Publications by Xudong Kong | EPFL Graph Search

Phage Display Selection against a Mixture of Protein Targets

Affinity selections by phage display or other display techniques are typically performed against single targets immobilized as a purified protein. In order to develop cross-specific binders that engage with multiple proteins, such as members of a related f ...

American Chemical Society (ACS)2025

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

Generation of a 100-billion cyclic peptide phage display library having a high skeletal diversity

Christian Heinis, Xudong Kong, Alice Comberlato, Vanessa Carle, Cristina Diaz Perlas

Phage display is a powerful technique routinely used for the generation of peptide- or protein-based ligands. The success of phage display selections critically depends on the size and structural diversity of the libraries, but the generation of large libr ...

2021

A minimalistic cyclic ice-binding peptide from phage display

Harm-Anton Klok, Luciano Andres Abriata, Matthew Gibson, Xudong Kong, Corey Alfred Stevens

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 ...

Nature Research2021

Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation

Christian Heinis, Chloé Rogg, Xudong Kong, Vanessa Carle, Cristina Diaz Perlas, Camille Villequey, Tamara Maric, Kaycie Marie Butler, Christina Lamers

Coagulation factor XI (FXI) has emerged as a promising target for the development of safer anticoagulation drugs that limit the risk of severe and life-threatening bleeding. Herein, we report the first cyclic peptide-based FXI inhibitor that selectively an ...

2021

Generation of a Large Peptide Phage Display Library by Self-Ligation of Whole-Plasmid PCR Product

Christian Heinis, Xudong Kong, Vanessa Carle, Cristina Diaz Perlas, Kaycie Marie Butler

The success of phage display, used for developing target-specific binders based on peptides and proteins, depends on the size and diversity of the library screened, but generating large libraries of phage-encoded polypeptides remains challenging. New pepti ...

2020

Cyclic peptide FXII inhibitor provides safe anticoagulation in a thrombosis model and in artificial lungs

Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Simon Jan Middendorp, Patrick Andreas Gonschorek, Christina Lamers

Inhibiting thrombosis without generating bleeding risks is a major challenge in medicine. A promising solution may be the inhibition of coagulation factor XII (FXII), because its knock-out or inhibition in animals reduced thrombosis without causing abnorma ...

Nature Research2020

De novo development of proteolytically resistant therapeutic peptides for oral administration

Christian Heinis, Luciano Andres Abriata, Florence Pojer, Xudong Kong, Vanessa Carle, Kaycie Marie Butler, 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 ...

2020

Engineered peptide macrocycles can inhibit matrix metalloproteinases with high selectivity

Christian Heinis, Xudong Kong, Jonas Alfred Karl Wilbs, Jeremy Touati, Maola Khan Mohammad Golam, Michal Sabisz, Alice Baumann, Kaycie Marie Butler

Matrix metalloproteinases (MMPs) are zinc‐dependent endopeptidases at the intersection of health and disease due to their involvement in processes such as tissue repair and immunity as well as cancer and inflammation. Because of the high structural conserv ...

2019

Thiol-to-amine cyclization reaction enables screening of large libraries of macrocyclic compounds and the generation of sub-kilodalton ligands

Christian Heinis, Gerardo Turcatti, Julien Bortoli Chapalay, Xudong Kong, Van Manh Pham, Patrick Andreas Gonschorek, Jonathan Patrice Vesin, Sangram Shivdas Kale, Milan Bergeron-Brlek, João Miguel Franco Machado

Macrocyclic compounds are an attractive modality for drug development, but the limited availability of large, structurally diverse macrocyclic libraries hampers the discovery of leads. Here, we describe the discovery of efficient macrocyclization reactions ...

2019