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Multimodal imaging and high-throughput image-processing for drug screening on living organisms on-chip

Publications associées (62)

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Benchmarking is a crucial step in evaluating virtual screening methods for drug discovery. One major issue that arises among benchmarking data sets is a lack of a standardized format for representing the protein and ligand structures used to benchmark the ...

2020

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Bimolecular fluorescence complementation (BiFC) was introduced a decade ago as a method to monitor alpha-synuclein (alpha-syn) oligomerization in intact cells. Since then, several alpha-syn BiFC cellular assays and animal models have been developed based o ...

2020

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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

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The nematode Caenorhabditis elegans is a suitable model organism in drug screening. Traditionally worms are grown on agar plates, posing many challenges for long-term culture and phenotyping of animals under identical conditions. Microfluidics allows for ' ...

2019

A novel cell-based sensor detecting the activity of individual basic proprotein convertases

Daniel Constam, Stefan Kunz

The basic proprotein convertases (PCs) furin, PC1/3, PC2, PC5/6, PACE4, PC4, and PC7 are promising drug targets for human diseases. However, developing selective inhibitors remains challenging due to overlapping substrate recognition motifs and limited str ...

WILEY2019

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

Nikolaos Stergiopoulos, Olivier Burri, Marc Chambon, Julien Bortoli Chapalay, Fabiana Pereira Da Costa Fraga, Augusto Martins Lima, Maiia Bragina

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

Studying the roundworm Caenorhabditis elegans using microfluidic chips

Martinus Gijs

C. elegans is an attractive model organism in biology, as it shows genetic similarity with humans, facilitates microscopic observation due to its transparency, and has a short life cycle. Moreover, many mutants expressing fluorescent proteins in particular ...

SPIE-INT SOC OPTICAL ENGINEERING2019

Integration of microfluidics and multimodal optics for translational bioanalytics

Daniel Migliozzi

Numerous analytical techniques for life sciences have been at the basis of the improvement of medical diagnostics and treatments. Current challenges in bioanalytics are related to the conception of methods enabling large amount of information to be extract ...

EPFL2019

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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

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

Gerardo Turcatti, Julien Bortoli Chapalay, Xudong Kong, Van Manh Pham, Patrick Andreas Gonschorek, 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