Publication

De novo development of proteolytically resistant therapeutic peptides for oral administration

Publications associées (45)

Synthesis 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 ...

EPFL2023

High-affinity peptides developed against calprotectin and their application as synthetic ligands in diagnostic assays

Christian Heinis, Florence Pojer, Kelvin Ka Ching Lau, Lluc Farrera Soler, Cristina Diaz Perlas

A peptide was developed that binds to calprotectin, a marker of major inflammatory disorders, and found to be suited for diagnostic tests. The use of synthetic peptides in assays is of great interest due to their high precision, robustness and low price. C ...

NATURE PORTFOLIO2023

Development 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 ...

Berlin2023

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

Towards the Development of Orally Available Peptide Therapeutics

Christian Heinis, Xudong Kong

Peptides have a number of attractive properties that make them an interesting modality for drug development, including their ability to bind challenging targets, their high target specificity, and their non-toxic metabolic products. However, a major limita ...

2021

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

Molecular basis for inhibition of adhesin-mediated bacterial-host interactions through a peptide-binding domain

Corey Alfred Stevens

Infections typically begin with pathogens adhering to host cells. For bacteria, this adhesion can occur through specific ligand-binding domains. We identify a 20-kDa peptide-binding domain (PBD) in a 1.5-MDa RTX adhesin of a Gram-negative marine bacterium ...

CELL PRESS2021

A 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 ...

2021

NCoR1 Protects Mice From Dextran Sodium Sulfate Induced Colitis by Guarding Colonic Crypt Cells From Luminal Insult

Johan Auwerx

BACKGROUND & AIMS: Colonic stem cells are essential for producing the mucosal lining, which in turn protects stem cells from insult by luminal factors. Discovery of genetic and biochemical events that control stem cell proliferation and differentiation can ...

2020

Bile Acids Signal via TGR5 to Activate Intestinal Stem Cells and Epithelial Regeneration

Kristina Schoonjans, Alessia Perino, Maroun Bou Sleiman, Giovanni Sorrentino, Ece Yildiz, Gaby El Alam

BACKGROUND & AIMS: Renewal and patterning of the intestinal epithelium is coordinated by intestinal stem cells (ISCs); dietary and metabolic factors provide signals to the niche that control ISC activity. Bile acids (BAs), metabolites in the gut, signal nu ...

2020

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