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Stewart Cole

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Publications associées (266)

Lansoprazole is an antituberculous prodrug targeting cytochrome bc1

Stewart Cole, Claudia Sala, Florence Pojer, Philippe Busso, Jan Lars Rybniker, Anthony Vocat, Andrej Benjak

Better antibiotics capable of killing multi-drug-resistant Mycobacterium tuberculosis are urgently needed. Despite extensive drug discovery efforts, only a few promising candidates are on the horizon and alternative screening protocols are required. Here, ...

Nature Publishing Group2015

Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-beta-D-ribose 2 '-oxidase

Stewart Cole, Florence Pojer, Anirban Ghosh, Joao Pedro De Almeida Neres

We report the discovery of benzothiazoles, a novel anti-mycobacterial series, identified from a whole cell based screening campaign. Benzothiazoles exert their bactericidal activity against Mycobacterium tuberculosis (Mtb) through potent inhibition of deca ...

Elsevier2015

In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis

Stewart Cole

Background Mycetoma is a neglected, chronic, and deforming infectious disease caused by fungi and actinomycetes. In Mexico, N. brasiliensis is the predominant etiologic agent. Therapeutic alternatives are necessary because the current drug regimens have se ...

Public Library of Science2015

Insight into the evolution and origin of leprosy bacilli from the genome sequence of Mycobacterium lepromatosis

Stewart Cole, Philippe Busso, Pushpendra Singh, Andrej Benjak, Charlotte Avanzi

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 Sciences2015

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG

Stewart Cole, Ruben Hartkoorn

To combat the emergence of drug-resistant strains of Mycobacterium tuberculosis, new antitubercular agents and novel drug targets are needed. Phenotypic screening of a library of 594 hit compounds uncovered two leads that were active against M. tuberculosi ...

Elsevier2015

Mycobacterium lepromatosis Infections in Nuevo Leon, Mexico

Stewart Cole, Philippe Busso, Pushpendra Singh, Andrej Benjak, Charlotte Avanzi

The frequency of infection caused by the recently described pathogen Mycobacterium lepromatosis is unknown. Here, we describe the demographics, clinical characteristics, and therapeutic outcomes of five lepromatous leprosy patients suffering from M. leprom ...

American Society for Microbiology2015

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library

Stewart Cole, Ruben Hartkoorn, Edina Rita Székely

Discovering new drugs to treat tuberculosis more efficiently and to overcome multidrug resistance is a world health priority. To find novel antitubercular agents several approaches have been used in various institutions worldwide, including target-based ap ...

Elsevier2015

Towards first in human clinical trial with the novel drug candidate PBTZ169

Stewart Cole, Benoit Lechartier, Jean-Yves Gillon

Wiley-Blackwell2015

Whole cell screen based identification of spiropiperidines with potent antitubercular properties

Stewart Cole, Ruben Hartkoorn

Whole cell based screens to identify hits against Mycobacterium tuberculosis (Mtb), carried out under replicating and non-replicating (NRP) conditions, resulted in the identification of multiple, novel but structurally related spiropiperidines with potent ...

Elsevier2015

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis

Gaëlle Séraphine Kolly, Stewart Cole, Ruben Hartkoorn, Joao Pedro De Almeida Neres, Anthony Vocat, Trent Michael Conroy, Jérémie Piton

8-Nitro-benzothiazinones (BTZs), such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-beta-D-ribose 2'-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. Structure-activity relationship (SAR) studie ...

American Society for Microbiology2015

Structure of EspB, a secreted substrate of the ESX-1 secretion system of Mycobacterium tuberculosis

Stewart Cole, Florence Pojer, Aleksandre Japaridze, Jérémie Piton

Mycobacterium tuberculosis secretes multiple virulence factors during infection via the general Sec and Tat pathways, and via specialized ESX secretion systems, also referred to as type VII secretion systems. The ESX-1 secretion system is an important viru ...

Elsevier2015

4-Pyrimidinylamino-benzenesulfonamide derivatives and their use for the inhibition of polo-like kinase 1 (PLK1) for the treatment of cancer and their use for the treatment of bacterial infections

Stewart Cole, Ruben Hartkoorn, Edina Rita Székely

The present invention relates to 4-pyrimidinylamino-benzenesulfonamide derivatives of general formula (I) and pharmaceutically acceptable salts, solvates, hydrates, regioisomeric and polymorphic forms thereof, processes for manufacturing of them, the use o ...

2015

Zoonotic Leprosy in the Southeastern United States

Stewart Cole, Pushpendra Singh, Rahul Sharma

Nine-banded armadillos (Dasypus novemcinctus) are naturally infected with Mycobacterium leprae and have been implicated in zoonotic transmission of leprosy. Early studies found this disease mainly in Texas and Louisiana, but armadillos in the southeastern ...

Centers Disease Control2015

Functional Dissection of Intersubunit Interactions in the EspR Virulence Regulator of Mycobacterium tuberculosis

Giovanni Dietler, Benjamin Blasco, Stewart Cole, Florence Pojer, Matteo Dal Peraro, Basile Isidore Martin Wicky, Aleksandre Japaridze, Marco Stenta

The nucleoid-associated protein EspR, a chromosome organizer, has pleiotropic effects on expression of genes associated with cell wall function and pathogenesis in Mycobacterium tuberculosis. In particular, EspR binds to several sites upstream of the espAC ...

American Society for Microbiology2014

Genome-wide re-sequencing of multidrug-resistant Mycobacterium leprae Airaku-3

Stewart Cole, Jacques Rougemont, Philippe Busso, Pushpendra Singh, Andrej Benjak, Charlotte Avanzi

Genotyping and molecular characterization of drug resistance mechanisms in Mycobacterium leprae enables disease transmission and drug resistance trends to be monitored. In the present study, we performed genome-wide analysis of Airaku-3, a multidrug-resist ...

Wiley-Blackwell2014

Mycobacterium leprae genomes from a British medieval leprosy hospital: towards understanding an ancient epidemic

Stewart Cole, Pushpendra Singh

Background: Leprosy has afflicted humankind throughout history leaving evidence in both early texts and the archaeological record. In Britain, leprosy was widespread throughout the Middle Ages until its gradual and unexplained decline between the 14th and ...

Biomed Central Ltd2014

Cross-Resistance between Clofazimine and Bedaquiline through Upregulation of MmpL5 in Mycobacterium tuberculosis

Stewart Cole, Swapna Uplekar, Ruben Hartkoorn

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 Microbiology2014

The cysteine desulfurase IscS of Mycobacterium tuberculosis is involved in iron sulfur cluster biogenesis and oxidative stress defence

Gaëlle Séraphine Kolly, Stewart Cole, Florence Pojer, Jeffrey Chen, Jan Lars Rybniker

The complex multiprotein systems for the assembly of protein-bound iron sulfur (Fe S) clusters are well defined in Gram-negative model organisms. However, little is known about Fe S cluster biogenesis in other bacterial species. The ISC (iron sulfur cluste ...

Portland Press2014

Pyridomycin bridges the NADH- and substratebinding pockets of the enoyl reductase InhA

Stewart Cole, Florence Pojer, Ruben Hartkoorn, Joao Pedro De Almeida Neres

Pyridomycin, a natural product with potent antituberculosis activity, inhibits a major drug target, the InhA enoyl reductase. Here, we unveil the co-crystal structure and unique ability of pyridomycin to block both the NADH cofactor- and lipid substrate-bi ...

Nature Publishing Group2014

Tuberculosis drug discovery in the post-post-genomic era

Stewart Cole, Benoit Lechartier, Jan Lars Rybniker

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 Access2014

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