Publications by Xudong Kong | EPFL Graph Search

Related publications (14)

Phage Selection of Cyclic Peptides for Application in Research and Drug Development

Christian Heinis, Xudong Kong, Kaycie Marie Butler

Cyclic peptides can bind to protein targets with high affinities and selectivities, which makes them an attractive modality for the development of research reagents and therapeutics. Additional properties, including low inherent toxicity, efficient chemica ...

American Chemical Society2017

De novo development of proteolytically resistant therapeutic peptides for oral administration

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

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, Kaycie Marie Butler, Jeremy Touati, Maola Khan Mohammad Golam, Michal Sabisz

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

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

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

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

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

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

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

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

A minimalistic cyclic ice-binding peptide from phage display

Harm-Anton Klok, Luciano Andres Abriata, 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

Phage Display Selection against a Mixture of Protein Targets

Christian Heinis, Xudong Kong

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

Precisely Regulated and Efficient Locking of Linear Peptides into Stable Multicyclic Topologies through a One-Pot Reaction

Christian Heinis, Xudong Kong

We report the discovery of a small phenyl molecule with four isosteric thiolate-reactive groups of sequentially varied reactivity. This molecule was exploited in combination with cysteine/penicillamine thiolates of different nucleophilic reactivity for pre ...

Wiley-Blackwell2017

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

Christian Heinis, Xudong Kong, Vanessa Carle, Alice Comberlato, 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

Bypassing bacterial infection in phage display by sequencing DNA released from phage particles

Christian Heinis, Xudong Kong, Camille Villequey

Phage display relies on a bacterial infection step in which the phage particles are replicated to perform multiple affinity selection rounds and to enable the identification of isolated clones by DNA sequencing. While this process is efficient for wild-typ ...

2017

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

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

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

Development of protease-resistant peptide ligands for oral delivery

Christian Heinis, Xudong Kong

WILEY2018

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

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

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