Publication
Polar Hinges as Functionalized Conformational Constraints in (Bi) cyclic Peptides
Publications associées (32)
Development 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 ...
EPFL2023Peptide-Hypervalent Iodine Reagent Chimeras: Enabling Peptide Functionalization and Macrocyclization
Jérôme Waser, Christian Heinis, Xinjian Ji, Xingyu Liu
Herein, we report a novel strategy for the modification of peptides based on the introduction of highly reactive hypervalent iodine reagents-ethynylbenziodoxolones (EBXs)-onto peptides. These peptide-EBXs can be readily accessed, by both solution- and soli ...
WILEY-V C H VERLAG GMBH2023Methods 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 ...
EPFL2021Hypervalent Iodine-Mediated Late-Stage Peptide and Protein Functionalization
Jérôme Waser, Elija Grinhagena, Emmanuelle Madeline Dominique Allouche
Hypervalent iodine compounds are powerful reagents for the development of novel transformations. As they exhibit low toxicity, high functional group tolerance, and stability in biocompatible media, they have been used for the functionalization of biomolecu ...
WILEY-V C H VERLAG GMBH2021A minimalistic cyclic ice-binding peptide from phage display
Harm-Anton Klok, Luciano Andres Abriata, Corey Alfred Stevens, Matthew Gibson, Xudong Kong
Developing molecules that emulate the properties of naturally occurring ice-binding proteins (IBPs) is a daunting challenge. Rather than relying on the (limited) existing structure–property relationships that have been established for IBPs, here we report ...
2021De novo development of proteolytically resistant therapeutic peptides for oral administration
Christian Heinis, Luciano Andres Abriata, Florence Pojer, Xudong Kong, Vanessa Carle, Jun Moriya
The oral administration of peptide drugs is hampered by their metabolic instability and limited intestinal uptake. Here, we describe a method for the generation of small target-specific peptides (less than 1,600 Da in size) that resist gastrointestinal pro ...
2020Crosslinking Allosteric Sites on the Nucleosome Core Particle
Designing compounds that bind to the acidic patch of the nucleosome core particle (NCP) is an emerging therapeutic approach that can inhibit the binding of key chromatin factors. Pretreatment of human ovarian carcinoma, A2780, cells with RAPTA-T, an antime ...
EPFL2019Development of cyclic peptide inhibitors of coagulation factor XII and matrix metalloproteinase 2
Peptides represent a promising molecular class for drug development. They combine several strengths of small molecules (e.g. efficient tissue diffusion, low immunogenicity and access to chemical synthesis) and key properties of biologics such as monoclonal ...
EPFL2018Development of an albumin-binding ligand for prolonging the plasma half-life of peptide therapeutics
Peptides represent a promising format for the development of therapeutics since they combine the advantages of proteins and small molecules. Several techniques based on rational design or in vitro evolution can be used to develop peptides as therapeutics. ...
EPFL2017Scanning tunneling microscopy on large bio-molecular systems on surfaces
The ever growing demand for the development of new technologies and materials has led to extensive studies inspired by biological functional complexes. Peptides with their outstanding ability to efficiently self-assemble can express a broad spectrum of int ...
EPFL2017