Manon Maurel

Towards Improved Peptidic α‐Ketoamide Inhibitors of the Plasmodial Subtilisin‐Like SUB1: Exploration of N‐Terminal Extensions and Cyclic Constraints

Anna Katarzyna Puszko, Fernando de Assis Batista, Abdelaziz Ejjoummany, Anthony Bouillon et autres

Abstract After more than 15 years of decline, the Malaria epidemy has increased again since 2017, reinforcing the need to identify drug candidates active on new targets involved in at least two biological stages of the Plasmodium life cycle. The SUB1 protease, …

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Insights from structure-activity relationships and the binding mode of peptidic α-ketoamide inhibitors of the malaria drug target subtilisin-like SUB1

Alice Legru, Fernando de Assis Batista, Anna Katarzyna Puszko, Anthony Bouillon et autres

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S-Ethyl-Isothiocitrullin-Based Dipeptides and 1,2,4-Oxadiazole Pseudo-Dipeptides: Solid Phase Synthesis and Evaluation as NO Synthase Inhibitors

Elodie Mauchauffée, Jérémy Leroy, Jihanne Chamcham, Abdelaziz Ejjoummany et autres

We previously reported dipeptidomimetic compounds as inhibitors of neuronal and/or inducible NO synthases (n/iNOS) with significant selectivity against endothelial NOS (eNOS). They were composed of an S-ethylisothiocitrullin-like moiety linked to an extension through a peptide bond or a 1,2,4-oxadiazole link. Here, we …

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3D structures of the Plasmodium vivax subtilisin-like drug target SUB1 reveal conformational changes to accommodate a substrate-derived α-ketoamide inhibitor

Mariano Martínez, Fernando de Assis Batista, Manon Maurel, Anthony Bouillon et autres

The constant selection and propagation of multi-resistant Plasmodium sp. parasites require the identification of new antimalarial candidates involved in as-yet untargeted metabolic pathways. Subtilisin-like protease 1 (SUB1) belongs to a new generation of drug targets because it plays a crucial role during …

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Active Targeted Nanoemulsions for Repurposing of Tegaserod in Alzheimer’s Disease Treatment

Line Séguy, Léna Guyon, Manon Maurel, Pascal Verdié et autres

Background and Purpose: The activation of 5-HT4 receptors with agonists has emerged as a valuable therapeutic strategy to treat Alzheimer’s disease (AD) by enhancing the nonamyloidogenic pathway. Here, the potential therapeutic effects of tegaserod, an effective agent for irritable bowel syndrome, were …

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Design of PEGylated Three Ligands Silica Nanoparticles for Multi-Receptor Targeting

Manon Maurel, Titouan Montheil, Julie Martin, Line Chaar et autres

The synthesis of silica nanoparticles (SiNPs) decorated on their surface with a range of various elements (e.g., ligands, drugs, fluorophores, vectors, etc.) in a controlled ratio remains a big challenge. We have previously developed an efficient strategy to obtain in one-step, well-defined …

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The presence of PEG on nanoparticles presenting the c[RGDfK]- and/or ATWLPPR peptides deeply affects the RTKs-AKT-GSK3β-eNOS signaling pathway and endothelial cells survival

Tao Jia, Jéremy Ciccione, Thibault Jacquet, Manon Maurel et autres

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Synthesis and evaluation of Plasmodium SUB1 inhibitors, a potential target for Malaria treatment

Alice Legru, Manon Maurel, Anthony Bouillon, Anne Marie Wehenkel et autres

International audience

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Sol-gel and peptides: an attractive route to unprecedented biomaterials

Gilles Subra, Laurine Valot, Manon Maurel, Cécile Echalier et autres

International audience

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Sol-gel and peptides: an attractive route to unprecedented biomaterials

Gilles Subra, Laurine Valot, Manon Maurel, Cécile Echalier et autres

Affording biological properties to a material is one of the challenges the chemists have to tackle, to improve the efficiency of existing devices and also to propose new biomaterials.Most of synthetic approaches to obtain functional materials rely on non-covalent coatings or post-grafting …

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