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Related publications (31)

Discovery of novel competitive dihydropteridine reductase inhibitors via high throughput screening and their effect on metabolic pterin balance of fibroblast

Yann Mathieu Pierson

The development of tool compounds for the study of the tetrahydrobiopterin (BH4) metabolic network perturbation is of interest especially in the case of oxidative and nitrosative stress genesis. A semisynthetic FRET sensor was engineered in order to study ...

EPFL2018

More Medicines for Tuberculosis: Fuelling Drug Discovery against Mycobacterium tuberculosis

Shi-Yan Caroline Foo

Tuberculosis (TB), whose etiological agent is Mycobacterium tuberculosis (M. tuberculosis), has plagued humanity since antiquity. Even with chemotherapy available today, TB is the leading cause of death due to an infectious disease. Modern day factors, suc ...

EPFL2018

Optimized Background Regimen for Treatment of Active Tuberculosis with the Next-Generation Benzothiazinone Macozinone (PBTZ169)

Stewart Cole, Anthony Vocat, Shi-Yan Caroline Foo, Andréanne Lupien, Jean-Yves Gillon

The efficacy of the standardized four-drug regimen (comprising isoniazid, rifampin, pyrazinamide, and ethambutol) for the treatment of tuberculosis (TB) is menaced by the emergence of multidrug-resistant (MDR) and extensively drugresistant (XDR) strains of ...

AMER SOC MICROBIOLOGY2018

Improvement of a Closed Chest Porcine Myocardial Infarction Model by Standardization of Tissue and Blood Sampling Procedures

Jonas Alfred Karl Wilbs

Myocardial ischemia reperfusion (I/R) injury contributes to almost half of the necrotic area after myocardial infarction. To date there is no approved drug to prevent or reduce myocardial I/R injury. The study and understanding of the pathophysiological me ...

JOURNAL OF VISUALIZED EXPERIMENTS2018

Mining the Potential of Label-Free Biosensors for In Vitro Antipsychotic Drug Screening

Sandro Carrara, Tugba Kilic, Hatice Altug, Maria Soler Aznar

The pharmaceutical industry is facing enormous challenges due to high drug attribution rates. For the past decades, novel methods have been developed for safety and efficacy testing, as well as for improving early development stages. In vitro screening met ...

2018

Direct amidation of esters with nitroarenes

Xile Hu, Chi Wai Cheung, Marten Leendert Ploeger

Esters are one of the most common functional groups in natural and synthetic products, and the one-step conversion of the ester group into other functional groups is an attractive strategy in organic synthesis. Direct amidation of esters is particularly ap ...

Nature Publishing Group2017

Real-time binding kinetics of ligand-receptor interactions : development and application of a label-free optical biosensor for living bacteria

Ekaterina Rostova

In principle, a major goal in drug development is to design a high-affinity compound with an appropriate pharmacological response, which requires understanding of physical processes underlying the drug-target interaction, affinity and specificity. This dru ...

EPFL2017

Therapeutic Proteins Engineered for Super-Affinity to the Extracellular Matrix in Regenerative Medicine

Priscilla Suhasna Maithili Briquez

Regenerative medicine aims to repair body tissues when natural mechanisms fail. Growth factors (GFs) are essential proteins that promote tissue regeneration upon injury, and as such, are very promising therapeutic drugs in regenerative medicine. Due to the ...

EPFL2016

Review of the role played by the photosensitizer's photobleaching during photodynamic therapy

Georges Wagnières, Matthieu Philippe Emmanuel Zellweger

Photodynamic therapy (PDT) is based on the combined administration of photosensitizing drugs and light to treat a variety of malignant, pre-malignant and also non-malignant diseases. The reactive species resulting from the excitation of the photosensitizer ...

Natl Inst Optoelectronics2016

Homogeneous time-resolved G protein-coupled receptor-ligand binding assay based on fluorescence cross-correlation spectroscopy

Luc Henry

G protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic target classes for a wide spectrum of diseases. Drug discovery projects generally benefit from a broad range of ...

Academic Press Inc Elsevier Science2016

Preclinical combination therapy of the investigational drug NAMI-A(+) with doxorubicin for mammary cancer

Paul Joseph Dyson, Tina Riedel, Gianni Sava

Aim of the study The tumor metastases targeting ruthenium complex NAMI-A synergistically improves the activity of gemcitabine in combination therapies. High-throughput screening was used to identify other potential drug combinations from a library of FDA a ...

Springer2015

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