Publications by Julien Bortoli Chapalay

Related publications (7)

An optimized and validated 384-well plate assay to test platelet function in a high-throughput screening format

Nikolaos Stergiopoulos, Olivier Burri, Rodrigo Araujo Fraga Da Silva, Marc Chambon, Augusto Martins Lima, Maiia Bragina, Julien Bortoli Chapalay

Despite significant advances in the treatment of cardiovascular diseases, antiplatelet therapies are still associated with a high risk of hemorrhage. In order to develop new drugs, methods to measure platelet function must be adapted for the high-throughpu ...

TAYLOR & FRANCIS INC2019

Loss of Bacterial Cell Pole Stabilization in Caulobacter crescentus Sensitizes to Outer Membrane Stress and Peptidoglycan-Directed Antibiotics

Gerardo Turcatti, Marc Chambon, Julien Bortoli Chapalay

Rod-shaped bacteria frequently localize proteins to one or both cellpoles in order to regulate processes such as chromosome replication or polar organ-elle development. However, the roles of polar factors in responses to extracellularstimuli have been gene ...

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

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

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

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

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

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

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

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

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

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

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

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