Publication
De novo developed small cyclic peptides that are orally available
Related publications (60)
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 Gmbh2024Methods 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 ...
EPFL2024Solid-phase peptide synthesis in 384-well plates
Christian Heinis, Edward Jeffrey Will, Anne Sofie Luise Zarda, Alexander Lund Nielsen, Sevan Mleh Habeshian, Mischa Schüttel, Gontran Sangouard
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 ...
Hoboken2024Synthesis and application of bifunctional hypervalent iodine reagents for peptide modification.
Protein-protein interactions (PPIs) are responsible for regulating many biological processes in human bodies. PPIs often have a large binding site and often interact through an alpha helical segment. Therefore, the inhibition of PPIs can be difficult using ...
EPFL2023Development of methods for the synthesis of large combinatorial libraries of macrocyclic compounds
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 ...
EPFL2023Development of cyclic peptides that can be administered orally to inhibit disease targets
Christian Heinis, Manuel Leonardo Merz
Cyclic peptides can bind challenging disease targets, but their oral application is hindered by digestion and absorption issues. We developed a versatile method for the synthesis and functional screening of vast numbers of synthetic cyclic peptides and ide ...
Berlin2023Generating 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 ...
EPFL2022Solid-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 CHEMISTRY2022Cyclative 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 ...
AMER CHEMICAL SOC2022Methods for the generation of large combinatorial macrocycle libraries
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