A method to screen a wide variety of drug candidates without laborious purification steps could advance the fight against drug-resistant bacteria. Efforts to combat the increasing threat of drug-resistant bacteria are being assisted by a new approach for streamlining the search for antimicrobial drug candidates, pioneered by researchers at Hokkaido University, led by Assistant Professor Kazuki Yamamoto and Professor Satoshi Ichikawa of the Faculty of Pharmaceutical Sciences. Their methods, developed together with researchers elsewhere in Japan and in the USA, are discussed in an article in the journal Nature Communications .
Antimicrobial resistance (AMR) in bacteria poses a major and ever-increasing challenge to healthcare worldwide, leaving clinicians struggling to treat a wide range of serious and potentially fatal infections. One promising target for new drugs against a variety of AMR bacteria is an enzyme embedded in bacterial cell membranes called phospho- N -acetylmuramoyl-pentapeptide-transferase (MraY). This enzyme catalyzes formation of a specific lipid molecule, called lipid I, that is essential for bacteria to survive.
Several inhibitors of MraY activity are already known, but improved versions are urgently required. In this study, we used four known classes of MraY inhibitors that are used as antibiotics. We developed a drug discovery platform (in situ build-up library method) that combines a comprehensive synthesis method for natural product derivatives and dire.
