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Expanding the Search for Small-molecule Antibacterials by Multidimensional Profiling by Karin Ortmayr; Roberto de la Cruz Moreno; Mattia Zampieri is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Beyond growth inhibition Early identification of antimicrobial targets. Because essentiality is condition-dependent , the translational relevance of in vitro susceptibility screens (Figs. ) hinges on the availability of experimental models that can mimic in vivo environments and interactions with the host. Environmental conditions can be so important that clinically relevant antibiotics, while potent antibacterials in vivo, exhibit poor activity in standard laboratory conditions. An emblematic example is daptomycin, for which the use of synthetic media with physiological concentrations of calcium is sufficient to reduce its minimum inhibitory concentration almost by 100-fold with respect to standard Mueller-Hinton broth . Conversely, compounds with promising in vitro activity, such as pyrimidine-imidazole derivatives, can target processes that become dispensable in vivo 5 . Thus, standard in vitro growth assays do not adequately evaluate the in vivo antimicrobial potential of bioactive small molecules, and screening for growth inhibitory compounds in rich laboratory conditions that fail to reproduce host environments can miss attractive antibiotic candidates or potential strategies

Who reads Expanding the Search for Small-molecule Antibacterials by Multidimensional Profiling?

Author

Karin Ortmayr; Roberto de la Cruz Moreno; Mattia Zampieri

Publisher

Springer Science and Business Media LLC

Published

2022

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)