Publications related to IC50 | EPFL Graph Search

Development of cyclic peptides that can be administered orally to inhibit disease targets

Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...

2023

Assessment of metal-based dihydrofolate reductase inhibitors on a novel mesofluidic platform

Paul Joseph Dyson, Sarah Alexandra Pais Pereira

A new miniaturized micro sequential injection coupled with the lab-on-valve (mu SIA-LOV) technique was full-blown to perform inhibitory studies on dihydrofolate reductase (DHFR). The system was used to evaluate the DHFR inhibition activity of metal-based a ...

ELSEVIER SCIENCE SA2022

Azole-Based Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors

Pierre Vogel, Florence Pojer, Somi Reddy Majjigapu, George Coukos, Olivier Michielin

The heme enzyme indoleamine 2,3-dioxygenase 1 (IDO1) plays an essential role in immunity, neuronal function, and aging through catalysis of the rate-limiting step in the kynurenine pathway of tryptophan metabolism. Many IDO1 inhibitors with different chemo ...

AMER CHEMICAL SOC2021

Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

Hilal Lashuel, Anass Chiki

Huntington's disease (HD) is caused by a CAG trinucleotide repeat expansion in the first exon of the huntingtin (HTT) gene coding for the huntingtin (HTT) protein. The misfolding and consequential aggregation of CAG-expanded mutant HTT (mHTT) underpin HD p ...

Nature Portfolio2021

Degradation study on molecules released from laser-based jet injector

Christophe Moser, Jan Krizek, Barbora Lavickova

Development of needle-free methods to administer injectable therapeutics has been researched for a few decades. We focused our attention on a laser-based jet injection technique where the liquid-jet actuation mechanism is based on optical cavitation. This ...

2021

Impact of the skull contour definition on Leksell Gamma Knife(R)Icon (TM) radiosurgery treatment planning

Constantin Tuleasca

Introduction The Gamma Knife(R)planning software (TMR 10, Elekta Instruments, AB, Sweden) affords two ways of defining the skull volume, the "historical" one using manual measurements (still perform in some centers) and the new one using image-based skull ...

2020

Design and validation of bioorthogonal probes for cellular disease models

Pier Luca D'Alessandro

Well-validated chemical probes enable testing of biological hypotheses, investigation of target tractability and translatability to the clinical phase. Consequently, these important tool compounds play a key role in the drug discovery process. Moreover, th ...

EPFL2019

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

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

Label-Free Detection of Tobramycin in Serum by Transmission-Localized Surface Plasmon Resonance

Carlotta Guiducci, Thierry Buclin, Anna Ferretti, Giulia Cappi, Fabio Mario Spiga, Laurent Décosterd, Michael Beyeler

In order to improve the efficacy and safety of treatments, drug dosage needs to be adjusted to the actual needs of each patient in a truly personalized medicine approach. Key for widespread dosage adjustment is the availability of point-of-care devices abl ...

Amer Chemical Soc2015

Dose-response curve of a microfluidic magnetic bead-based surface coverage sandwich assay

Martinus Gijs, Thomas Lehnert, Matteo Cornaglia, Raphaël Etienne Jean Trouillon, Hüseyin Cumhur Tekin

Magnetic micro-and nanoparticles ('magnetic beads') have been used to advantage in many microfluidic devices for sensitive antigen (Ag) detection. Today, assays that use as read-out of the signal the number count of immobilized beads on a surface for quant ...

Elsevier2015

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

Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR

Geoffrey Bodenhausen, Sandrine Gerber, Aurélien Bornet, Jonas Milani, Sami Jannin, Basile Vuichoud, Solène Marcelle Françoise Marie Passemard, Nicola Salvi, Daniele Mammoli, Roberto Buratto, Maninder Singh, Aurélien Laguerre

Transverse and longitudinal relaxation times (T11 and T1) have been widely exploited in NMR to probe the binding of ligands and putative drugs to target proteins. We have shown recently that long-lived states (LLS) can be more sensitive to ligand binding. ...

Wiley-Blackwell2014

A new target for gold(I) compounds: glutathione-S.transferase inhibition by auranofin

Paul Joseph Dyson, Christian Hartinger, Angela Casini

Nowadays, gold compounds occupy a relevant position constituting a promising class of experimental anticancer metallodrugs. Several research efforts have been devoted to the investigations of the pharmacological properties of gold(I) complexes bearing phos ...

Elsevier Science Inc2013

Arene ruthenium dichloro complexes containing isonicotinic ester ligands: Synthesis, molecular structure and cytotoxicity

Paul Joseph Dyson, Olivier Pierre Zava

A series of p-cymene ruthenium dichloro complexes containing isonicotinic ester ligands, [(arene) RuCl2NC5H4-4-COO-C6H4-p-O-(CH2)(n)-CH3] (n = 1: 1, n = 3: 2, n = 5: 3, n = 7:4, n = 9: 5, n = 11: 6, n = 13: 7, n = 15: 8), were prepared from p-cymene ruthen ...

Elsevier2013

Personalized Drug Administrations Using Support Vector Machine

Giovanni De Micheli, Alena Simalatsar, Wenqi You Dubout

The decision-making process regarding drug dose, regularly used in everyday medical practice, is critical to patients’ health and recovery. It is a challenging process, especially for a drug with narrow therapeutic ranges, in which a medical doctor decides ...

2013

Metal-based Chemosensors for Carbohydrates and Biologically Important Ligands

Vera Janowski

Chemosensors based on indicator displacement were developed for the optical detection of different analytes in aqueous solution. The sensing of carbohydrates, including glucose, in aqueous solution at pH 7.4 was achieved by a fluorescent indicator displace ...

EPFL2012

Comparison of Three Methods of Biocompatible Multi-Walled Carbon Nanotubes Confinement for the Development of Implantable Amperometric Adenosine-5′-Triphosphate Biosensors

Giovanni De Micheli, Sandro Carrara, Andrea Cavallini

An amperometric biosensor for adenosine 5 -triphosphate (ATP) was developed applying a competitive assay of two glucose converting enzymes: glucose oxidase (GOD) and hexokinase (HEX). Competition between GOD and HEX for glucose in presence of ATP, lead to ...

American Scientific Publishers2011

An integrative in silico methodology for the identification of modulators of macrophage migration inhibitory factor (MIF) tautomerase activity

Hilal Lashuel, Bruno Claude Daniel Fauvet, Hajer Ouertatani-Sakouhi, Farah El Turk

Macrophage migration inhibitory factor (MIF) is a major proinflammatory cytokine that has been increasingly implicated in the pathogenesis of several inflammatory, autoimmune, infectious and oncogenic diseases. Accumulating evidence suggests that the tauto ...

Elsevier2010

Synthesis and glycosidase inhibitory activity of 1-amino-3,6-anhydro-1-deoxy-D-sorbitol derivatives

Pierre Vogel, Claudia Bello

3,6-Anhydro-1-(aryl or alkylamino)-1-deoxy-D-sorbitol derivatives have been prepared in four steps from isosorbide, a by-product from the starch industry. The inhibitory activities of these new compounds have been evaluated towards 13 glycosidases. A first ...

2010