Publication

Inhibition of Thiol‐Mediated Uptake with Irreversible Covalent Inhibitors

Publications associées (30)

A virtual screening approach to identifying the greenest compound for a task: application to switchable-hydrophilicity solvents

A virtual or in silico screening approach makes it much easier to identify the molecular structure that best combines efficacy for a specific task with safety and minimum environmental or health impacts. In this approach, software is used to generate a lar ...

Royal Soc Chemistry2015

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

Enzyme inhibition by metal complexes: concepts, strategies and applications

Paul Joseph Dyson, Kelly Joan Kilpin

Metal complexes are increasingly being used to inhibit enzymes. The reasons for this increased interest arise from the special features that metal complexes offer, e.g. the facile construction of 3D architectures that tightly fill enzyme active sites incre ...

2013

Monitoring proliferative activities of hormone-like odorants in human breast cancer cells by gene transcription profiling and electrical impedance spectroscopy

Horst Vogel, Samuel Terrettaz, Horst Pick, Olivia Baud, Cathrin Brisken

The human estrogen receptor alpha (ER!) mediates the proliferative action of hormones in breast cancer cells by regulating the expression of target genes to control cellular functions. Current methodologies do not permit a real-time assessment of these pro ...

Elsevier2013

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

Single-Cell Analysis of Mycobacterial Persistence Using Microfabricated Tools

Meltem Elitas

Bacterial cells behave as individuals despite being genetically identical and subject to the same environment. Although the underlying mechanisms of cellular individuality are not well understood, temporal variation of gene expression and protein levels in ...

EPFL2012

Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

Paul Joseph Dyson, Ursula Röthlisberger, Wee Han Ang, Pablo Campomanes Ramos

Platinum-based cancer drugs, such as cisplatin, are highly effective chemotherapeutic agents used extensively for the treatment of solid tumors. However, their effectiveness is limited by drug resistance, which, in some cancers, has been associated with an ...

Wiley-Blackwell2011

Thioredoxin reductase, an emerging target for anticancer metallodrugs

Angela Casini

Enzyme inhibition by cytotoxic gold(III) compounds studied with combined mass spectrometry and biochemical assays ...

2011

Elucidating the Role of Quaternary Structure in Modulating Macrophage Migration Inhibitory Factor (MIF) Functions

Farah El Turk

Macrophage Migration Inhibitory Factor (MIF) is a multifunctional protein and a major mediator of innate immunity. The paramount importance of MIF in the pathogenesis of many inflammatory, infectious, auto-immune and oncogenic diseases led to its emergence ...

EPFL2010

A Simple Model for Testing Drugs against Non-replicating Mycobacterium tuberculosis

Stewart Cole, Neeraj Dhar, Claudia Sala, Ruben Hartkoorn, Ming Zhang

Non-replicating or dormant cells of Mycobacterium tuberculosis constitute a challenge to tuberculosis (TB) therapy because of their tolerance or phenotypic resistance to most drugs. Here, we propose a simple model for testing drugs against non-growing cell ...

2010