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51. Identification of antiviral compounds against equid herpesvirus‐1 using Real‐Time Cell Analysis: screening of 2,891 molecules

Author

Thieulent, Côme, Hue, Erika, Sutton, Gabrielle, Fortier, Christine, Dallemagne, Patrick, Zientara, Stephan, Munier-Lehmann, Hélène, Hans, Aymeric, Paillot, Romain, Vidalain, Pierre-Olivier, Pronost, Stéphane, LABÉO, Pôle d’analyses et de recherche de Normandie (LABÉO), Biologie, génétique et thérapies ostéoarticulaires et respiratoires (BIOTARGEN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), ImpedanCELL, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Virologie UMR1161 (VIRO), École nationale vétérinaire d'Alfort (ENVA)-Agence nationale de sécurité sanitaire de l'alimentation, de l'environnement et du travail (ANSES)-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE), Chimie organique (UCO), Institut Pasteur [Paris]-Centre National de la Recherche Scientifique (CNRS), Criblage chémogénomique et biologique (Plateforme) - Chemogenomic and Biological Screening Platform (PF-CCB), Institut Pasteur [Paris], ANSES, Laboratoire de Santé Animale - site de Dozulé, Agence nationale de sécurité sanitaire de l'alimentation, de l'environnement et du travail (ANSES), School of Equine and Veterinary Physiotherapy, Writtle University College (WUC), Centre International de Recherche en Infectiologie - UMR (CIRI), École normale supérieure - Lyon (ENS Lyon)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Institut National de la Santé et de la Recherche Médicale (INSERM)-École normale supérieure - Lyon (ENS Lyon)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Centre National de la Recherche Scientifique (CNRS), Interactions Cellules Organismes Environnement (ICORE), Normandie Université (NU)-Normandie Université (NU)-CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN), École nationale vétérinaire - Alfort (ENVA)-Agence nationale de sécurité sanitaire de l'alimentation, de l'environnement et du travail (ANSES)-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE), Institut Pasteur [Paris] (IP)-Centre National de la Recherche Scientifique (CNRS)-Université Paris Cité (UPCité), Physiopathologie et épidémiologie des maladies équines (PhEED), Laboratoire de santé animale, sites de Maisons-Alfort et de Normandie, Agence nationale de sécurité sanitaire de l'alimentation, de l'environnement et du travail (ANSES)-Agence nationale de sécurité sanitaire de l'alimentation, de l'environnement et du travail (ANSES), Centre International de Recherche en Infectiologie (CIRI), École normale supérieure de Lyon (ENS de Lyon)-Université Claude Bernard Lyon 1 (UCBL), Université de Lyon-Université de Lyon-Université Jean Monnet - Saint-Étienne (UJM)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), ABÉO, IFCE (Institut Français du Cheval et de l’Equitation, project AMIE), Fonds Eperon (project N87-2014, N07-2015, N07-2016, N13-2017 and N62-2017), Région Normandie (CPER R25 P3) and CENTAURE European project co-funded by Normandy County Council, European Union in the framework of the ERDF-ESF operational programme 2014-2020., CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-CHU Caen, and Normandie Université (NU)

Subjects
0403 veterinary science, [SDV.BA.MVSA]Life Sciences [q-bio]/Animal biology/Veterinary medicine and animal Health, 040301 veterinary sciences, 0402 animal and dairy science, 04 agricultural and veterinary sciences, General Medicine, 040201 dairy & animal science, ComputingMilieux_MISCELLANEOUS, 3. Good health
Abstract

International audience

Published
2021
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54. Biginelli Reaction Synthesis of Novel Multitarget-Directed Ligands with Ca 2+ Channel Blocking Ability, Cholinesterase Inhibition, Antioxidant Capacity, and Nrf2 Activation.

Author

Malek, Rim, Simakov, Alexey, Davis, Audrey, Maj, Maciej, Bernard, Paul J., Wnorowski, Artur, Martin, Helene, Marco-Contelles, José, Chabchoub, Fakher, Dallemagne, Patrick, Rochais, Christophe, Jozwiak, Krzysztof, and Ismaili, Lhassane

Subjects
OXIDANT status, NUCLEAR factor E2 related factor, LIGANDS (Biochemistry), CALCIUM channels
Abstract

Novel multitarget-directed ligands BIGI 4a-d and BIGI 5a-d were designed and synthesized with a simple and cost-efficient procedure via a one-pot three-component Biginelli reaction targeting acetyl-/butyrylcholinesterases inhibition, calcium channel antagonism, and antioxidant ability. Among these multitarget-directed ligands, BIGI 4b, BIGI 4d, and BIGI 5b were identified as promising new hit compounds showing in vitro balanced activities toward the recognized AD targets. In addition, these compounds showed suitable physicochemical properties and a good druglikeness score predicted by Data Warrior software. [ABSTRACT FROM AUTHOR]

Published
2023
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57. Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

Author

Peronne, Lauralie, Denarier, Eric, Rai, Ankit, Prudent, Renaud, Vernet, Audrey, Suzanne, Peggy, Ramirez-Rios, Sacnicté, Michallet, Sophie, Guidetti, Mélanie, Vollaire, Julien, Lucena-Agell, Daniel, Ribba, Anne-Sophie, Josserand, Véronique, Coll, Jean-Luc, Dallemagne, Patrick, Díaz, J Fernando, Oliva, María Ángela, Sadoul, Karin, Akhmanova, Anna, Andrieux, Annie, Lafanechère, Laurence, Sub Cell Biology, and Celbiologie

Subjects
microtubules, paclitaxel, drug synergy, carbazole, cancer therapy
Abstract

Paclitaxel is a microtubule stabilizing agent and a successful drug for cancer chemotherapy inducing, however, adverse effects. To reduce the effective dose of paclitaxel, we searched for pharmaceutics which could potentiate its therapeutic effect. We screened a chemical library and selected Carba1, a carbazole, which exerts synergistic cytotoxic effects on tumor cells grown in vitro, when co-administrated with a low dose of paclitaxel. Carba1 targets the colchicine binding-site of tubulin and is a microtubule-destabilizing agent. Catastrophe induction by Carba1 promotes paclitaxel binding to microtubule ends, providing a mechanistic explanation of the observed synergy. The synergistic effect of Carba1 with paclitaxel on tumor cell viability was also observed in vivo in xenografted mice. Thus, a new mechanism favoring paclitaxel binding to dynamic microtubules can be transposed to in vivo mouse cancer treatments, paving the way for new therapeutic strategies combining low doses of microtubule targeting agents with opposite mechanisms of action.

Published
2020

58. Matrix metalloproteinases as new targets in Alzheimer's disease: Opportunities and Challenges

Author

Zipfel, Pauline, Rochais, Christophe, Baranger, Kévin, Rivera, Santiago, Dallemagne, Patrick, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Institut de neurophysiopathologie (INP), and Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS)

Subjects
MT5-MMP, Inhibitor, Quantitative Biology - Neurons and Cognition, FOS: Biological sciences, Brain, Neurons and Cognition (q-bio.NC), [SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC], [SDV.IB]Life Sciences [q-bio]/Bioengineering, MMPs, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Alzheimer's disease, Development, Nervous System
Abstract

International audience; Although matrix metalloproteinases (MMPs) are implicated in the regulation of numerous physiological processes, evidences of their pathological roles have also been obtained in the last decades, making MMPs attractive therapeutic targets for several diseases. Recent discoveries of their involvement in central nervous system (CNS) disorders, and in particular in Alzheimer's disease (AD), have paved the way to consider MMP modulators as promising therapeutic strategies. Over the past few decades, diverse approaches have been undertaken in the design of

Published
2020

59. Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

Author

Adnet, Thomas, Groo, Anne-Claire, Picard, Céline, Davis, Audrey, Corvaisier, Sophie, Since, Marc, Bounoure, Frédéric, Rochais, Christophe, Le Pluart, Loïc, Dallemagne, Patrick, and Malzert-Fréon, Aurélie

Subjects
lcsh:Pharmacy and materia medica, nanocomposite, thermosensitive hydrogel, nose-to-brain delivery, lcsh:RS1-441, Article
Abstract

Direct nose-to-brain delivery has been raised as a non-invasive powerful strategy to deliver drugs to the brain bypassing the blood-brain barrier (BBB). This study aimed at preparing and characterizing an innovative composite formulation, associating the liposome and hydrogel approaches, suitable for intranasal administration. Thermosensitive gel formulations were obtained based on a mixture of two hydrophilic polymers (Poloxamer 407, P407 and Poloxamer 188, P188) for a controlled delivery through nasal route via liposomes of an active pharmaceutical ingredient (API) of potential interest for Alzheimer’s disease. The osmolarity and the gelation temperature (T° sol-gel) of formulations, defined in a ternary diagram, were investigated by rheometry and visual determination. Regarding the issue of assays, a mixture composed of P407/P188 (15/1%, w/w) was selected for intranasal administration in terms of T° sol-gel and for the compatibility with the olfactory mucosal (280 ± 20 mOsmol, pH 6). Liposomes of API were prepared by the thin film hydration method. Mucoadhesion studies were performed by using mucin disc, and they showed the good natural mucoadhesive characteristics of in situ gel formulations, which increased when liposomes were added. The study demonstrated successful pharmacotechnical development of a promising API-loaded liposomes in a thermosensitive hydrogel intended for nasal Alzheimer’s disease treatment.

Published
2020

63. First Synthesis of Racemic Trans Propargylamino-Donepezil, a Pleiotrope Agent Able to Both Inhibit AChE and MAO-B, with Potential Interest against Alzheimer’s Disease

Author

Guieu, Benjamin, primary, Lecoutey, Cedric, additional, Legay, Rémi, additional, Davis, Audrey, additional, Sopkova de Oliveira Santos, Jana, additional, Altomare, Cosimo Damiano, additional, Catto, Marco, additional, Rochais, Christophe, additional, and Dallemagne, Patrick, additional

Published
2020
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64. Disproportionality analysis in VigiBase as a drug repositioning method for the discovery of potentially useful drugs in Alzheimer's disease

Author

Chrétien, Basile, primary, Jourdan, Jean‐Pierre, additional, Davis, Audrey, additional, Fedrizzi, Sophie, additional, Bureau, Ronan, additional, Sassier, Marion, additional, Rochais, Christophe, additional, Alexandre, Joachim, additional, Lelong‐Boulouard, Véronique, additional, Dolladille, Charles, additional, and Dallemagne, Patrick, additional

Published
2020
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65. Screening of potential antiviral molecules against equid herpesvirus-1 using cellular impedance measurement: Dataset of 2,891 compounds.

Author

Thieulent, Côme, primary, Fortier, Christine, additional, Munier-Lehmann, Hélène, additional, Suzanne, Peggy, additional, Dallemagne, Patrick, additional, Zientara, Stephan, additional, Hans, Aymeric, additional, Paillot, Romain, additional, Vidalain, Pierre-Olivier, additional, Pronost, Stéphane, additional, and Hue, Erika, additional

Published
2020
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68. Replication of Equine arteritis virus is efficiently suppressed by purine and pyrimidine biosynthesis inhibitors

Author

Valle-Casuso, José Carlos, primary, Gaudaire, Delphine, additional, Martin-Faivre, Lydie, additional, Madeline, Anthony, additional, Dallemagne, Patrick, additional, Pronost, Stéphane, additional, Munier-Lehmann, Hélène, additional, Zientara, Stephan, additional, Vidalain, Pierre-Olivier, additional, and Hans, Aymeric, additional

Published
2020
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70. Donecopride, a Swiss army knife with potential interest against Alzheimer's disease

Author

Rochais, Christophe, Lecoutey, Cédric, Hamidouche, Katia, Giannoni, Patrizia, Gaven, Florence, Cem, Eleazere, Mignani, Serge, Baranger, Kévin, Freret, Thomas, Bockaert, Joël, Rivera, Santiago, Boulouard, Michel, Dallemagne, Patrick, Claeysen, Sylvie, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Université de Caen Normandie - UFR Santé (UNICAEN Santé), Mobilités : Vieillissement, Pathologie, Santé (COMETE), Normandie Université (NU)-Normandie Université (NU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Institut de Génomique Fonctionnelle (IGF), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Détection, évaluation, gestion des risques CHROniques et éMErgents (CHROME) / Université de Nîmes (CHROME), Université de Nîmes (UNIMES), Centre de recherche en Biologie cellulaire de Montpellier (CRBM), Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Laboratoire de Chimie et de Biochimie Pharmacologiques et Toxicologiques (LCBPT - UMR 8601), Université Paris Descartes - Paris 5 (UPD5)-Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS), Institut de neurophysiopathologie (INP), Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS), This work was supported by funding from Normandie Valorisation, Normandie Incubation, and BPI France (AAP Maturation Preclinicalz), the French Agence Nationale de la Recherche (project MALAD ANR-12-JS007-0012-01, project ADAMGUARD ANR-12-BSV4-008-01 and project MAD5 ANR-15-CE16-0006), and The Fondation Vaincre Alzheimer (grant number #12721). K.B. was granted a research associate fellowship (Management of Talents) by the Excellence Initiative of Aix-Marseille University - A*MIDEX, a French 'Programme Investissements d’Avenir.', ANR-12-BSV4-0008,ADAMGUARD,Les réseaux protéiques associés aux récepteurs 5 HT4 : gardes rapprochées du trafic de l'ADAM10 et de l'APP(2012), ANR-15-CE16-0006,MAD5,Validation de MT5-MMP comme nouvelle cible thérapeutique dans la maladie d'Alzheimer et mécanismes d'action(2015), ANR-12-JS07-0012,MALAD,Developpement de Ligands pluriactifs d'intérêt potentiel dans le traitement de la maladie d'Alzheimer(2012), Université de Montpellier (UM)-Université Montpellier 1 (UM1)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Montpellier 2 - Sciences et Techniques (UM2)-Centre National de la Recherche Scientifique (CNRS), Centre de recherche en Biologie Cellulaire (CRBM), Université Montpellier 1 (UM1)-Université Montpellier 2 - Sciences et Techniques (UM2)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Université Montpellier 2 - Sciences et Techniques (UM2)-Centre National de la Recherche Scientifique (CNRS)-Université de Montpellier (UM)-Université Montpellier 1 (UM1), Université Paris Descartes - Paris 5 (UPD5)-Centre National de la Recherche Scientifique (CNRS), and Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Caen Normandie (UNICAEN)

Subjects
[SDV.NEU.NB]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology, [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology
Abstract

International audience; BACKGROUND AND PURPOSE: We recently identified donecopride as a pleiotropic compound able to inhibit acetylcholinesterase and to activate serotonin subtype 4 receptor. The purpose of the present article is to establish its potential therapeutic interest against Alzheimer's disease (AD).EXPERIMENTAL APPROACH: The present work used both in cellulo and in vivo models of AD.KEY RESULTS: In the present study, we show that, in vivo under chronic administration, donecopride displays potent anti-amnesic properties in two different animal models of Alzheimer's disease (AD) (transgenic 5XFAD mice and mice exposed to soluble amyloid-β peptides). Donecopride preserved learning capacities, including working and long-term spatial memories, which were evaluated with various behavioral tests (novel object recognition, Y-maze, Morris water maze). These behavioral observations found molecular correlation with the interactions of donecopride related to the two main types of molecular damage in AD. Indeed, a decrease in amyloid aggregation was observed in the brain of the treated transgenic mice, as well as a reduction in tau hyperphosphorylation in rat primary cultures of hippocampal neurons. At the cellular level, donecopride exerted neuroprotective effects toward neurons and the neurite network, as well as neurotrophic benefits, expressed as the formation of new synapses.CONCLUSIONS & IMPLICATIONS: Pleiotropic donecopride acts like a Swiss army knife, displaying sustainable symptomatic therapeutic effects and potential disease-modifying roles against AD. Clinical trials with this promising drug candidate will soon be undertaken to confirm its therapeutic potential in humans.

Published
2020
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71. Two Antagonistic Microtubule Targeting Drugs Act Synergistically to Kill Cancer Cells

Author

Sub Cell Biology, Celbiologie, Peronne, Lauralie, Denarier, Eric, Rai, Ankit, Prudent, Renaud, Vernet, Audrey, Suzanne, Peggy, Ramirez-Rios, Sacnicté, Michallet, Sophie, Guidetti, Mélanie, Vollaire, Julien, Lucena-Agell, Daniel, Ribba, Anne-Sophie, Josserand, Véronique, Coll, Jean-Luc, Dallemagne, Patrick, Díaz, J Fernando, Oliva, María Ángela, Sadoul, Karin, Akhmanova, Anna, Andrieux, Annie, Lafanechère, Laurence, Sub Cell Biology, Celbiologie, Peronne, Lauralie, Denarier, Eric, Rai, Ankit, Prudent, Renaud, Vernet, Audrey, Suzanne, Peggy, Ramirez-Rios, Sacnicté, Michallet, Sophie, Guidetti, Mélanie, Vollaire, Julien, Lucena-Agell, Daniel, Ribba, Anne-Sophie, Josserand, Véronique, Coll, Jean-Luc, Dallemagne, Patrick, Díaz, J Fernando, Oliva, María Ángela, Sadoul, Karin, Akhmanova, Anna, Andrieux, Annie, and Lafanechère, Laurence

Published
2020

72. Two antagonistic microtubule targeting drugs act synergistically to kill cancer cells

Author

Université Grenoble Alpes, Institut National de la Santé et de la Recherche Médicale (France), Centre National de la Recherche Scientifique (France), Institut National du Cancer (France), Fondation ARC pour la Recherche sur le Cancer, European Commission, Ministerio de Economía y Competitividad (España), Netherlands Organization for Scientific Research, Peronne, Lauralie, Denarier, Eric, Rai, Ankit, Prudent, Renaud, Vernet, Audrey, Suzanne, Peggy, Ramírez-Ríos, Sacnicte, Michallet, Sophie, Guidetti, Mélanie, Vollaire, Julien, Lucena-Agell, Daniel, Ribba, Anne-Sophie, Josserand, Véronique, Coll, Jean-Luc, Dallemagne, Patrick, Díaz, José Fernando, Oliva, María A., Sadoul, Karin, Akhmanova, Anna, Andrieux, Annie, Lafanechère, Laurence, Université Grenoble Alpes, Institut National de la Santé et de la Recherche Médicale (France), Centre National de la Recherche Scientifique (France), Institut National du Cancer (France), Fondation ARC pour la Recherche sur le Cancer, European Commission, Ministerio de Economía y Competitividad (España), Netherlands Organization for Scientific Research, Peronne, Lauralie, Denarier, Eric, Rai, Ankit, Prudent, Renaud, Vernet, Audrey, Suzanne, Peggy, Ramírez-Ríos, Sacnicte, Michallet, Sophie, Guidetti, Mélanie, Vollaire, Julien, Lucena-Agell, Daniel, Ribba, Anne-Sophie, Josserand, Véronique, Coll, Jean-Luc, Dallemagne, Patrick, Díaz, José Fernando, Oliva, María A., Sadoul, Karin, Akhmanova, Anna, Andrieux, Annie, and Lafanechère, Laurence

Abstract

Paclitaxel is a microtubule stabilizing agent and a successful drug for cancer chemotherapy inducing, however, adverse effects. To reduce the effective dose of paclitaxel, we searched for pharmaceutics which could potentiate its therapeutic effect. We screened a chemical library and selected Carba1, a carbazole, which exerts synergistic cytotoxic effects on tumor cells grown in vitro, when co-administrated with a low dose of paclitaxel. Carba1 targets the colchicine binding-site of tubulin and is a microtubule-destabilizing agent. Catastrophe induction by Carba1 promotes paclitaxel binding to microtubule ends, providing a mechanistic explanation of the observed synergy. The synergistic effect of Carba1 with paclitaxel on tumor cell viability was also observed in vivo in xenografted mice. Thus, a new mechanism favoring paclitaxel binding to dynamic microtubules can be transposed to in vivo mouse cancer treatments, paving the way for new therapeutic strategies combining low doses of microtubule targeting agents with opposite mechanisms of action.

Published
2020

76. Drug repositioning: a brief overview.

Author

Jourdan, Jean-Pierre, Bureau, Ronan, Rochais, Christophe, and Dallemagne, Patrick

Subjects
DRUG repositioning, ASPIRIN, DRUG utilization, DATA mining, SILDENAFIL
Abstract

Objectives Drug repositioning, that is, the use of a drug in an indication other than the one for which it was initially marketed, is a growing trend. Its origins lie mainly in the attrition experienced in recent years in the field of new drug discovery. Key findings Despite some regulatory and economic challenges, drug repositioning offers many advantages, and a number of recent successes have confirmed both its public health benefits and its commercial value. The first examples of successful drug repositioning mainly came about through serendipity like acetylsalicylic acid, thalidomide, sildenafil or dimethylfumarate. Conclusion The history of great-repositioned drugs has given some solutions to various pathologies. Serendipity is not yet useful to find repositioning drugs. Drug repositioning is of growing interest. Nowadays, a more rational approach to the identification of drug candidates for repositioning is possible, especially using data mining. [ABSTRACT FROM AUTHOR]

Published
2021
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77. Aminothiaindanone as an Accessible Scaffold for a Three-Point Chemical Diversity.

Author

Zipfel, Pauline, Lalut, Julien, Sopková-de Oliveira Santos, Jana, Rochais, Christophe, and Dallemagne, Patrick

Subjects
PHARMACEUTICAL chemistry, CHEMICAL reactions
Abstract

Aminothiaindanone heterocycle appears to be a scaffold of interest in medicinal chemistry. To increase the chemical diversity in this series, the introduction of three-point chemical diversity on the cyclopenta[ b ]thiophen-4-one scaffold was explored. About thirty newly functionalized thiophene-containing bicycles were obtained using various chemical reactions, paving the way for novel possibilities in medicinal chemistry projects. [ABSTRACT FROM AUTHOR]

Published
2021
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79. Additional file 1: of A chemical screen identifies two novel small compounds that alter Arabidopsis thaliana pollen tube growth

Author

Ferdousse Laggoun, Dardelle, Flavien, Dehors, Jérémy, Falconet, Denis, Azeddine Driouich, Rochais, Christophe, Dallemagne, Patrick, Lehner, Arnaud, and Mollet, Jean-Claude

Abstract

Figure S1. Dose-response effect of the compounds on (a) Solanum lycopersicum and (b) Nicotiana tabacum pollen tubes after 6 h of culture. (PDF 3876 kb)

Published
2019
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80. Additional file 2: of A chemical screen identifies two novel small compounds that alter Arabidopsis thaliana pollen tube growth

Author

Ferdousse Laggoun, Dardelle, Flavien, Dehors, Jérémy, Falconet, Denis, Azeddine Driouich, Rochais, Christophe, Dallemagne, Patrick, Lehner, Arnaud, and Mollet, Jean-Claude

Abstract

Figure S2. Time-lapse observations of actin dynamics in Arabidopsis thaliana pollen tubes treated for 2, 4 and 6 h with the compounds. (PDF 220 kb)

Published
2019
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81. A Novel in vivo Anti-amnesic Agent, Specially Designed to Express Both Acetylcholinesterase (AChE) Inhibitory, Serotonergic Subtype 4 Receptor (5-HT4R) Agonist and Serotonergic Subtype 6 Receptor (5-HT6R) Inverse Agonist Activities, With a Potential Interest Against Alzheimer’s Disease

Author

Hatat, Bérénice, Yahiaoui, Samir, Lecoutey, Cédric, Davis, Audrey, Freret, Thomas, Boulouard, Michel, Claeysen, Sylvie, Rochais, Christophe, Dallemagne, Patrick, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Institut de Génomique Fonctionnelle (IGF), Université de Montpellier (UM)-Université Montpellier 1 (UM1)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Université Montpellier 2 - Sciences et Techniques (UM2)-Centre National de la Recherche Scientifique (CNRS), GIP Cyceron (Cyceron), Normandie Université (NU)-Normandie Université (NU)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-CHU Caen, Normandie Université (NU)-Tumorothèque de Caen Basse-Normandie (TCBN)-Tumorothèque de Caen Basse-Normandie (TCBN)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), This work was supported by funding from the Fondation Vaincre Alzheimer (#FR-15072) and the Fondation Plan Alzheimer (AAP2015 Project TRIAD 016). The authors gratefully acknowledge the Conseil Régional de Normandie, as well as the European Community (FEDER) for theircontribution to the CERMN’s analytical platform. European COST action CA15135 (Multi-Target Paradigm for Innovative Ligand Identification in the Drug Discovery Process, MuTaLig) supports this article., and Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS)

Subjects
Aging, Cognitive Neuroscience, [SDV.NEU.NB]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC]/Neurobiology, 5-HT 6 receptors, acetylcholinesterase, [CHIM.THER]Chemical Sciences/Medicinal Chemistry, Alzheimer's disease, 5-HT 4 receptors, MTDL
Abstract

International audience; This work describes the conception, synthesis, in vitro and in vivo biological evaluation of novel Multi-Target Directed Ligands (MTDL) able to both activate 5-HT4 receptors, block 5-HT6 receptors and inhibit acetylcholinesterase activity (AChE), in order to exert a synergistic anti-amnesic effect, potentially useful in the treatment of Alzheimer's disease (AD). Indeed, both activation of 5-HT4 and blockage of 5-HT6 receptors led to an enhanced acetylcholine release, suggesting it could lead to efficiently restoring the cholinergic neurotransmission deficit observed in AD. Furthermore, 5-HT4 receptor agonists are able to promote the non-amyloidogenic cleavage of the amyloid precursor protein (APP) and to favor the production of the neurotrophic protein sAPPα. Finally, we identified a pleiotropic compound, [1-(4-amino-5-chloro-2-methoxyphenyl)-3-(1-(3-methylbenzyl)piperidin-4-yl)propan-1-one fumaric acid salt (10)], which displayed in vivo an anti-amnesic effect in a model of scopolamine-induced deficit of working memory at a dose of 0.3 mg/kg.

Published
2019
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82. Donecopride, a Swiss army knife with potential against Alzheimer's disease

Author

Rochais, Christophe, primary, Lecoutey, Cédric, additional, Hamidouche, Katia, additional, Giannoni, Patrizia, additional, Gaven, Florence, additional, Cem, Eleazere, additional, Mignani, Serge, additional, Baranger, Kevin, additional, Freret, Thomas, additional, Bockaert, Joël, additional, Rivera, Santiago, additional, Boulouard, Michel, additional, Dallemagne, Patrick, additional, and Claeysen, Sylvie, additional

Published
2020
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83. Two antagonistic microtubule targeting drugs act synergistically to kill cancer cells

Author

Peronne, Lauralie, primary, Denarier, Eric, additional, Rai, Ankit, additional, Prudent, Renaud, additional, Vernet, Audrey, additional, Suzanne, Peggy, additional, Ramirez-Rios, Sacnicté, additional, Michallet, Sophie, additional, Guidetti, Mélanie, additional, Vollaire, Julien, additional, Lucena-Agell, Daniel, additional, Ribba, Anne-Sophie, additional, Josserand, Véronique, additional, Coll, Jean-Luc, additional, Dallemagne, Patrick, additional, Díaz, J. Fernando, additional, Oliva, María Ángela, additional, Sadoul, Karin, additional, Akhmanova, Anna, additional, Andrieux, Annie, additional, and Lafanechère, Laurence, additional

Published
2020
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85. Inhibiting Acetylcholinesterase to Activate Pleiotropic Prodrugs with Therapeutic Interest in Alzheimer’s Disease

Author

Toublet, François-Xavier, primary, Lecoutey, Cédric, additional, Lalut, Julien, additional, Hatat, Bérénice, additional, Davis, Audrey, additional, Since, Marc, additional, Corvaisier, Sophie, additional, Freret, Thomas, additional, Sopkova de Oliveira Santos, Jana, additional, Claeysen, Sylvie, additional, Boulouard, Michel, additional, Dallemagne, Patrick, additional, and Rochais, Christophe, additional

Published
2019
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89. Disproportionality analysis in VigiBase as a drug repositioning method for the discovery of potentially useful drugs in Alzheimer's disease.

Author

Chrétien, Basile, Jourdan, Jean‐Pierre, Davis, Audrey, Fedrizzi, Sophie, Bureau, Ronan, Sassier, Marion, Rochais, Christophe, Alexandre, Joachim, Lelong‐Boulouard, Véronique, Dolladille, Charles, and Dallemagne, Patrick

Subjects
ALZHEIMER'S disease, SEROTONIN, DRUG side effects, DRUG analysis, DRUG utilization, HUMAN behavior
Abstract

Aims: Drug repositioning aims to propose new indications for marketed drugs. Although several methods exist, the utility of pharmacovigilance databases for this purpose is unclear. We conducted a disproportionality analysis in the World Health Organization pharmacovigilance database VigiBase to identify potential anticholinesterase drug candidates for repositioning in Alzheimer's disease (AD). Methods: Disproportionality analysis is a validated method for detecting significant associations between drugs and adverse events (AEs) in pharmacovigilance databases. We applied this approach in VigiBase to establish the safety profile displayed by the anticholinesterase drugs used in AD and searched the database for drugs with similar safety profiles. The detected drugs with potential activity against acetylcholinesterase and butyrylcholinesterases (BuChEs) were then evaluated to confirm their anticholinesterase potential. Results: We identified 22 drugs with safety profiles similar to AD medicines. Among these drugs, 4 (clozapine, aripiprazole, sertraline and S‐duloxetine) showed a human BuChE inhibition rate of over 70% at 10−5 M. Their human BuChE half maximal inhibitory concentration values were compatible with clinical anticholinesterase action in humans at their normal doses. The most active human BuChE inhibitor in our study was S‐duloxetine, with a half maximal inhibitory concentration of 1.2 μM. Combined with its ability to inhibit serotonin (5‐HT) reuptake, the use of this drug could represent a novel multitarget directed ligand therapeutic strategy for AD. Conclusion: We identified 4 drugs with repositioning potential in AD using drug safety profiles derived from a pharmacovigilance database. This method could be useful for future drug repositioning efforts. [ABSTRACT FROM AUTHOR]

Published
2021
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90. Dérivés du m-Gaïacol, leur préparation et leurs utilisations en tant que biocides, notamment en tant qu’antibactériens ou désinfectants. Brevet Français LABÉO-CERMN (Université de Caen)

Author

Rochais, C., Lemaitre, S., Xiao, F., Rault, Sylvain, Dallemagne, Patrick, Suzanne, Peggy, Castagnet, Sophie, Léon, Albertine, HUE, Erika, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), LABÉO, Pôle d’analyses et de recherche de Normandie (LABÉO), and LABÉO-CERMN

Subjects
[SDV.BA.MVSA]Life Sciences [q-bio]/Animal biology/Veterinary medicine and animal Health, [SDV.BA.MVSA] Life Sciences [q-bio]/Animal biology/Veterinary medicine and animal Health
Published
2018

92. Edema Factor Of Bacillus Anthracis Interacting with its Inhibitors

Author

Pitard, Irène, primary, Simenel, Catherine, additional, Monet, Damien, additional, Thomas, Christophe, additional, Suzanne, Peggy, additional, Blondel, Arnaud, additional, Bellalou, Jacques, additional, Dallemagne, Patrick, additional, Guijarro, Inaki, additional, Ladant, Daniel, additional, Goossens, Pierre, additional, and Malliavin, Therese E., additional

Published
2019
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95. Development of a nasal drug delivery composite nanosystem for Alzheimer’s desease treatment

Author

thomas, adnet, Groo, Anne-Claire, Le Pluart, Loïc, Picard, Celine, Davis, A., Corvaisier, Sophie, E., demissy, Since, Marc, Rochais, Christophe, Dallemagne, Patrick, Malzert-Fréon, Aurélie, Le Pluart, Loïc, Centre d'Etudes et de Recherche sur le Médicament de Normandie (CERMN), Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Normandie Université (NU), Laboratoire de chimie moléculaire et thioorganique (LCMT), Centre National de la Recherche Scientifique (CNRS)-Institut Normand de Chimie Moléculaire Médicinale et Macromoléculaire (INC3M), Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU)-Normandie Université (NU)-Institut national des sciences appliquées Rouen Normandie (INSA Rouen Normandie), Institut National des Sciences Appliquées (INSA)-Normandie Université (NU)-Institut National des Sciences Appliquées (INSA)-Université Le Havre Normandie (ULH), Normandie Université (NU)-Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Centre National de la Recherche Scientifique (CNRS)-Université de Caen Normandie (UNICAEN), Normandie Université (NU)-Institut de Chimie du CNRS (INC)-École Nationale Supérieure d'Ingénieurs de Caen (ENSICAEN), Normandie Université (NU), Unité de Recherche en Chimie Organique et Macromoléculaire (URCOM), and Université Le Havre Normandie (ULH)

Subjects
[CHIM] Chemical Sciences, [CHIM]Chemical Sciences, ComputingMilieux_MISCELLANEOUS
Abstract

International audience

Published
2017

98. Back Cover: Benzylphenylpyrrolizinones with Anti-amyloid and Radical Scavenging Effects, Potentially Useful in Alzheimer's Disease Treatment (ChemMedChem 12/2017)

Author

Jourdan, Jean-Pierre, primary, Since, Marc, additional, El Kihel, Laïla, additional, Lecoutey, Cédric, additional, Corvaisier, Sophie, additional, Legay, Rémi, additional, Sopková-de Oliveira Santos, Jana, additional, Cresteil, Thierry, additional, Malzert-Fréon, Aurélie, additional, Rochais, Christophe, additional, and Dallemagne, Patrick, additional

Published
2017
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