Ligand design for riboswitches, an emerging target class for novel antibiotics

Riboswitches are -acting gene regulatory elements and constitute potential targets for new antibiotics. Recent studies in this field have started to explore these targets for drug discovery. New ligands found by fragment screening, design of analogs of the natural ligands or serendipitously by pheno...

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Bibliographic Details
Published in:Future medicinal chemistry 2017-09, Vol.9 (14), p.1649-1662
Main Authors: Rekand, Illimar Hugo, Brenk, Ruth
Format: Article
Language:English
Subjects:
Animals
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
antibiotics
Bacteria - drug effects
Binding Sites
Drug Design
drug targets
Ligands
Molecular Dynamics Simulation
Riboswitch - drug effects
riboswitch ligands
riboswitches
RNA
Structure-Activity Relationship
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Summary:Riboswitches are -acting gene regulatory elements and constitute potential targets for new antibiotics. Recent studies in this field have started to explore these targets for drug discovery. New ligands found by fragment screening, design of analogs of the natural ligands or serendipitously by phenotypic screening have shown antibacterial effects in cell assays against a range of bacteria strains and in animal models. In this review, we highlight the most advanced drug design work of riboswitch ligands and discuss the challenges in the field with respect to the development of antibiotics with a new mechanism of action.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2017-0063