Publications de Zsolt Bognár | EPFL Graph Search

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

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-VCH Verlag GmbH2024

Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

Gerardo Turcatti, Christian Heinis, Julien Bortoli Chapalay, Jonathan Patrice Vesin, Alessandro Angelini, Manuel Leonardo Merz, Sevan Mleh Habeshian, Mischa Schüttel, Ganesh Kumar Mothukuri, Gontran Sangouard

Macrocycles have excellent potential as therapeutics due to their ability to bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome this, ...

Nature Research2022

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