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Related publications (69)

A microfluidics platform for combinatorial drug screening on cancer biopsies

Screening drugs on patient biopsies from solid tumours has immense potential, but is challenging due to the small amount of available material. To address this, we present here a plug-based microfluidics platform for functional screening of drug combinatio ...

2018

Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria

Paul Joseph Dyson, Stewart Cole, John McKinney, Neeraj Dhar, Thierry Laroche, Jérémie Piton, Joao Pedro De Almeida Neres, Raphael Christopher Sommer, Raju Mukherjee

Benzothiazinones (BTZ) are highly potent bactericidal inhibitors of mycobacteria and the lead compound, BTZ043, and the optimized drug candidate, PBTZ169, have potential for the treatment of tuberculosis. Here, we exploited the tractability of the BTZ scaf ...

2018

Microfluidic high-content phenotypic screening on a Caenorhabditis elegans model

Maria Cristina Letizia

Caenorhabditis elegans is a performant model system for studying human biological processes and diseases and for pre-clinical phenotyping screenings of compounds. Microfluidics has been instrumental in enabling C. elegans-based drug assays, facilitating th ...

EPFL2018

A design of experiment approach for efficient multi-parametric drug testing using a Caenorhabditis elegans model

Martinus Gijs, Matteo Cornaglia, Raphaël Etienne Jean Trouillon, Maria Cristina Letizia, Giuseppe Tranchida

When studying the drug effectiveness towards a target model, one should distinguish the effects of the drug itself and of all the other factors that could influence the screening outcome. This comprehensive knowledge is crucial, especially when model organ ...

2018

Arylvinylpiperazine Amides, a New Class of Potent Inhibitors Targeting QcrB of Mycobacterium tuberculosis

Stewart Cole, Andrej Benjak, Anthony Vocat, Jérémie Piton, Shi-Yan Caroline Foo, Andréanne Lupien, Raphael Christopher Sommer

New drugs are needed to control the current tuberculosis (TB) pandemic caused by infection with Mycobacterium tuberculosis. We report here on our work with AX-35, an arylvinylpiperazine amide, and four related analogs, which are potent antitubercular agent ...

AMER SOC MICROBIOLOGY2018

Computational design of environmental sensors for the potent opioid fentanyl

Kai Johnsson, Luc Reymond

We describe the computational design of proteins that bind the potent analgesic fentanyl. Our approach employs a fast docking algorithm to find shape complementary ligand placement in protein scaffolds, followed by design of the surrounding residues to opt ...

Elife Sciences Publications Ltd2017

Inhibiting Mycobacterium tuberculosis within and without

Stewart Cole

Tuberculosis remains a scourge of global health with shrinking treatment options due to the spread of drug-resistant strains of Mycobacterium tuberculosis. Intensive efforts have been made in the past 15 years to find leads for drug development so that bet ...

Royal Soc2016

New optical tools for non-invasive imaging and quantification of glucose and nicotinamide riboside in living cells and animals

Aleksandra Konovalova

Glucose is one of the most important metabolites that plays a key role in living organisms, as it is the primary energy source. Glucose metabolism is also an integral part in the pathogenesis of diabetes and cancer. Despite this tremendous impact of glucos ...

EPFL2016

SIRT2-and NRF2-Targeting Thiazole-Containing Compound with Therapeutic Activity in Huntington's Disease Models

Heike Runne

There are currently no disease-modifying therapies for the neurodegenerative disorder Huntington's disease (HD). This study identified novel thiazole-containing inhibitors of the deacetylase sirtuin-2 (SIRT2) with neuroprotective activity in ex vivo brain ...

Cell Press2016

Development of Stapling Methods by Selective Side Chain Modifications of Bioactive Peptides

Christopher Matthew Bandeli Kourra

Cyclic peptide therapeutics fill the gap between small molecules (5000 Da) as a separate class of drugs, combining the advantages of both in terms of high selectivity, bioavailability, synthetic accessibility and low toxicity. Howe ...

EPFL2016

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