Publications associées à Bibliothèque publique

Generating macrocyclic inhibitors of protein-protein interactions

Protein-protein interactions (PPIs) play important roles in many diseases and their modulation is an attractive strategy for developing new therapeutics. However, the relatively large and often flat binding surfaces of PPIs makes the development of inhibit ...

EPFL2022

De novo developed small cyclic peptides that are orally available

Manuel Leonardo Merz

Cyclic peptides are ring-shaped molecules that emerged as a promising class of therapeutics. While it is often difficult to find small molecule binders for challenging disease targets, cyclic peptides can bind to featureless surfaces or inhibit protein-pro ...

EPFL2022

Solid-phase peptide synthesis on disulfide-linker resin followed by reductive release affords pure thiol-functionalized peptides

Christian Heinis, Zsolt Bognár, Alexander Lund Nielsen, Manuel Leonardo Merz, Ganesh Kumar Mothukuri, Peter Matei Frisius Pânzar

Thiol groups are suitable handles for site-selectively modifying, immobilizing or cyclizing individual peptides or entire peptide libraries. A limiting step in producing the thiol-functionalized peptides is the chromatographic purification, which is partic ...

2022

Enclosure: Language-Based Restriction of Untrusted Libraries

James Richard Larus, Mathias Josef Payer, Edouard Bugnion, Evangelos Marios Kogias, Adrien Ghosn

Programming languages and systems have failed to address the security implications of the increasingly frequent use of public libraries to construct modern software. Most languages provide tools and online repositories to publish, import, and use libraries ...

ACM2021

Methods for the generation of large combinatorial macrocycle libraries

Sevan Mleh Habeshian

Macrocycles are an attractive class of molecules due to their good binding properties and yet rather small size that allows, in many cases, crossing membranes to reach intracellular targets. In comparison to classical small molecule drugs, macrocycles are ...

EPFL2021

Le maker, construction d’une figure politique de l’innovation en Chine urbaine

Florence Graezer Bideau, Clément Luc Guillaume Renaud

En Chine, les politiques urbaines se construisent autour d’une transition industrielle du modèle Made in China vers une nouvelle modernité centrée sur l’innovation technologique. Les discours accompagnant ces vastes réformes mettent en scène de nouvelles f ...

Association Espaces Temps2020

Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

Christian Heinis, Gerardo Turcatti, Julien Bortoli Chapalay, Xudong Kong, Van Manh Pham, Patrick Andreas Gonschorek, Jonathan Patrice Vesin, Sangram Shivdas Kale, Milan Bergeron-Brlek, João Miguel Franco Machado

Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions ...

2019

A sequence-dependent coarse-grain model of B-DNA with explicit description of bases and phosphate groups parametrised from large scale Molecular Dynamics simulations

Alessandro Samuele Patelli

We introduce a sequence-dependent coarse-grain model of double-stranded DNA with an explicit description of both the bases and the phosphate groups as interacting rigid-bodies. The model parameters are trained on extensive, state-of-the-art large scale mol ...

EPFL2019

Rational design of a high-throughput droplet sorter

Tobias Schneider, Simon Sebastian Schütz

The high-throughput selection of individual droplets is an essential function in droplet-based microfluidics. Fluorescence-activated droplet sorting is achieved using electric fields triggered at rates up to 30 kHz, providing the ultra-high throughput rele ...

2019

SMoTherSpectre: Exploiting Speculative Execution through Port Contention

Babak Falsafi, Mathias Josef Payer, Atri Bhattacharyya

Spectre, Meltdown, and related attacks have demonstrated that kernels, hypervisors, trusted execution environments, and browsers are prone to information disclosure through micro-architectural weaknesses. However, it remains unclear as to what extent other ...

ACM2019

New Techniques for the Digitization of Art Historical Photographic Archives - the Case of the Cini Foundation in Venice

Frédéric Kaplan, Isabella Di Lenardo, Benoît Laurent Auguste Seguin

Numerous libraries and museums hold large art historical photographic collections, numbering millions of images. Because of their non-standard format, these collections pose special challenges for digitization. This paper address these difficulties by prop ...

2018

Synthesis of cyclic peptide disulfide-PHPMA conjugates via sequential active ester aminolysis and CuAAC coupling

Harm-Anton Klok

Cyclic peptide disulfides (CXC) are an important class of biomolecules. The conjugation of cyclic peptide disulfides to synthetic polymers, however, is often difficult due to the presence of the disulfide bond combined with other potentially reactive side ...

Royal Society of Chemistry2016

Live mammalian cell arrays

Matthias Lütolf, Sebastian Maerkl, Samy Gobaa, Kristina Pan Woodruff, Luis Miguel Fidalgo Rabanera

High-content assays have the potential to drastically increase throughput in cell biology and drug discovery, but handling and culturing large libraries of cells such as primary tumor or cancer cell lines requires expensive, dedicated robotic equipment. We ...

Nature Publishing Group2013

Indole Alkaloids Synthesis via a Selective Cyclization of Aminocyclopropanes

Jérôme Waser, Filippo De Simone

The continuous progress in medicinal chemistry requires more versatile synthetic strategies for the generation of large libraries of active compounds and their analogues. As a result, the research for new effective cyclization and cycloaddition reactions i ...

2012

On-line monitoring of nine different batch cultures of E-coli by mid-infrared spectroscopy, using a single spectra library for calibration

Urs von Stockar, Ian William Marison, Jonas Schenk, Carla Viscasillas Nadal

A single spectra library was used to monitor on-line, by mid-infrared spectroscopy, nine different batch cultures of Escherichia coli performed with various medium compositions, including chemically complex formulations. Whereas the classic chemometrics ap ...

2008