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Designing focused chemical libraries enriched in protein-protein interaction inhibitors using machine-learning methods.

Christelle Reynès , Hélène Host , Anne-Claude Camproux , Guillaume Laconde , Florence Leroux , et al.
PLoS Computational Biology, 2010, 6 (3), pp.e1000695. ⟨10.1371/journal.pcbi.1000695⟩
Journal articles inserm-00705646v1
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Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches

Baptiste Villemagne , Marion Flipo , Nicolas Blondiaux , Celine Crauste , Sandra Malaquin , et al.
Journal of Medicinal Chemistry, 2014, 57 (11), pp.4876-4888. ⟨10.1021/jm500422b⟩
Journal articles hal-02309782v1

Beyond the Rule of 5: Impact of PEGylation with Various Polymer Sizes on Pharmacokinetic Properties, Structure–Properties Relationships of mPEGylated Small Agonists of TGR5 Receptor

Vanessa Hoguet , Manuel Lasalle , Mathieu Maingot , Geoffroy Dequirez , Rajaa Boulahjar , et al.
Journal of Medicinal Chemistry, 2021, 64 (3), pp.1593-1610. ⟨10.1021/acs.jmedchem.0c01774⟩
Journal articles hal-03185533v1
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Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox

Paul Hermant , Damien Bosc , Catherine Piveteau , Ronan Gealageas , Baovy Lam , et al.
Journal of Medicinal Chemistry, 2017, 60 (21), pp.9067-9089. ⟨10.1021/acs.jmedchem.7b01444⟩
Journal articles hal-03054238v1
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Drug Target Engagement using coupled Cellular Thermal Shift Assay -acoustic Reverse Phase Protein Array

Adrien Herledan , Marine Andres , Aurore Lejeune-Dodge , Florence Leroux , Alexandre Biela , et al.
Slas Discovery, 2019, 25 (2), pp.207-214. ⟨10.1177/2472555219897256⟩
Journal articles hal-03051837v1
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Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology

Sandrine Belouzard , Arnaud Machelart , Valentin Sencio , Thibaut Vausselin , Eik Hoffmann , et al.
Preprints, Working Papers, ... hal-03357964v1
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Modulators of hERAP2 discovered by High-Throughput Screening

Laura Medve , Ronan Gealageas , Vy Lam Bao , Valentin Guillaume , Omar Castillo-Aguilera , et al.
European Journal of Medicinal Chemistry, 2020, 211, pp.113053. ⟨10.1016/j.ejmech.2020.113053⟩
Journal articles hal-03059990v1
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Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening

Léo Faion , Kamel Djaout , Rosangela Frita , Catalin Pintiala , Francois-Xavier Cantrelle , et al.
European Journal of Medicinal Chemistry, 2020, 200, pp.112440. ⟨10.1016/j.ejmech.2020.112440⟩
Journal articles hal-02988077v1

Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737

Anne-Laure Mathieu , Olivier Sperandio , Virginie Pottiez , Sophie Balzarin , Adrien Herlédan , et al.
Journal of Biomolecular Screening, 2014, 19 (7), pp.1035-1046. ⟨10.1177/1087057114534070⟩
Journal articles hal-01911441v1
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Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance

Manuel Lasalle , Vanessa Hoguet , Nathalie Hennuyer , Florence Leroux , Catherine Piveteau , et al.
Journal of Medicinal Chemistry, 2017, 60 (10), pp.4185-4211. ⟨10.1021/acs.jmedchem.6b01873⟩
Journal articles inserm-02115415v1

Exploring the Antitubercular Activity of Anthranilic Acid Derivatives: From MabA (FabG1) Inhibition to Intrabacterial Acidification

Léo Faïon , Kamel Djaout , Catalin Pintiala , Catherine Piveteau , Florence Leroux , et al.
Pharmaceuticals, 2023, 16 (3), pp.335. ⟨10.3390/ph16030335⟩
Journal articles hal-04007450v1

BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr348 phosphorylation

Maxime Sartori , Tiago P. Mendes , Shruti Desai , Alessia Lasorsa , Adrien Herledan , et al.
Acta Neuropathologica, 2019, 138 (4), pp.631-652. ⟨10.1007/s00401-019-02017-9⟩
Journal articles hal-02337166v1
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Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors

Rébecca F. Déprez-Poulain , Marion Flipo , Catherine Piveteau , Florence Leroux , Sandrine Dassonneville , et al.
Journal of Medicinal Chemistry, 2012, 55 (24), pp.10909-10917. ⟨10.1021/jm301506h⟩
Journal articles hal-03051765v1
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A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2

Hugues Prevet , Martin Moune , Abdalkarim Tanina , Christian Kemmer , Adrien Herledan , et al.
European Journal of Medicinal Chemistry, 2019, 167, pp.426-438. ⟨10.1016/j.ejmech.2019.02.023⟩
Journal articles hal-03102744v1

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity

Baptiste Villemagne , Arnaud Machelart , Ngoc Chau Tran , Marion Flipo , Martin Moune , et al.
ACS Infectious Diseases, 2020, 6 (3), pp.366-378. ⟨10.1021/acsinfecdis.9b00277⟩
Journal articles hal-03096012v1
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Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening

Florence Leroux , Damien Bosc , Terence Beghyn , Paul Hermant , Sandrine Warenghem , et al.
European Journal of Medicinal Chemistry, 2019, 179, pp.557-566. ⟨10.1016/j.ejmech.2019.06.057⟩
Journal articles hal-03243182v1
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Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice

Rebecca Déprez-Poulain , Nathalie Hennuyer , Damien Bosc , Wenguang Liang , Emmanuelle Enée , et al.
Nature Communications, 2015, 6 (8250), ⟨10.1038/ncomms9250⟩
Journal articles hal-02511111v1

Identification of indole-based activators of insulin degrading enzyme

Nicolas Kraupner , Chau Phi Dinh , Xiaoan Wen , Valérie Landry , Adrien Herledan , et al.
European Journal of Medicinal Chemistry, 2021, pp.113982. ⟨10.1016/j.ejmech.2021.113982⟩
Journal articles hal-03430475v1
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ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease

Florent Letronne , Geoffroy Laumet , Anne-Marie Ayral , Julien Chapuis , Florie Demiautte , et al.
EBioMedicine, 2016, 9, pp.278-292. ⟨10.1016/j.ebiom.2016.06.002⟩
Journal articles hal-02155738v1
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Insulin-Degrading Enzyme, an Under-Estimated Potential Target to Treat Cancer?

Laetitia Lesire , Florence Leroux , Rebecca Déprez-Poulain , Benoit Deprez
Cells, 2022, 11 (7), pp.1228. ⟨10.3390/cells11071228⟩
Journal articles hal-03657094v1