Publication
Whole cell screen based identification of spiropiperidines with potent antitubercular properties
Publications associées (66)
Insight into the evolution and origin of leprosy bacilli from the genome sequence of Mycobacterium lepromatosis
Stewart Cole, Andrej Benjak, Charlotte Avanzi, Philippe Busso, Pushpendra Singh
Mycobacterium lepromatosis is an uncultured human pathogen associated with diffuse lepromatous leprosy and a reactional state known as Lucio's phenomenon. By using deep sequencing with and without DNA enrichment, we obtained the near-complete genome sequen ...
National Academy of Sciences2015Tuberculosis drug discovery in the post-post-genomic era
Stewart Cole, Jan Lars Rybniker, Benoit Lechartier
The expectation that genomics would result in new therapeutic interventions for infectious diseases remains unfulfilled. In the post-genomic era, the decade immediately following the availability of the genome sequence of Mycobacterium tuberculosis, tuberc ...
Wiley Open Access20144-Aminoquinolone Piperidine Amides: Noncovalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity
John McKinney, Neeraj Dhar, Joao Pedro De Almeida Neres, François Signorino-Gelo
4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaffold starting from a whole cell screen, with potent cidality on Mycobacterium tuberculosis (Mtb). Evaluation of the minimum inhibitory concentrations, followed by whole genome sequenci ...
Amer Chemical Soc2014Genetic analysis of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis
The tuberculosis (TB) epidemic still represents a major global health problem as it kills more than one million people every year. Africa and Asia are arguably the most affected regions due to the dramatic increase of TB cases in HIV-positive patients and ...
EPFL2014Mechanism of Action of 5-Nitrothiophenes against Mycobacterium tuberculosis
On using the streptomycin-starved 18b strain as a model for nonreplicating Mycobacterium tuberculosis, we identified a 5-nitrothiophene compound as highly active but not cytotoxic. Mutants resistant to 5-nitrothiophenes were found be cross-resistant to the ...
Amer Soc Microbiology2014A Single-Cell Perspective on Non-Growing but Metabolically Active (NGMA) Bacteria
A long-standing and fundamental problem in microbiology is the non-trivial discrimination between live and dead cells. The existence of physically intact and possibly viable bacterial cells that fail to replicate during a more or less protracted period of ...
Springer-Verlag2014Cross-Resistance between Clofazimine and Bedaquiline through Upregulation of MmpL5 in Mycobacterium tuberculosis
Stewart Cole, Ruben Hartkoorn, Swapna Uplekar
The antileprosy drug clofazimine is also of interest for the treatment of multidrug-resistant tuberculosis. To understand possible resistance mechanisms, clofazimine-resistant Mycobacterium tuberculosis mutants were isolated in vitro, and, unexpectedly, fo ...
Amer Soc Microbiology2014Genome-wide comparison of medieval and modern Mycobacterium leprae
Stewart Cole, Andrej Benjak, Philippe Busso, Pushpendra Singh
Leprosy was endemic in Europe until the Middle Ages. Using DNA array capture, we have obtained genome sequences of Mycobacterium leprae from skeletons of five medieval leprosy cases from the United Kingdom, Sweden, and Denmark. In one case, the DNA was so ...
Amer Assoc Advancement Science2013A Single-Cell Perspective on Non-Growing but Metabolically Active (NGMA) Bacteria
A long-standing and fundamental problem in microbiology is the non-trivial discrimination between live and dead cells. The existence of physically intact and possibly viable bacterial cells that fail to replicate during a more or less protracted period of ...
Springer Verlag2013Identification of a small molecule with activity against drug-resistant and persistent tuberculosis
Jian Wang, Yi Zhang, Claudia Trefzer, Ji Hyun Kim
A cell-based phenotypic screen for inhibitors of biofilm formation in mycobacteria identified the small molecule TCA1, which has bactericidal activity against both drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb) and sterilizes Mtb in vitro ...
National Academy of Sciences2013