title: [Novel targets for antibiotics discovery: riboswitches].
abstract: Riboswitches are cis-acting domains located in mRNA sequences that could regulate gene expression by sensing small molecules without employing protein. Most known riboswitches in bacteria have naturally evolved to bind essential metabolite ligands and are involved in the regulation of critical genes that are responsible for the biosynthesis or transport of the cognate ligand. The riboswitch-mediated gene expression could be repressed by metabolite analogs, which caused bacterial growth inhibition or even death. A number of leading compounds targeting riboswitches have been discovered. A promising avenue for the development of new class of riboswitch-based antibiotics has been opened. Herein we reviewed the current findings of riboswitches that served as targets for antibacterial drug development and the underlying mechanisms. The development of high-throughput methods and rational drug design for riboswitch-specific drug discovery are relevant challenges are discussed. summarized.
authors.affiliation: Institute of Molecular Medicine, Huaqiao University, Quanzhou 362021, China.
authors.forename: Dong-fang
authors.initials: DF
authors.lastname: Jia
authors.affiliation: Institute of Molecular Medicine, Huaqiao University, Quanzhou 362021, China.
authors.forename: Dong-fang
authors.initials: DF
authors.lastname: Jia
authors.affiliation: Institute of Molecular Medicine, Huaqiao University, Quanzhou 362021, China.
authors.forename: Dong-fang
authors.initials: DF
authors.lastname: Jia
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects / Q000235:genetics; D001426:Bacterial Proteins / Q000737:chemistry / Q000235:genetics; D015195:Drug Design; D055808:Drug Discovery; D005486:Flavin Mononucleotide / Q000737:chemistry / Q000235:genetics; D015964:Gene Expression Regulation, Bacterial; D006147:Guanine / Q000737:chemistry; D057166:High-Throughput Screening Assays / Q000379:methods*; D008024:Ligands; D008239:Lysine / Q000031:analogs & derivatives / Q000737:chemistry / Q000235:genetics; D058928:Riboswitch / Q000187:drug effects; D013834:Thiamine Pyrophosphatase / Q000737:chemistry / Q000235:genetics; D005945:Glutamine-Fructose-6-Phosphate Transaminase (Isomerizing)
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D005486:Flavin Mononucleotide; D006147:Guanine; D008024:Ligands; D008239:Lysine; D058928:Riboswitch; D013834:Thiamine Pyrophosphatase; C000731191:component S, glutamate mutase protein, Bacteria; D005945:Glutamine-Fructose-6-Phosphate Transaminase (Isomerizing)