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Items: 1 to 50 of 96

1.

Correction to Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.

Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martinez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Urmaliya V, Teisman A, Moechars D.

J Med Chem. 2018 Dec 7. doi: 10.1021/acs.jmedchem.8b01859. [Epub ahead of print] No abstract available.

PMID:
30525600
2.

BACE2 distribution in major brain cell types and identification of novel substrates.

Voytyuk I, Mueller SA, Herber J, Snellinx A, Moechars D, van Loo G, Lichtenthaler SF, De Strooper B.

Life Sci Alliance. 2018 Feb 15;1(1):e201800026. doi: 10.26508/lsa.201800026. eCollection 2018 Jan.

3.

Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.

Gijsen HJM, Alonso de Diego SA, De Cleyn M, García-Molina A, Macdonald GJ, Martínez-Lamenca C, Oehlrich D, Prokopcova H, Rombouts FJR, Surkyn M, Trabanco AA, Van Brandt S, Van den Bossche D, Van Gool M, Austin N, Borghys H, Dhuyvetter D, Moechars D.

J Med Chem. 2018 Jun 28;61(12):5292-5303. doi: 10.1021/acs.jmedchem.8b00304. Epub 2018 Jun 11.

PMID:
29809004
4.

Emergence of early alterations in network oscillations and functional connectivity in a tau seeding mouse model of Alzheimer's disease pathology.

Ahnaou A, Moechars D, Raeymaekers L, Biermans R, Manyakov NV, Bottelbergs A, Wintmolders C, Van Kolen K, Van De Casteele T, Kemp JA, Drinkenburg WH.

Sci Rep. 2017 Oct 27;7(1):14189. doi: 10.1038/s41598-017-13839-6.

5.

Fragment Binding to β-Secretase 1 without Catalytic Aspartate Interactions Identified via Orthogonal Screening Approaches.

Rombouts FJR, Alexander R, Cleiren E, De Groot A, Carpentier M, Dijkmans J, Fierens K, Masure S, Moechars D, Palomino-Schätzlein M, Pineda-Lucena A, Trabanco AA, Van Glabbeek D, Vos A, Tresadern G.

ACS Omega. 2017 Feb 28;2(2):685-697. doi: 10.1021/acsomega.6b00482. Epub 2017 Feb 24.

6.

Tau association with synaptic vesicles causes presynaptic dysfunction.

Zhou L, McInnes J, Wierda K, Holt M, Herrmann AG, Jackson RJ, Wang YC, Swerts J, Beyens J, Miskiewicz K, Vilain S, Dewachter I, Moechars D, De Strooper B, Spires-Jones TL, De Wit J, Verstreken P.

Nat Commun. 2017 May 11;8:15295. doi: 10.1038/ncomms15295.

7.

Preclinical Evaluation of 18F-JNJ64349311, a Novel PET Tracer for Tau Imaging.

Declercq L, Rombouts F, Koole M, Fierens K, Mariën J, Langlois X, Andrés JI, Schmidt M, Macdonald G, Moechars D, Vanduffel W, Tousseyn T, Vandenberghe R, Van Laere K, Verbruggen A, Bormans G.

J Nucl Med. 2017 Jun;58(6):975-981. doi: 10.2967/jnumed.116.185199. Epub 2017 Feb 23.

8.

Progressive leukoencephalopathy impairs neurobehavioral development in sialin-deficient mice.

Stroobants S, Van Acker NG, Verheijen FW, Goris I, Daneels GF, Schot R, Verbeek E, Knaapen MW, De Bondt A, Göhlmann HW, Crauwels ML, Mancini GM, Andries LJ, Moechars DW, D'Hooge R.

Exp Neurol. 2017 May;291:106-119. doi: 10.1016/j.expneurol.2017.02.009. Epub 2017 Feb 9.

9.

BACE1 Dynamics Upon Inhibition with a BACE Inhibitor and Correlation to Downstream Alzheimer's Disease Markers in Elderly Healthy Participants.

Timmers M, Barão S, Van Broeck B, Tesseur I, Slemmon J, De Waepenaert K, Bogert J, Shaw LM, Engelborghs S, Moechars D, Mercken M, Van Nueten L, Tritsmans L, de Strooper B, Streffer JR.

J Alzheimers Dis. 2017;56(4):1437-1449. doi: 10.3233/JAD-160829.

10.

Developmental Expression of 4-Repeat-Tau Induces Neuronal Aneuploidy in Drosophila Tauopathy Models.

Malmanche N, Dourlen P, Gistelinck M, Demiautte F, Link N, Dupont C, Vanden Broeck L, Werkmeister E, Amouyel P, Bongiovanni A, Bauderlique H, Moechars D, Royou A, Bellen HJ, Lafont F, Callaerts P, Lambert JC, Dermaut B.

Sci Rep. 2017 Jan 23;7:40764. doi: 10.1038/srep40764.

11.

Discovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer's Disease.

Rombouts FJ, Andrés JI, Ariza M, Alonso JM, Austin N, Bottelbergs A, Chen L, Chupakhin V, Cleiren E, Fierens K, Fontana A, Langlois X, Leenaerts JE, Mariën J, Martínez Lamenca C, Salter R, Schmidt ME, Te Riele P, Wintmolders C, Trabanco AA, Zhang W, Macdonald G, Moechars D.

J Med Chem. 2017 Feb 23;60(4):1272-1291. doi: 10.1021/acs.jmedchem.6b01173. Epub 2017 Feb 10.

PMID:
28106992
12.

Tau interactome mapping based identification of Otub1 as Tau deubiquitinase involved in accumulation of pathological Tau forms in vitro and in vivo.

Wang P, Joberty G, Buist A, Vanoosthuyse A, Stancu IC, Vasconcelos B, Pierrot N, Faelth-Savitski M, Kienlen-Campard P, Octave JN, Bantscheff M, Drewes G, Moechars D, Dewachter I.

Acta Neuropathol. 2017 May;133(5):731-749. doi: 10.1007/s00401-016-1663-9. Epub 2017 Jan 12.

13.

IP3 accumulation and/or inositol depletion: two downstream lithium's effects that may mediate its behavioral and cellular changes.

Sade Y, Toker L, Kara NZ, Einat H, Rapoport S, Moechars D, Berry GT, Bersudsky Y, Agam G.

Transl Psychiatry. 2016 Dec 6;6(12):e968. doi: 10.1038/tp.2016.217.

14.

Loss of Bin1 Promotes the Propagation of Tau Pathology.

Calafate S, Flavin W, Verstreken P, Moechars D.

Cell Rep. 2016 Oct 18;17(4):931-940. doi: 10.1016/j.celrep.2016.09.063.

15.

Profiling the dynamics of CSF and plasma Aβ reduction after treatment with JNJ-54861911, a potent oral BACE inhibitor.

Timmers M, Van Broeck B, Ramael S, Slemmon J, De Waepenaert K, Russu A, Bogert J, Stieltjes H, Shaw LM, Engelborghs S, Moechars D, Mercken M, Liu E, Sinha V, Kemp J, Van Nueten L, Tritsmans L, Streffer JR.

Alzheimers Dement (N Y). 2016 Aug 24;2(3):202-212. doi: 10.1016/j.trci.2016.08.001. eCollection 2016 Sep.

16.

The Dynamics and Turnover of Tau Aggregates in Cultured Cells: INSIGHTS INTO THERAPIES FOR TAUOPATHIES.

Guo JL, Buist A, Soares A, Callaerts K, Calafate S, Stevenaert F, Daniels JP, Zoll BE, Crowe A, Brunden KR, Moechars D, Lee VM.

J Biol Chem. 2016 Jun 17;291(25):13175-93. doi: 10.1074/jbc.M115.712083. Epub 2016 Apr 18.

17.

Comparison of New Tau PET-Tracer Candidates With [18F]T808 and [18F]T807.

Declercq L, Celen S, Lecina J, Ahamed M, Tousseyn T, Moechars D, Alcazar J, Ariza M, Fierens K, Bottelbergs A, Mariën J, Vandenberghe R, Andres IJ, Van Laere K, Verbruggen A, Bormans G.

Mol Imaging. 2016 Jan 27;15. pii: 1536012115624920. doi: 10.1177/1536012115624920. Print 2016.

18.

BACE1 Physiological Functions May Limit Its Use as Therapeutic Target for Alzheimer's Disease.

Barão S, Moechars D, Lichtenthaler SF, De Strooper B.

Trends Neurosci. 2016 Mar;39(3):158-169. doi: 10.1016/j.tins.2016.01.003. Epub 2016 Jan 30. Review.

PMID:
26833257
19.

Heterotypic seeding of Tau fibrillization by pre-aggregated Abeta provides potent seeds for prion-like seeding and propagation of Tau-pathology in vivo.

Vasconcelos B, Stancu IC, Buist A, Bird M, Wang P, Vanoosthuyse A, Van Kolen K, Verheyen A, Kienlen-Campard P, Octave JN, Baatsen P, Moechars D, Dewachter I.

Acta Neuropathol. 2016 Apr;131(4):549-69. doi: 10.1007/s00401-015-1525-x. Epub 2016 Jan 6.

20.

1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.

Rombouts FJ, Tresadern G, Delgado O, Martínez-Lamenca C, Van Gool M, García-Molina A, Alonso de Diego SA, Oehlrich D, Prokopcova H, Alonso JM, Austin N, Borghys H, Van Brandt S, Surkyn M, De Cleyn M, Vos A, Alexander R, Macdonald G, Moechars D, Gijsen H, Trabanco AA.

J Med Chem. 2015 Oct 22;58(20):8216-35. doi: 10.1021/acs.jmedchem.5b01101. Epub 2015 Oct 10.

PMID:
26378740
21.

Synaptic Contacts Enhance Cell-to-Cell Tau Pathology Propagation.

Calafate S, Buist A, Miskiewicz K, Vijayan V, Daneels G, de Strooper B, de Wit J, Verstreken P, Moechars D.

Cell Rep. 2015 May 26;11(8):1176-83. doi: 10.1016/j.celrep.2015.04.043. Epub 2015 May 14.

22.

Templated misfolding of Tau by prion-like seeding along neuronal connections impairs neuronal network function and associated behavioral outcomes in Tau transgenic mice.

Stancu IC, Vasconcelos B, Ris L, Wang P, Villers A, Peeraer E, Buist A, Terwel D, Baatsen P, Oyelami T, Pierrot N, Casteels C, Bormans G, Kienlen-Campard P, Octave JN, Moechars D, Dewachter I.

Acta Neuropathol. 2015 Jun;129(6):875-94. doi: 10.1007/s00401-015-1413-4. Epub 2015 Apr 11.

23.

Tau Positron Emission Tomography (PET) Imaging: Past, Present, and Future.

Ariza M, Kolb HC, Moechars D, Rombouts F, Andrés JI.

J Med Chem. 2015 Jun 11;58(11):4365-82. doi: 10.1021/jm5017544. Epub 2015 Feb 25.

PMID:
25671691
24.

LRRK2 functions in synaptic vesicle endocytosis through a kinase-dependent mechanism.

Arranz AM, Delbroek L, Van Kolen K, Guimarães MR, Mandemakers W, Daneels G, Matta S, Calafate S, Shaban H, Baatsen P, De Bock PJ, Gevaert K, Vanden Berghe P, Verstreken P, De Strooper B, Moechars D.

J Cell Sci. 2015 Feb 1;128(3):541–52.

25.

GSK-3β dysregulation contributes to parkinson's-like pathophysiology with associated region-specific phosphorylation and accumulation of tau and α-synuclein.

Credle JJ, George JL, Wills J, Duka V, Shah K, Lee YC, Rodriguez O, Simkins T, Winter M, Moechars D, Steckler T, Goudreau J, Finkelstein DI, Sidhu A.

Cell Death Differ. 2015 May;22(5):838-51. doi: 10.1038/cdd.2014.179. Epub 2014 Nov 14.

26.

Intracerebral injection of preformed synthetic tau fibrils initiates widespread tauopathy and neuronal loss in the brains of tau transgenic mice.

Peeraer E, Bottelbergs A, Van Kolen K, Stancu IC, Vasconcelos B, Mahieu M, Duytschaever H, Ver Donck L, Torremans A, Sluydts E, Van Acker N, Kemp JA, Mercken M, Brunden KR, Trojanowski JQ, Dewachter I, Lee VM, Moechars D.

Neurobiol Dis. 2015 Jan;73:83-95. doi: 10.1016/j.nbd.2014.08.032. Epub 2014 Sep 16.

27.

Increasing brain protein O-GlcNAc-ylation mitigates breathing defects and mortality of Tau.P301L mice.

Borghgraef P, Menuet C, Theunis C, Louis JV, Devijver H, Maurin H, Smet-Nocca C, Lippens G, Hilaire G, Gijsen H, Moechars D, Van Leuven F.

PLoS One. 2013 Dec 23;8(12):e84442. doi: 10.1371/journal.pone.0084442. eCollection 2013.

28.

Inositol-related gene knockouts mimic lithium's effect on mitochondrial function.

Toker L, Bersudsky Y, Plaschkes I, Chalifa-Caspi V, Berry GT, Buccafusca R, Moechars D, Belmaker RH, Agam G.

Neuropsychopharmacology. 2014 Jan;39(2):319-28. doi: 10.1038/npp.2013.194. Epub 2013 Aug 8.

29.

Comment on "ApoE-directed therapeutics rapidly clear β-amyloid and reverse deficits in AD mouse models".

Tesseur I, Lo AC, Roberfroid A, Dietvorst S, Van Broeck B, Borgers M, Gijsen H, Moechars D, Mercken M, Kemp J, D'Hooge R, De Strooper B.

Science. 2013 May 24;340(6135):924-e. doi: 10.1126/science.1233937.

30.

Increased expression of BIN1 mediates Alzheimer genetic risk by modulating tau pathology.

Chapuis J, Hansmannel F, Gistelinck M, Mounier A, Van Cauwenberghe C, Kolen KV, Geller F, Sottejeau Y, Harold D, Dourlen P, Grenier-Boley B, Kamatani Y, Delepine B, Demiautte F, Zelenika D, Zommer N, Hamdane M, Bellenguez C, Dartigues JF, Hauw JJ, Letronne F, Ayral AM, Sleegers K, Schellens A, Broeck LV, Engelborghs S, De Deyn PP, Vandenberghe R, O'Donovan M, Owen M, Epelbaum J, Mercken M, Karran E, Bantscheff M, Drewes G, Joberty G, Campion D, Octave JN, Berr C, Lathrop M, Callaerts P, Mann D, Williams J, Buée L, Dewachter I, Van Broeckhoven C, Amouyel P, Moechars D, Dermaut B, Lambert JC; GERAD consortium.

Mol Psychiatry. 2013 Nov;18(11):1225-34. doi: 10.1038/mp.2013.1. Epub 2013 Feb 12.

31.

Haploinsufficiency of VGluT1 but not VGluT2 impairs extinction of spatial preference and response suppression.

Callaerts-Vegh Z, Moechars D, Van Acker N, Daneels G, Goris I, Leo S, Naert A, Meert T, Balschun D, D'Hooge R.

Behav Brain Res. 2013 May 15;245:13-21. doi: 10.1016/j.bbr.2013.01.042. Epub 2013 Feb 5.

PMID:
23396167
32.

Development of an enzyme-linked immunosorbent assay for detection of cellular and in vivo LRRK2 S935 phosphorylation.

Delbroek L, Van Kolen K, Steegmans L, da Cunha R, Mandemakers W, Daneels G, De Bock PJ, Zhang J, Gevaert K, De Strooper B, Alessi DR, Verstreken P, Moechars DW.

J Pharm Biomed Anal. 2013 Mar 25;76:49-58. doi: 10.1016/j.jpba.2012.12.002. Epub 2012 Dec 16.

33.

LRRK2 controls an EndoA phosphorylation cycle in synaptic endocytosis.

Matta S, Van Kolen K, da Cunha R, van den Bogaart G, Mandemakers W, Miskiewicz K, De Bock PJ, Morais VA, Vilain S, Haddad D, Delbroek L, Swerts J, Chávez-Gutiérrez L, Esposito G, Daneels G, Karran E, Holt M, Gevaert K, Moechars DW, De Strooper B, Verstreken P.

Neuron. 2012 Sep 20;75(6):1008-21. doi: 10.1016/j.neuron.2012.08.022.

34.

The neural cell adhesion molecules L1 and CHL1 are cleaved by BACE1 protease in vivo.

Zhou L, Barão S, Laga M, Bockstael K, Borgers M, Gijsen H, Annaert W, Moechars D, Mercken M, Gevaert K, De Strooper B.

J Biol Chem. 2012 Jul 27;287(31):25927-40. doi: 10.1074/jbc.M112.377465. Epub 2012 Jun 12. Erratum in: J Biol Chem. 2012 Sep 28;287(40):33719. Gevaer, Kris [corrected to Gevaert, Kris].

35.

Inactivation of the constitutively active ghrelin receptor attenuates limbic seizure activity in rodents.

Portelli J, Thielemans L, Ver Donck L, Loyens E, Coppens J, Aourz N, Aerssens J, Vermoesen K, Clinckers R, Schallier A, Michotte Y, Moechars D, Collingridge GL, Bortolotto ZA, Smolders I.

Neurotherapeutics. 2012 Jul;9(3):658-72. doi: 10.1007/s13311-012-0125-x.

36.

Time course of tinnitus development following noise exposure in mice.

Turner J, Larsen D, Hughes L, Moechars D, Shore S.

J Neurosci Res. 2012 Jul;90(7):1480-8. doi: 10.1002/jnr.22827. Epub 2012 Mar 21.

37.

Rational design and synthesis of aminopiperazinones as β-secretase (BACE) inhibitors.

Tresadern G, Delgado F, Delgado O, Gijsen H, Macdonald GJ, Moechars D, Rombouts F, Alexander R, Spurlino J, Van Gool M, Vega JA, Trabanco AA.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7255-60. doi: 10.1016/j.bmcl.2011.10.050. Epub 2011 Oct 20.

PMID:
22071305
38.

Synaptic dysfunction in hippocampus of transgenic mouse models of Alzheimer's disease: a multi-electrode array study.

Chong SA, Benilova I, Shaban H, De Strooper B, Devijver H, Moechars D, Eberle W, Bartic C, Van Leuven F, Callewaert G.

Neurobiol Dis. 2011 Dec;44(3):284-91. doi: 10.1016/j.nbd.2011.07.006. Epub 2011 Jul 18.

PMID:
21807097
39.

Vglut2 haploinsufficiency enhances behavioral sensitivity to MK-801 and amphetamine in mice.

Naert A, Callaerts-Vegh Z, Moechars D, Meert T, D'Hooge R.

Prog Neuropsychopharmacol Biol Psychiatry. 2011 Jul 1;35(5):1316-21. doi: 10.1016/j.pnpbp.2011.03.023. Epub 2011 Apr 14.

PMID:
21514350
40.

Nav2 hypomorphic mutant mice are ataxic and exhibit abnormalities in cerebellar development.

McNeill EM, Klöckner-Bormann M, Roesler EC, Talton LE, Moechars D, Clagett-Dame M.

Dev Biol. 2011 May 15;353(2):331-43. doi: 10.1016/j.ydbio.2011.03.008. Epub 2011 Mar 16.

41.

Preclinical evaluation of 18F-JNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain.

Celen S, Koole M, De Angelis M, Sannen I, Chitneni SK, Alcazar J, Dedeurwaerdere S, Moechars D, Schmidt M, Verbruggen A, Langlois X, Van Laere K, Andrés JI, Bormans G.

J Nucl Med. 2010 Oct;51(10):1584-91. doi: 10.2967/jnumed.110.077040. Epub 2010 Sep 16.

42.

Nav2 is necessary for cranial nerve development and blood pressure regulation.

McNeill EM, Roos KP, Moechars D, Clagett-Dame M.

Neural Dev. 2010 Feb 25;5:6. doi: 10.1186/1749-8104-5-6.

43.

Demonstration of vesicular glutamate transporter-1 in corticotroph cells in the anterior pituitary of the rat.

Kocsis ZS, Molnár CS, Watanabe M, Daneels G, Moechars D, Liposits Z, Hrabovszky E.

Neurochem Int. 2010 Feb;56(3):479-86. doi: 10.1016/j.neuint.2009.12.007. Epub 2009 Dec 16.

PMID:
20025917
44.

Knockout mice in understanding the mechanism of action of lithium.

Agam G, Bersudsky Y, Berry GT, Moechars D, Lavi-Avnon Y, Belmaker RH.

Biochem Soc Trans. 2009 Oct;37(Pt 5):1121-5. doi: 10.1042/BST0371121.

PMID:
19754464
45.

Vesicular glutamate transporter VGLUT1 has a role in hippocampal long-term potentiation and spatial reversal learning.

Balschun D, Moechars D, Callaerts-Vegh Z, Vermaercke B, Van Acker N, Andries L, D'Hooge R.

Cereb Cortex. 2010 Mar;20(3):684-93. doi: 10.1093/cercor/bhp133. Epub 2009 Jul 2.

PMID:
19574394
46.

Requirement of central ghrelin signaling for alcohol reward.

Jerlhag E, Egecioglu E, Landgren S, Salomé N, Heilig M, Moechars D, Datta R, Perrissoud D, Dickson SL, Engel JA.

Proc Natl Acad Sci U S A. 2009 Jul 7;106(27):11318-23. doi: 10.1073/pnas.0812809106. Epub 2009 Jun 29.

47.

In vivo evidence for ligand-specific receptor activation in the central CRF system, as measured by local cerebral glucose utilization.

Warnock G, Moechars D, Langlois X, Steckler T.

Peptides. 2009 May;30(5):947-54. doi: 10.1016/j.peptides.2009.01.005. Epub 2009 Jan 22.

PMID:
19428773
48.

Mammalian Navigators are microtubule plus-end tracking proteins that can reorganize the cytoskeleton to induce neurite-like extensions.

van Haren J, Draegestein K, Keijzer N, Abrahams JP, Grosveld F, Peeters PJ, Moechars D, Galjart N.

Cell Motil Cytoskeleton. 2009 Oct;66(10):824-38. doi: 10.1002/cm.20370.

PMID:
19396870
49.

Decreased expression of multidrug efflux transporters in the brains of GSK-3beta transgenic mice.

Lim JC, Mickute Z, Zaman M, Hopkins S, Wijesuriya H, Steckler T, Moechars D, Van Leuven F, Sarnyai Z, Hladky SB, Barrand MA.

Brain Res. 2009 Jun 18;1276:1-10. doi: 10.1016/j.brainres.2009.04.031. Epub 2009 Apr 22.

PMID:
19393634
50.

Impairment of VGLUT2 but not VGLUT1 signaling reduces neuropathy-induced hypersensitivity.

Leo S, Moechars D, Callaerts-Vegh Z, D'Hooge R, Meert T.

Eur J Pain. 2009 Nov;13(10):1008-17. doi: 10.1016/j.ejpain.2008.12.001. Epub 2009 Jan 26.

PMID:
19171494

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