Publications de Stewart Cole | EPFL Graph Search

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

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

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, Jérémie Piton, Aleksandre Japaridze

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

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

Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis

Stewart Cole, Benoit Lechartier

Clofazimine (CZM) is an antileprosy drug that was recently repurposed for treatment of multidrug-resistant tuberculosis. In Mycobacterium tuberculosis, CZM appears to act as a prodrug, which is reduced by NADH dehydrogenase (NDH-2), to release reactive oxy ...

Amer Soc Microbiology2015

Zoonotic Leprosy in the Southeastern United States

Stewart Cole, Rahul Sharma, Pushpendra Singh

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

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

Combined Measurement of the Higgs Boson Mass in $pp$ Collisions at $\sqrt{s}=7$ and 8 TeV with the ATLAS and CMS Experiments

Jian Wang, Matthias Finger, Lesya Shchutska, Qian Wang, Yiming Li, Matthias Wolf, Varun Sharma, Konstantin Androsov, Jan Steggemann, Leonardo Cristella, Stewart Cole, Roberto Castello, Alessandro Degano, Xin Chen, James Henderson, Sofia Vallecorsa, Lulu Liu, Yi Jiang, Clement Helsens, Christophe Clément, Snezana Nektarijevic, Valerio Rossetti, Mingkui Wang, Zhirui Xu, Chao Wang, João Miguel das Neves Duarte, Lei Zhang, Tian Cheng, Yixing Chen, Werner Lustermann, Andromachi Tsirou, Alexis Kalogeropoulos, Andrea Rizzi, Ioannis Papadopoulos, Paolo Ronchese, Thomas Muller, Ho Ling Li, Giuseppe Codispoti, Hua Zhang, Siyuan Wang, Peter Hansen, Daniel Gonzalez, Greig Alan Cowan, Michele Bianco, Sun Hee Kim, Hang Yin, Paul Turner, Wei Sun, Preema Rennee Pais, Raffaele Tito D'Agnolo, Maria Elena Stramaglia, Songmei Wu, Tommaso Colombo, Federica Legger, Yu Bai, Géraldine Conti, Dong Liu, John Wilson, Jin Wang, Stefano Rosati, Sven Kreiss, Jun Guo, Andreas Alexander Maier, Lorenzo Massa, Lei Zhou, Nicolas Berger, Stefan Simion, Ruslan Mashinistov, Ourania Sidiropoulou, Peter Lichard, Eduardo Ros, Susan Cheatham, Ji Hyun Kim, Donghyun Kim, Dipanwita Dutta, Zheng Wang, Sanjeev Kumar, Wei Li, Yong Yang, Geng Chen, Ajay Kumar, Ashish Sharma, Georgios Anagnostou, Joao Varela, Csaba Hajdu, Muhammad Ahmad, Ekaterina Kuznetsova, Ioannis Evangelou, Matthias Weber, Muhammad Shoaib, Milos Dordevic, Vineet Kumar, Vladimir Petrov, Francesco Fiori, Quentin Python, Meng Xiao, Hao Liu, Sourav Sen, Yanlin Liu, Viktor Khristenko

A measurement of the Higgs boson mass is presented based on the combined data samples of the ATLAS and CMS experiments at the CERN LHC in the

H \rightarrow \gamma\gamma

and

H \rightarrow ZZ\rightarrow 4\ell

decay channels. The results are obtained from ...

2015

2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1

Stewart Cole, Neeraj Dhar, Florence Pojer, Ruben Hartkoorn, Gaëlle Séraphine Kolly, Joao Pedro De Almeida Neres

Phenotypic screening of a quinoxaline library against replicating Mycobacterium tuberculosis led to the identification of lead compound Ty38c (3-((4-methoxybenzyl)amino)-6-(trifluoromethyl)quinoxaline-2-carboxylic acid). With an MIC99 and MBC of 3.1 mu M, ...

American Chemical Society2015

GtrA Protein Rv3789 Is Required for Arabinosylation of Arabinogalactan in Mycobacterium tuberculosis

Stewart Cole, Matteo Dal Peraro, Luciano Andres Abriata, Claudia Sala, Gaëlle Séraphine Kolly, Mahé Cécile Raccaud, Raju Mukherjee

Mycobacterium tuberculosis possesses a thick and highly hydrophobic cell wall principally composed of a mycolyl-arabinogalactan-peptidoglycan complex, which is critical for survival and virulence. DprE1 is a well-characterized component of decaprenyl-phosp ...

Amer Soc Microbiology2015

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, Joao Pedro De Almeida Neres, Anirban Ghosh

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