Publications by Jonathan Patrice Vesin

Identification of glutathione transferase (GST P1) inhibitors via a high-throughput screening assay and implications as alternative treatment options for breast cancers

Gerardo Turcatti, Marc Chambon, Jonathan Patrice Vesin, Paul Joseph Dyson

Glutathione S-transferase P1-1 (GST P1) is an important drug target as it is implicated in drug resistance. GST P1-1 inhibitors are typically non-productive analogues of glutathione which covers broad chemical space; hence it is likely that several clinica ...

Public Library of Science (PLoS)2025

Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Angelini, Gontran Sangouard, Julien Bortoli Chapalay, Mischa Schüttel, Ganesh Kumar Mothukuri, Manuel Leonardo Merz, Sevan Mleh Habeshian, Cristina Diaz Perlas, Zsolt Bognár

Macrocycles have excellent potential as therapeutics due to their ability to bind challenging targets. However, generating macrocycles against new targets is hindered by a lack of large macrocycle libraries for high-throughput screening. To overcome this, ...

Nature Research2022

Picomole-Scale Synthesis and Screening of Macrocyclic Compound Libraries by Acoustic Liquid Transfer

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Zorzi, Gontran Sangouard, Julien Bortoli Chapalay, Sangram Shivdas Kale, Mischa Schüttel, Yu Teng Wu, Cristina Diaz Perlas

Macrocyclic compounds are an attractive class of therapeutic ligands against challenging targets, such as protein-protein interactions. However, the development of macrocycles as drugs is hindered by the lack of large combinatorial macrocyclic libraries, w ...

Wiley-VCH Verlag GmbH2021

Highly Potent Host-Specific Small-Molecule Inhibitor of Paramyxovirus and Pneumovirus Replication with High Resistance Barrier

Gerardo Turcatti, Marc Chambon, Damiano Banfi, Jonathan Patrice Vesin

Multiple enveloped RNA viruses of the family Paramyxoviridae and Pneumoviridae, like measles virus (MeV), Nipah virus (NiV), canine distemper virus (CDV), or respiratory syncytial virus (RSV), are of high clinical relevance. Each year a huge number of live ...

AMER SOC MICROBIOLOGY2021

Antiviral Screen against Canine Distemper Virus-Induced Membrane Fusion Activity

Gerardo Turcatti, Marc Chambon, Jonathan Patrice Vesin

Canine distemper virus (CDV), a close relative of the human pathogen measles virus (MeV), is an enveloped, negative sense RNA virus that belongs to the genus Morbillivirus and causes severe diseases in dogs and other carnivores. Although the vaccination is ...

2021

Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

Gerardo Turcatti, Jonathan Patrice Vesin, Christian Heinis, Alessandro Angelini, Alessandro Zorzi, Julien Bortoli Chapalay, Sangram Shivdas Kale, Kaycie Marie Butler, Ganesh Kumar Mothukuri, Carl Leonard Stenbratt

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...

2020

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

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

A Universal Assay for Aminopeptidase Activity and Its Application for Dipeptidyl Peptidase-4 Drug Discovery

Gerardo Turcatti, Marc Chambon, Jonathan Patrice Vesin, Elena Goun, Arkadiy Bazhin, Julien Bortoli Chapalay, James William Collins

Aminopeptidases, such as dipeptidyl peptidase 4 (DPP-4, CD26), are potent therapeutic targets for pharmacological interventions because they play key roles in many important pathological pathways. To analyze amino-peptidase activity in vitro (including hig ...

AMER CHEMICAL SOC2019