Publications associées à High-Density Immobilization of TCEP on Silica Beads for Efficient Disulfide Reduction and Thiol Alkylation in Peptides

Methods for high-throughput synthesis and screening of peptide libraries

Macrocycles provide an attractive modality for drug development but the identification of ligands to targets of interest is hindered by the lack of large macrocyclic compound libraries for high-throughput screening. A strategy to efficiently synthesize lar ...

EPFL2024

Solid-phase peptide synthesis in 384-well plates

Christian Heinis, Gontran Sangouard, Mischa Schüttel, Sevan Mleh Habeshian, Edward Jeffrey Will, Alexander Lund Nielsen, Anne Sofie Luise Zarda

Newer solid-phase peptide synthesis and release strategies enable the production of short peptides with high purity, allowing direct screening for desired bioactivity without prior chromatographic purification. However, the maximum number of peptides that ...

2024

Development of methods for the synthesis of large combinatorial libraries of macrocyclic compounds

Mischa Schüttel

Macrocycles have raised much interest in the pharmaceutical industry due to their ability to bind challenging targets while often still being able to cross membranes to reach intracellular proteins. However, the development of macrocyclic ligands to new di ...

EPFL2023

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

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

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

Cyclative Release Strategy to Obtain Pure Cyclic Peptides Directly from the Solid Phase

Christian Heinis, Manuel Leonardo Merz, Sevan Mleh Habeshian, Ganesh Ashokrao Sable

The synthesis of large numbers of cyclic peptides-required, for example, in screens for drug development-is currently limited by the need of chromatographic purification of individual peptides. Herein, we have developed a strategy in which cyclic peptides ...

2022

Characterization of water sorption cycle in the cement microstructure of controlled oxide composition

Monisha Rastogi

This thesis investigates the water vapour sorption behaviour of samples with maximized calcium-silicate-hydrate (C-S-H) content. Primarily, the role of heterogeneous and homogeneous cavitation has been studied during the drying of cementitious materials. C ...

EPFL2022

Abnormal temperature dependent elastic properties of fused silica irradiated by ultrafast lasers

Yves Bellouard, Pieter Vlugter

Materials with thermal-invariant elastic properties are of interest for resonant device frequency and dimensional stability of precision devices. Here, we demonstrate that the temperature coefficient of elasticity (TCE) of amorphous silica can be locally r ...

2022

Strong silicon oxide inclusions in iron

Andreas Mortensen, Léa Deillon, Alejandra Inés Slagter, Joris Pierre Everaerts

Oxide inclusions are ubiquitous in steel and are known to affect, generally in a negative sense, the mechanical performance of steel products. Micromechanical properties of those phases are therefore important, yet they have remained largely unexplored. We ...

2022

Effect of different ions on dissolution rates of silica and feldspars at high pH

Karen Scrivener, Barbara Lothenbach, Mahsa Bagheri, Mahdieh Shakoorioskooie

The dissolution kinetics of silica-containing minerals in aggregates influences strongly the process of ASR in concrete. In this paper, the effect of different ions on the dissolution rates of SiO2 (amorphous and quartz) and feldspars at high pH values was ...

Pergamon-Elsevier Science Ltd2022

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

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

Amphiphilic Iodine(III) Reagents for the Lipophilization of Peptides in Water

Jérôme Waser, Durga Prasada Rao Hari, Romain Gaëtan Tessier, Abhaya Kumar Mishra

We report the functionalization of cysteine residues with lipophilic alkynes bearing a silyl group or an alkyl chain using amphiphilic ethynylbenziodoxolone reagents (EBXs). The reactions were carried out in buffer (pH 6 to 9), without organic co-solvent o ...

Wiley-VCH Verlag GmbH2021

Grafting of Alkali Metals on Fumed Silica for the Catalytic Dehydrogenation of Methanol to Formaldehyde

Christophe Jean Baranowski, Oliver Kröcher, Alimohammad Bahmanpour, Jack Brandon

Water free, non-oxidative catalytic dehydrogenation of methanol to formaldehyde is an important process for the formation of anhydrous, molecular formaldehyde (FA). Sodium or sodium-containing salts were shown to catalyze the reaction, but their reaction m ...

Wiley-VCH Verlag2021

A smart low molecular weight gelator for the triple detection of copper (II), mercury (II), and cyanide ions in water resources

Rosario Scopelliti

Novel supramolecular gelators based on quinoline-indolin-2-one structure were synthesized. These gelators formed stable organogels in a mixture of DMSO/H2O (1:1). The scanning electron microscopy (SEM), IR and NMR spectroscopies, and rheological measuremen ...

ELSEVIER2020

Synthesis of DNA‐encoded disulfide‐ and thioether‐cyclized peptides

Christian Heinis, Van Manh Pham, Milan Bergeron-Brlek

DNA-encoded chemical library technologies enable the screening of large combinatorial libraries of chemically and structurally diverse molecules, including short cyclic peptides. A challenge in the combinatorial synthesis of cyclic peptides is the final st ...

2020

Influence of curing temperature on cement paste microstructure measured by H-1 NMR relaxometry

Karen Scrivener, Arnaud Charles Albert Muller

H-1 nuclear magnetic resonance (NMR) relaxometry, supported by X-Ray diffraction and thermogravimetric analysis, has been used to characterise microstructure of white cement pastes underwater cured at temperatures in the range 10 degrees C to 60 degrees C. ...

Pergamon-Elsevier Science Ltd2019

Water Redistribution-Microdiffusion in Cement Paste under Mechanical Loading Evidenced by H-1 NMR

Karen Scrivener, Pietro Lura

The mobility of water within the microstructure of hardened cement paste has been at the center of a long-lasting debate, motivated by the need to understand the fundamental mechanisms that play a role in drying, shrinkage, creep, and thermal expansion. Ou ...

2019

Application of Hypervalent Iodine Reagents for Novel Cysteine Labeling

Romain Gaëtan Tessier

Selective functionalization of peptides and proteins has always been a valuable tool for the study and manipulation of biological processes. In this context, cysteines are of particular interest. Their intrinsic high nucleophilicity makes these amino acids ...

EPFL2019

C-Terminal Bioconjugation of Peptides through Photoredox Catalyzed Decarboxylative Alkynylation

Jérôme Waser, Franck Le Vaillant, Marion Marie-Agnès Garreau

We report the first decarboxylative alkynylation of the C-terminus of peptides starting from free carboxylic acids. The reaction is fast, metal-free, and proceeds cleanly to afford alkynylated peptides with a broad tolerance for the C-terminal amino acid. ...

Wiley-VCH Verlag GmbH2019

Slowing the Kinetics of Alumina Sol-Gel Chemistry for Controlled Catalyst Overcoating and Improved Catalyst Stability and Selectivity

Jeremy Luterbacher, Florent Emmanuel Héroguel, Yuan-Peng Du

Catalyst overcoating is an emerging approach to engineer surface functionalities on supported metal catalyst and improve catalyst selectivity and durability. Alumina deposition on high surface area material by sol–gel chemistry is traditionally difficult t ...

2018