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Polypharmacology

For a number of years CERMN has been developing several research programmes in the field of polypharmacology. The programmes aim at both improving by means of data mining the characterization of pharmacological networks that cause certain pathologies · known as the MinOmics programme · but also suggesting innovative therapeutic approaches to multifactorial pathologies. The PLEIAD programme is thus designed to develop pleiotropic molecules of interest in the treatment of Alzheimer’s disease.

Major Publications

Rochais, C. et al. Novel Multi-Target Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities as Potential Agents against Alzheimer’s Disease: The Design of Donecopride. J. Med. Chem. 2015, 58, 3172–3187.

Lepailleur, A. et al. Dual Histamine H3R/Serotonin 5-HT4R Ligands with Antiamnesic Properties: Pharmacophore-Based Virtual Screening and Polypharmacology. J. Chem. Inf. Model. 2014, 54, 1773–1784.

Lecoutey, C. et al. Design of Donecopride, a Dual Serotonin Subtype 4 Receptor Agonist/acetylcholinesterase Inhibitor with Potential Interest for Alzheimer’s Disease Treatment. Proc. Natl. Acad. Sci. U. S. A. 2014, 111, E3825–E3830.

Lecoutey, C. et al. Synthesis of Dual AChE/5-HT4 Receptor Multi-Target Directed Ligands. MedChemComm, 2012, 3, 627–634.

Sopkova-de Oliveira Santos, J. et al. Virtual Screening Discovery of New Acetylcholinesterase Inhibitors Issued from CERMN Chemical Library. J. Chem. Inf. Model. 2010, 50, 422–428.

Major collaborations

  • Institut de Génomique Fonctionnelle · Montpellier, Sylvie Claeysen
  • Groupe Mémoire et Plasticité Comportementale · Caen, Michel Boulouard
  • Imagerie et Stratégies Thérapeutiques des pathologies Cérébrales et Tumorales · Caen, Louisa Barré
  • Groupe de Recherche en Informatique, Image, Automatique et Instrumentation de Caen · GREYC · Caen, Bertrand Cuissart et Bruno Crémilleux

Financial supports


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Last update : July 4, 2016


CONTACT

Pr Christophe Rochais
+33 (0)2 31 56 68 13
christophe.rochais@unicaen.fr

Université de Caen Normandie
CERMN Centre détudes et de recherche sur le médicament de Normandie
Boulevard Becquerel | 14032 Caen Cedex | France