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Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

Sara Vigne

Polymer-block-peptide conjugates are tailored to render hydrophobic small molecule drugs water soluble. The combinatorial strategy selects for bioconjugates that exhibit sequence-specific solubilization and switchable release profiles of the cargo through ...

Wiley-V C H Verlag Gmbh2015

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

Automated multi-parameter measurement of cardiomyocytes dynamics with digital holographic microscopy

Gerardo Turcatti, Benjamin Rappaz, Pierre Marquet

Compounds tested during drug development may have adverse effects on the heart; therefore all new chemical entities have to undergo extensive preclinical assessment for cardiac liability. Conventional intensity-based imaging techniques are not robust enoug ...

Optical Society of America2015

Simple and Rapid Method To Determine Antimycobacterial Potency of Compounds by Using Autoluminescent Mycobacterium tuberculosis

Neeraj Dhar, Ekaterina Gelman

A major obstacle in the process of discovery of drugs against Mycobacterium tuberculosis is its extremely slow growth rate and long generation time (similar to 20 to 24 h). Consequently, determination of MICs and minimum bactericidal concentrations (MBCs) ...

Amer Soc Microbiology2014

Exploring Weak Ligand-Protein Interactions by Long-Lived NMR States: Improved Contrast in Fragment-Based Drug Screening

Geoffrey Bodenhausen, Daniele Mammoli, Roberto Buratto

Ligands that have an affinity for protein targets can be screened very effectively by exploiting favorable properties of long-lived states (LLS) in NMR spectroscopy. In this work, we describe the use of LLS for competitive binding experiments to measure ac ...

Wiley-Blackwell2014

Assessing the essentiality of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants

Stewart Cole, John McKinney, Claudia Sala, Neeraj Dhar, Ruben Hartkoorn, Gaëlle Séraphine Kolly

In Mycobacterium tuberculosis the decaprenyl-phospho-d-arabinofuranose (DPA) pathway is a validated target for the drugs ethambutol and benzothiazinones. To identify other potential drug targets in the pathway, we generated conditional knock-down mutants o ...

Wiley-Blackwell2014

Abcb4 acts as multixenobiotic transporter and active barrier against chemical uptake in zebrafish (Danio rerio) embryos

Kristin Schirmer

Background: In mammals, ABCB1 constitutes a cellular "first line of defense" against a wide array of chemicals and drugs conferring cellular multidrug or multixenobiotic resistance (MDR/MXR). We tested the hypothesis that an ABCB1 ortholog serves as protec ...

Biomed Central Ltd2013

Detection of Drug-Protein Interactions with an Improved Yeast Three-Hybrid System

Cindy Fellay

The identification of the targets of therapeutic drugs is one of the major challenges for pharmaceutical companies. The main target responsible for drug action is often known, but most drugs also bind other targets, either causing deleterious side effects ...

EPFL2013

Highly efficient production of the Alzheimer's γ-Secretase integral membrane protease complex by a multi-gene stable integration approach

Florian Maria Wurm, David Hacker, Lorène Aeschbach, Patrick Fraering, Mitko Dimitrov, Sowmya Balasubramanian

Inefficient production of membrane-embedded multi-protein complexes by conventional methods has largely prevented the generation of high-resolution structural information and the performance of high-throughput drug discovery screens for this class of prote ...

2013

Probing Odorant-Mediated Receptor Activation

Olivia Baud

Molecular interactions of odorants with their olfactory receptors (ORs) are of central importance for the mammalian olfactory system to detect and discriminate a large variety of odors with a limited set of receptors. How a particular OR binds and distingu ...

EPFL2012

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