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Items: 45


Novel multi target-directed ligands targeting 5-HT4 receptors with in cellulo antioxidant properties as promising leads in Alzheimer's disease.

Lanthier C, Payan H, Liparulo I, Hatat B, Lecoutey C, Since M, Davis A, Bergamini C, Claeysen S, Dallemagne P, Bolognesi ML, Rochais C.

Eur J Med Chem. 2019 Aug 6;182:111596. doi: 10.1016/j.ejmech.2019.111596. [Epub ahead of print]


Inhibiting Acetylcholinesterase to Activate Pleiotropic Prodrugs with Therapeutic Interest in Alzheimer's Disease.

Toublet FX, Lecoutey C, Lalut J, Hatat B, Davis A, Since M, Corvaisier S, Freret T, Sopkova de Oliveira Santos J, Claeysen S, Boulouard M, Dallemagne P, Rochais C.

Molecules. 2019 Jul 31;24(15). pii: E2786. doi: 10.3390/molecules24152786.


Chronic treatments with a 5-HT4 receptor agonist decrease amyloid pathology in the entorhinal cortex and learning and memory deficits in the 5xFAD mouse model of Alzheimer's disease.

Baranger K, Giannoni P, Girard SD, Girot S, Gaven F, Stephan D, Migliorati M, Khrestchatisky M, Bockaert J, Marchetti-Gauthier E, Rivera S, Claeysen S, Roman FS.

Neuropharmacology. 2017 Nov;126:128-141. doi: 10.1016/j.neuropharm.2017.08.031. Epub 2017 Aug 26.


Phosphorylation of β-arrestin2 at Thr383 by MEK underlies β-arrestin-dependent activation of Erk1/2 by GPCRs.

Cassier E, Gallay N, Bourquard T, Claeysen S, Bockaert J, Crépieux P, Poupon A, Reiter E, Marin P, Vandermoere F.

Elife. 2017 Feb 7;6. pii: e23777. doi: 10.7554/eLife.23777.


Longitudinal In Vivo Imaging of the Cerebrovasculature: Relevance to CNS Diseases.

Arango-Lievano M, Giannoni P, Claeysen S, Marchi N, Jeanneteau F.

J Vis Exp. 2016 Dec 6;(118). doi: 10.3791/54796.


Cerebrovascular pathology during the progression of experimental Alzheimer's disease.

Giannoni P, Arango-Lievano M, Neves ID, Rousset MC, Baranger K, Rivera S, Jeanneteau F, Claeysen S, Marchi N.

Neurobiol Dis. 2016 Apr;88:107-17. doi: 10.1016/j.nbd.2016.01.001. Epub 2016 Jan 8.


Serotonin: A New Hope in Alzheimer's Disease?

Claeysen S, Bockaert J, Giannoni P.

ACS Chem Neurosci. 2015 Jul 15;6(7):940-3. doi: 10.1021/acschemneuro.5b00135. Epub 2015 May 26.


Novel multitarget-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.

Rochais C, Lecoutey C, Gaven F, Giannoni P, Hamidouche K, Hedou D, Dubost E, Genest D, Yahiaoui S, Freret T, Bouet V, Dauphin F, Sopkova de Oliveira Santos J, Ballandonne C, Corvaisier S, Malzert-Fréon A, Legay R, Boulouard M, Claeysen S, Dallemagne P.

J Med Chem. 2015 Apr 9;58(7):3172-87. doi: 10.1021/acs.jmedchem.5b00115. Epub 2015 Mar 31.


SAP97-mediated ADAM10 trafficking from Golgi outposts depends on PKC phosphorylation.

Saraceno C, Marcello E, Di Marino D, Borroni B, Claeysen S, Perroy J, Padovani A, Tramontano A, Gardoni F, Di Luca M.

Cell Death Dis. 2014 Nov 27;5:e1547. doi: 10.1038/cddis.2014.492.


Primary culture of mouse dopaminergic neurons.

Gaven F, Marin P, Claeysen S.

J Vis Exp. 2014 Sep 8;(91):e51751. doi: 10.3791/51751.


Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatment.

Lecoutey C, Hedou D, Freret T, Giannoni P, Gaven F, Since M, Bouet V, Ballandonne C, Corvaisier S, Malzert Fréon A, Mignani S, Cresteil T, Boulouard M, Claeysen S, Rochais C, Dallemagne P.

Proc Natl Acad Sci U S A. 2014 Sep 9;111(36):E3825-30. doi: 10.1073/pnas.1410315111. Epub 2014 Aug 25.


Early administration of RS 67333, a specific 5-HT4 receptor agonist, prevents amyloidogenesis and behavioral deficits in the 5XFAD mouse model of Alzheimer's disease.

Giannoni P, Gaven F, de Bundel D, Baranger K, Marchetti-Gauthier E, Roman FS, Valjent E, Marin P, Bockaert J, Rivera S, Claeysen S.

Front Aging Neurosci. 2013 Dec 24;5:96. doi: 10.3389/fnagi.2013.00096. eCollection 2013.


Serotonin type 4 receptor dimers.

Claeysen S, Donneger R, Giannoni P, Gaven F, Pellissier LP.

Methods Cell Biol. 2013;117:123-39. doi: 10.1016/B978-0-12-408143-7.00007-4.


5-HT4 receptors constitutively promote the non-amyloidogenic pathway of APP cleavage and interact with ADAM10.

Cochet M, Donneger R, Cassier E, Gaven F, Lichtenthaler SF, Marin P, Bockaert J, Dumuis A, Claeysen S.

ACS Chem Neurosci. 2013 Jan 16;4(1):130-40. doi: 10.1021/cn300095t. Epub 2012 Oct 13.


Pharmacological profile of engineered 5-HT₄ receptors and identification of 5-HT₄ receptor-biased ligands.

Gaven F, Pellissier LP, Queffeulou E, Cochet M, Bockaert J, Dumuis A, Claeysen S.

Brain Res. 2013 May 20;1511:65-72. doi: 10.1016/j.brainres.2012.11.005. Epub 2012 Nov 10. Review.


Alzheimer culprits: cellular crossroads and interplay.

Claeysen S, Cochet M, Donneger R, Dumuis A, Bockaert J, Giannoni P.

Cell Signal. 2012 Sep;24(9):1831-40. doi: 10.1016/j.cellsig.2012.05.008. Epub 2012 May 22. Review.


5-HT(4) receptors, a place in the sun: act two.

Bockaert J, Claeysen S, Compan V, Dumuis A.

Curr Opin Pharmacol. 2011 Feb;11(1):87-93. doi: 10.1016/j.coph.2011.01.012. Epub 2011 Feb 20. Review.


G protein activation by serotonin type 4 receptor dimers: evidence that turning on two protomers is more efficient.

Pellissier LP, Barthet G, Gaven F, Cassier E, Trinquet E, Pin JP, Marin P, Dumuis A, Bockaert J, Banères JL, Claeysen S.

J Biol Chem. 2011 Mar 25;286(12):9985-97. doi: 10.1074/jbc.M110.201939. Epub 2011 Jan 19.


Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.

de la Fuente T, Martín-Fontecha M, Sallander J, Benhamú B, Campillo M, Medina RA, Pellissier LP, Claeysen S, Dumuis A, Pardo L, López-Rodríguez ML.

J Med Chem. 2010 Feb 11;53(3):1357-69. doi: 10.1021/jm901672k.


Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling.

Barthet G, Carrat G, Cassier E, Barker B, Gaven F, Pillot M, Framery B, Pellissier LP, Augier J, Kang DS, Claeysen S, Reiter E, Banères JL, Benovic JL, Marin P, Bockaert J, Dumuis A.

EMBO J. 2009 Sep 16;28(18):2706-18. doi: 10.1038/emboj.2009.215. Epub 2009 Aug 6.


Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors.

Pellissier LP, Sallander J, Campillo M, Gaven F, Queffeulou E, Pillot M, Dumuis A, Claeysen S, Bockaert J, Pardo L.

Mol Pharmacol. 2009 Apr;75(4):982-90. doi: 10.1124/mol.108.053686. Epub 2009 Jan 23.


Engineering GPCR signaling pathways with RASSLs.

Conklin BR, Hsiao EC, Claeysen S, Dumuis A, Srinivasan S, Forsayeth JR, Guettier JM, Chang WC, Pei Y, McCarthy KD, Nissenson RA, Wess J, Bockaert J, Roth BL.

Nat Methods. 2008 Aug;5(8):673-8. doi: 10.1038/nmeth.1232. Review.


5-HT(4) receptors: history, molecular pharmacology and brain functions.

Bockaert J, Claeysen S, Compan V, Dumuis A.

Neuropharmacology. 2008 Nov;55(6):922-31. doi: 10.1016/j.neuropharm.2008.05.013. Epub 2008 May 23. Review.


Modifying ligand-induced and constitutive signaling of the human 5-HT4 receptor.

Chang WC, Ng JK, Nguyen T, Pellissier L, Claeysen S, Hsiao EC, Conklin BR.

PLoS One. 2007 Dec 19;2(12):e1317. doi: 10.1371/journal.pone.0001317.


5-hydroxytryptamine 4 receptor activation of the extracellular signal-regulated kinase pathway depends on Src activation but not on G protein or beta-arrestin signaling.

Barthet G, Framery B, Gaven F, Pellissier L, Reiter E, Claeysen S, Bockaert J, Dumuis A.

Mol Biol Cell. 2007 Jun;18(6):1979-91. Epub 2007 Mar 21.


Neuronal 5-HT metabotropic receptors: fine-tuning of their structure, signaling, and roles in synaptic modulation.

Bockaert J, Claeysen S, Bécamel C, Dumuis A, Marin P.

Cell Tissue Res. 2006 Nov;326(2):553-72. Epub 2006 Aug 1. Review.


Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements.

Barthet G, Gaven F, Framery B, Shinjo K, Nakamura T, Claeysen S, Bockaert J, Dumuis A.

J Biol Chem. 2005 Jul 29;280(30):27924-34. Epub 2005 May 26.


Drosophila molting neurohormone bursicon is a heterodimer and the natural agonist of the orphan receptor DLGR2.

Mendive FM, Van Loy T, Claeysen S, Poels J, Williamson M, Hauser F, Grimmelikhuijzen CJ, Vassart G, Vanden Broeck J.

FEBS Lett. 2005 Apr 11;579(10):2171-6.


An activation switch in the rhodopsin family of G protein-coupled receptors: the thyrotropin receptor.

Urizar E, Claeysen S, Deupí X, Govaerts C, Costagliola S, Vassart G, Pardo L.

J Biol Chem. 2005 Apr 29;280(17):17135-41. Epub 2005 Feb 18.


New sorting nexin (SNX27) and NHERF specifically interact with the 5-HT4a receptor splice variant: roles in receptor targeting.

Joubert L, Hanson B, Barthet G, Sebben M, Claeysen S, Hong W, Marin P, Dumuis A, Bockaert J.

J Cell Sci. 2004 Oct 15;117(Pt 22):5367-79. Epub 2004 Oct 5.


5-HT4 receptors.

Bockaert J, Claeysen S, Compan V, Dumuis A.

Curr Drug Targets CNS Neurol Disord. 2004 Feb;3(1):39-51. Review.


A single mutation in the 5-HT4 receptor (5-HT4-R D100(3.32)A) generates a Gs-coupled receptor activated exclusively by synthetic ligands (RASSL).

Claeysen S, Joubert L, Sebben M, Bockaert J, Dumuis A.

J Biol Chem. 2003 Jan 10;278(2):699-702. Epub 2002 Nov 18.


A conserved Asn in TM7 of the thyrotropin receptor is a common requirement for activation by both mutations and its natural agonist.

Claeysen S, Govaerts C, Lefort A, Van Sande J, Costagliola S, Pardo L, Vassart G.

FEBS Lett. 2002 Apr 24;517(1-3):195-200.


A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists.

Joubert L, Claeysen S, Sebben M, Bessis AS, Clark RD, Martin RS, Bockaert J, Dumuis A.

J Biol Chem. 2002 Jul 12;277(28):25502-11. Epub 2002 Apr 25. Erratum in: J Biol Chem 2002 Oct 18;277(42):40167.


G protein-coupled receptors: dominant players in cell-cell communication.

Bockaert J, Claeysen S, Bécamel C, Pinloche S, Dumuis A.

Int Rev Cytol. 2002;212:63-132. Review.


Constitutively active mutants of 5-HT4 receptors are they in unique active states?

Claeysen S, Sebben M, Bécamel C, Parmentier ML, Dumuis A, Bockaert J.

EMBO Rep. 2001 Jan;2(1):61-7.


Inhibition of glucose-induced insulin secretion by a peripheral-type benzodiazepine receptor ligand (PK11195).

Pujalte D, Claeysen S, Dietz S, Chapal J, Hillaire-Buys D, Petit P.

Naunyn Schmiedebergs Arch Pharmacol. 2000 Jul;362(1):46-51.


Pharmacological properties of 5-Hydroxytryptamine(4) receptor antagonists on constitutively active wild-type and mutated receptors.

Claeysen S, Sebben M, Bécamel C, Eglen RM, Clark RD, Bockaert J, Dumuis A.

Mol Pharmacol. 2000 Jul;58(1):136-44.


Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain.

Claeysen S, Sebben M, Becamel C, Bockaert J, Dumuis A.

Mol Pharmacol. 1999 May;55(5):910-20.


5-HT4 receptors: cloning and expression of new splice variants.

Claeysen S, Faye P, Sebben M, Taviaux S, Bockaert J, Dumuis A.

Ann N Y Acad Sci. 1998 Dec 15;861:49-56. Review.


5-HT4 receptors: gene, transduction and effects on olfactory memory.

Bockaert J, Claeysen S, Sebben M, Dumuis A.

Ann N Y Acad Sci. 1998 Dec 15;861:1-15. Review.


Cloning and expression of human 5-HT4S receptors. Effect of receptor density on their coupling to adenylyl cyclase.

Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A.

Neuroreport. 1997 Oct 20;8(15):3189-96.


Assignment of 5-hydroxytryptamine receptor (HTR4) to human chromosome 5 bands q31-->q33 by in situ hybridization.

Claeysen S, Faye P, Sebben M, Lemaire S, Bockaert J, Dumuis A, Taviaux S.

Cytogenet Cell Genet. 1997;78(2):133-4. No abstract available.


Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor.

Claeysen S, Sebben M, Journot L, Bockaert J, Dumuis A.

FEBS Lett. 1996 Nov 25;398(1):19-25.

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