Concept

Thiol

Publications associées (64)

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

Large Libraries of Structurally Diverse Macrocycles Suitable for Membrane Permeation

Christian Heinis, Xinjian Ji, Edward Jeffrey Will, Anne Sofie Luise Zarda, Alessandro Angelini, Alexander Lund Nielsen, Manuel Leonardo Merz, Mischa Schüttel, Ganesh Kumar Mothukuri, Zsolt Bognár

Macrocycles offer an attractive format for drug development due to their good binding properties and potential to cross cell membranes. To efficiently identify macrocyclic ligands for new targets, methods for the synthesis and screening of large combinator ...

Wiley-V C H Verlag Gmbh2024

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

Christian Heinis

Tris-(2-carboxyethyl)phosphine (TCEP) linked to agarose beads is widely used for reducing disulfide bridges in proteins and peptides. The immobilization of TCEP on beads allows efficient removal after reduction to prevent its reaction with alkylating reage ...

Weinheim2023

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

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

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 ...

ROYAL SOC CHEMISTRY2022

Controlling lignin solubility and hydrogenolysis selectivity by acetal-mediated functionalization

Jeremy Luterbacher, Anastasiia Komarova, Graham Reid Dick

Existing lignocellulosic biomass fractionation processes produce lignin with random, interunit C-C bonds that inhibit its depolymerization and constrain its use. Here, we exploit the aldehyde stabilization of lignin to tailor its structure, functionality, ...

ROYAL SOC CHEMISTRY2021

The Effect of Thiol Structure on Allyl Sulfide Photodegradable Hydrogels and their Application as a Degradable Scaffold for Organoid Passaging

Matthias Lütolf, Nikolche Gjorevski

Intestinal organoids are useful in vitro models for basic and translational studies aimed at understanding and treating disease. However, their routine culture relies on animal-derived matrices that limit translation to clinical applications. In fact, ther ...

WILEY-V C H VERLAG GMBH2020

Ethynylation of Cysteine Residues: From Peptides to Proteins in Vitro and in Living Cells

Jérôme Waser, Romain Gaëtan Tessier, Charlotte Marie Sornay, Raj Kumar Nandi

Current approaches to introduce terminal alkynes for bioorthogonal reactions into biomolecules still present limitations in terms of either reactivity, selectivity, or adduct stability. We present a method for the ethynylation of cysteine residues based on ...

2020

Photocatalysis with organic dyes: facile access to reactive intermediates for synthesis

Jérôme Waser, Marion Marie-Agnès Garreau, Stephanie Grace Elizabeth Amos, Luca Buzzetti

Organic dyes have emerged as a reliable class of photoredox catalysts. Their great structural variety combined with the easy finetuning of their electronic properties has unlocked new possibilities for the generation of reactive intermediates. In this revi ...

2020

Reversibly Cross-Linking Polymer Brushes Using Interchain Disulfide Bonds

Harm-Anton Klok, Piotr Mocny

The introduction of interchain cross-links in surface-grafted polymer brushes increases the robustness and mechanical properties of these thin polymer films. In most cases, cross-linked polymer brushes contain permanent interchain cross-links. The use of r ...

AMER CHEMICAL SOC2020

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

Christian Heinis, Van Manh Pham

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 ...

2019

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