Publication
Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry
Publications associées (32)
Next-generation antimicrobials: from chemical biology to first-in-class drugs
The global emergence of multi-drug resistant bacteria invokes an urgent and imperative necessity for the identification of novel antimicrobials. The general lack of success in progressing novel chemical entities from target-based drug screens have prompted ...
Pharmaceutical Soc Korea2015Effects of physiological self-crowding of DNA on shape and biological properties of DNA molecules with various levels of supercoiling
Giovanni Dietler, Julien Dorier, Yannis Burnier, Fabrizio Benedetti, Andrzej Stasiak, Aleksandre Japaridze, Robert Sebastian Kwapich
DNA in bacterial chromosomes and bacterial plasmids is supercoiled. DNA supercoiling is essential for DNA replication and gene regulation. However, the density of supercoiling in vivo is circa twice smaller than in deproteinized DNA molecules isolated from ...
Oxford University Press2015Detection of Drug-Protein Interactions with an Improved Yeast Three-Hybrid System
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 ...
EPFL2013On the active site of mononuclear B1 metallo beta-lactamases: a computational study
Matteo Dal Peraro, Paolo Carloni
Metallo-beta-lactamases (M beta Ls) are Zn(II)-based bacterial enzymes that hydrolyze beta-lactam antibiotics, hampering their beneficial effects. In the most relevant subclass (B1), X-ray crystallography studies on the enzyme from point to either two zinc ...
2012Insights into Intrastrand Cross-Link Lesions of DNA from QM/MM Molecular Dynamics Simulations
Ursula Röthlisberger, Chandan Patel
DNA damages induced by oxidative intrastrand cross-links have been the subject of intense research during the past decade. Yet, the currently available experimental protocols used to isolate such lesions only allow to get structural information about linke ...
2012Study of Topoisomerase-DNA Interaction Using Atomic Force Microscopy
The aim of this thesis was to explore the topoisomerase-DNA interactions using atomic force microscopy (AFM) in a liquid environment. Firstly, we present a programmable microcontroller-driven injection system for the exchange of an imaging medium while usi ...
EPFL2012From hydrolytically labile to hydrolytically stable Ru(II)-arene anticancer complexes with carbohydrate-derived co-ligands
Paul Joseph Dyson, Christian Hartinger, Alexey Nazarov, Muhammad Hanif
The synthesis, characterization, reactivity and in vitro anticancer activity of a series of Ru-II-arene complexes with carbohydrate-derived phosphite and biscarboxylato co-ligands are reported. The compounds were characterized by NMR spectroscopy and elect ...
2011A Novel Yeast-Based Platform for Small Molecule Target Deconvolution Reveals Previously Unknown Binding Partners for the Approved Drugs Erlotinib, Atorvastatin, and Sulfasalazine
The identification of all protein targets of a small molecule drug, i.e. target deconvolution, provides the basis for understanding its beneficial or deleterious actions. Target deconvolution remains a major and often problematic task within the biotechnol ...
EPFL2010Small Molecule Based Approaches to Inhibit Macrophage Migration Inhibitory Factor (MIF) Activities and Elucidate its Role in Health and Disease
Macrophage migration inhibitory factor (MIF) is a major mediator in innate immunity and inflammation and a potential therapeutic target in multiple inflammatory, infectious and autoimmune diseases including cancer. Current therapeutic strategies for target ...
EPFL2010Hybrid Polymer Therapeutics Incorporating Bioresponsive, Coiled Coil Peptide Linkers
Nanopharmaceuticals or nanomedicines are defined as nanometer sized (1 to 1000 nm) complex systems, consisting of at least two components, one of which being the biologically active moiety such as a drug, peptide, protein or nucleotide. Several nano-sized ...
EPFL2010