aminoglycoside inactivation by Staphylococcus aureus ANT4, both in vivo and in vitro.

Apa Reference Asensio, J.L., Hidalgo, A., Bastida, A., Torrado, M., Corzana, F., Chiara, J.L., García-Junceda, E., Cañada, J. & Jiménez-Barbero, J. (2005). A Simple Structural-Based Approach to Prevent Aminoglycoside Inactivation by Bacterial Defense Proteins. Conformational Restriction Provides Effective Protection against Neomycin-B Nucleotidylation by ANT4. Journal of the American Chemical Society, 127(23), 8278-8279. 10.1021/ja051722z
Doi 10.1021/ja051722z
Publication Date 17 May 2005
Publication Type Article
Researcher Agatha Bastida
Ontology Molecular flexibility
Research Groups
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