A5049727251- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
- Biochemical and Molecular Research
- Mycobacterium research and diagnosis
- Bioactive Compounds and Antitumor Agents
- Microbial Natural Products and Biosynthesis
Inserm
2017-2022
Centre Hospitalier Universitaire de Lille
2017-2022
Université de Lille
2017-2022
Centre National de la Recherche Scientifique
2017-2022
Center for Infection and Immunity of Lille
2017-2022
Institut Pasteur de Lille
2017-2022
Antibiotic resistance is one of the biggest threats to human health globally. Alarmingly, multidrug-resistant and extensively drug-resistant Mycobacterium tuberculosis have now spread worldwide. Some key antituberculosis antibiotics are prodrugs, for which mechanisms mainly driven by mutations in bacterial enzymatic pathway required their bioactivation. We developed drug-like molecules that activate a cryptic alternative bioactivation ethionamide M. tuberculosis, circumventing classic...
The sensitivity of Mycobacterium tuberculosis , the pathogen that causes (TB), to antibiotic prodrugs is dependent on efficacy activation process transforms into their active antibacterial moieties. Various oxidases M. have potential activate prodrug ethionamide. Here, we used medicinal chemistry coupled with a phenotypic assay select N-acylated 4-phenylpiperidine compound series. lead compound, SMARt751, interacted transcriptional regulator VirS which regulates mymA operon encoding...
Killing more than one million people each year, tuberculosis remains the leading cause of death from a single infectious agent. The growing threat multidrug-resistant strains Mycobacterium stresses need for alternative therapies. EthR, mycobacterial transcriptional regulator, is involved in control bioactivation second-line drug ethionamide. We have previously reported discovery vitro nanomolar boosters ethionamide through fragment-based approaches. In this study, we further explored...