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Items: 1 to 50 of 94

1.

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators.

Bischoff FP, Velter AI, Minne G, Pieters S, Berthelot D, De Cleyn M, Gijsen HJM, Macdonald G, Surkyn M, Van Brandt S, Van Roosbroeck Y, Zavattaro C, Mercken M, Austin N, Dhuyvetter D, Borghys H, Ahmad I, Samanta SK.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1737-1745. doi: 10.1016/j.bmcl.2019.05.023. Epub 2019 May 15.

PMID:
31122869
2.

Extracellular interface between APP and Nicastrin regulates Aβ length and response to γ-secretase modulators.

Petit D, Hitzenberger M, Lismont S, Zoltowska KM, Ryan NS, Mercken M, Bischoff F, Zacharias M, Chávez-Gutiérrez L.

EMBO J. 2019 May 20. pii: e101494. doi: 10.15252/embj.2019101494. [Epub ahead of print]

3.

Anti-Tau Monoclonal Antibodies Derived from Soluble and Filamentous Tau Show Diverse Functional Properties in vitro and in vivo.

Vandermeeren M, Borgers M, Van Kolen K, Theunis C, Vasconcelos B, Bottelbergs A, Wintmolders C, Daneels G, Willems R, Dockx K, Delbroek L, Marreiro A, Ver Donck L, Sousa C, Nanjunda R, Lacy E, Van De Casteele T, Van Dam D, De Deyn PP, Kemp JA, Malia TJ, Mercken MH.

J Alzheimers Dis. 2018;65(1):265-281. doi: 10.3233/JAD-180404.

PMID:
30040731
4.

Enhancement of therapeutic potential of a naturally occurring human antibody targeting a phosphorylated Ser422 containing epitope on pathological tau.

van Ameijde J, Crespo R, Janson R, Juraszek J, Siregar B, Verveen H, Sprengers I, Nahar T, Hoozemans JJ, Steinbacher S, Willems R, Delbroek L, Borgers M, Dockx K, Van Kolen K, Mercken M, Pascual G, Koudstaal W, Apetri A.

Acta Neuropathol Commun. 2018 Jul 12;6(1):59. doi: 10.1186/s40478-018-0562-9.

5.

Mass spectrometric characterization of intact desferal-conjugated monoclonal antibodies for immuno-PET imaging.

De Vijlder T, Fissers J, Van Broeck B, Wyffels L, Mercken M, Pemberton DJ.

Rapid Commun Mass Spectrom. 2018 Jun 26. doi: 10.1002/rcm.8209. [Epub ahead of print]

PMID:
29943865
6.

A common antigenic motif recognized by naturally occurring human VH5-51/VL4-1 anti-tau antibodies with distinct functionalities.

Apetri A, Crespo R, Juraszek J, Pascual G, Janson R, Zhu X, Zhang H, Keogh E, Holland T, Wadia J, Verveen H, Siregar B, Mrosek M, Taggenbrock R, Ameijde J, Inganäs H, van Winsen M, Koldijk MH, Zuijdgeest D, Borgers M, Dockx K, Stoop EJM, Yu W, Brinkman-van der Linden EC, Ummenthum K, van Kolen K, Mercken M, Steinbacher S, de Marco D, Hoozemans JJ, Wilson IA, Koudstaal W, Goudsmit J.

Acta Neuropathol Commun. 2018 May 31;6(1):43. doi: 10.1186/s40478-018-0543-z.

7.

Alzheimer's-Causing Mutations Shift Aβ Length by Destabilizing γ-Secretase-Aβn Interactions.

Szaruga M, Munteanu B, Lismont S, Veugelen S, Horré K, Mercken M, Saido TC, Ryan NS, De Vos T, Savvides SN, Gallardo R, Schymkowitz J, Rousseau F, Fox NC, Hopf C, De Strooper B, Chávez-Gutiérrez L.

Cell. 2017 Jul 27;170(3):443-456.e14. doi: 10.1016/j.cell.2017.07.004.

8.

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.

9.

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.

10.

Restricted Location of PSEN2/γ-Secretase Determines Substrate Specificity and Generates an Intracellular Aβ Pool.

Sannerud R, Esselens C, Ejsmont P, Mattera R, Rochin L, Tharkeshwar AK, De Baets G, De Wever V, Habets R, Baert V, Vermeire W, Michiels C, Groot AJ, Wouters R, Dillen K, Vints K, Baatsen P, Munck S, Derua R, Waelkens E, Basi GS, Mercken M, Vooijs M, Bollen M, Schymkowitz J, Rousseau F, Bonifacino JS, Van Niel G, De Strooper B, Annaert W.

Cell. 2016 Jun 30;166(1):193-208. doi: 10.1016/j.cell.2016.05.020. Epub 2016 Jun 9.

11.

Impact of frequent cerebrospinal fluid sampling on Aβ levels: systematic approach to elucidate influencing factors.

Van Broeck B, Timmers M, Ramael S, Bogert J, Shaw LM, Mercken M, Slemmon J, Van Nueten L, Engelborghs S, Streffer JR.

Alzheimers Res Ther. 2016 May 19;8(1):21. doi: 10.1186/s13195-016-0184-z.

12.

In Vivo Amyloid-β Imaging in the APPPS1-21 Transgenic Mouse Model with a (89)Zr-Labeled Monoclonal Antibody.

Waldron AM, Fissers J, Van Eetveldt A, Van Broeck B, Mercken M, Pemberton DJ, Van Der Veken P, Augustyns K, Joossens J, Stroobants S, Dedeurwaerdere S, Wyffels L, Staelens S.

Front Aging Neurosci. 2016 Mar 31;8:67. doi: 10.3389/fnagi.2016.00067. eCollection 2016.

13.

Synthesis and Evaluation of a Zr-89-Labeled Monoclonal Antibody for Immuno-PET Imaging of Amyloid-β Deposition in the Brain.

Fissers J, Waldron AM, De Vijlder T, Van Broeck B, Pemberton DJ, Mercken M, Van Der Veken P, Joossens J, Augustyns K, Dedeurwaerdere S, Stroobants S, Staelens S, Wyffels L.

Mol Imaging Biol. 2016 Aug;18(4):598-605. doi: 10.1007/s11307-016-0935-z.

PMID:
26846128
14.

Epitope mapping and structural basis for the recognition of phosphorylated tau by the anti-tau antibody AT8.

Malia TJ, Teplyakov A, Ernst R, Wu SJ, Lacy ER, Liu X, Vandermeeren M, Mercken M, Luo J, Sweet RW, Gilliland GL.

Proteins. 2016 Apr;84(4):427-34. doi: 10.1002/prot.24988. Epub 2016 Feb 5.

15.

APLP1 as a cerebrospinal fluid biomarker for γ-secretase modulator treatment.

Sjödin S, Andersson KK, Mercken M, Zetterberg H, Borghys H, Blennow K, Portelius E.

Alzheimers Res Ther. 2015 Dec 22;7(1):77. doi: 10.1186/s13195-015-0160-z.

16.

Impact of cerebrospinal fluid matrix on the detection of Alzheimer's disease with Aβ42 and influence of disease on the total-Aβ42/Aβ40 ratio.

Slemmon JR, Shapiro A, Mercken M, Streffer J, Romano G, Andreasen N, Zetterberg H, Blennow K.

J Neurochem. 2015 Dec;135(5):1049-58. doi: 10.1111/jnc.13297. Epub 2015 Sep 29.

17.

Diagnostic Accuracy of Cerebrospinal Fluid Amyloid-β Isoforms for Early and Differential Dementia Diagnosis.

Struyfs H, Van Broeck B, Timmers M, Fransen E, Sleegers K, Van Broeckhoven C, De Deyn PP, Streffer JR, Mercken M, Engelborghs S.

J Alzheimers Dis. 2015;45(3):813-22. doi: 10.3233/JAD-141986.

PMID:
25633670
18.

Erratum to: Acute function of secreted amyloid precursor protein fragment APPsα in synaptic plasticity.

Hick M, Herrmann U, Weyer SW, Mallm JP, Tschäpe JA, Borgers M, Mercken M, Roth FC, Draguhn A, Slomianka L, Wolfer DP, Korte M, Müller UC.

Acta Neuropathol. 2015 Jan;129(1):161-2. doi: 10.1007/s00401-014-1374-z. No abstract available.

PMID:
25527084
19.

Anilinotriazoles as potent gamma secretase modulators.

Velter AI, Bischoff FP, Berthelot D, De Cleyn M, Oehlrich D, Jaroskova L, Macdonald G, Minne G, Pieters S, Rombouts F, Van Brandt S, Van Roosbroeck Y, Surkyn M, Trabanco AA, Tresadern G, Wu T, Borghys H, Mercken M, Masungi C, Gijsen H.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5805-5813. doi: 10.1016/j.bmcl.2014.10.024. Epub 2014 Oct 18.

PMID:
25454273
20.

Acute function of secreted amyloid precursor protein fragment APPsα in synaptic plasticity.

Hick M, Herrmann U, Weyer SW, Mallm JP, Tschäpe JA, Borgers M, Mercken M, Roth FC, Draguhn A, Slomianka L, Wolfer DP, Korte M, Müller UC.

Acta Neuropathol. 2015 Jan;129(1):21-37. doi: 10.1007/s00401-014-1368-x. Epub 2014 Nov 29. Erratum in: Acta Neuropathol. 2015 Jan;129(1):161-2.

PMID:
25432317
21.

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.

22.

Comparison of two different methods for measurement of amyloid-β peptides in cerebrospinal fluid after BACE1 inhibition in a dog model.

Borghys H, Jacobs T, Van Broeck B, Dillen L, Dhuyvetter D, Gijsen H, Mercken M.

J Alzheimers Dis. 2014;38(1):39-48. doi: 10.3233/JAD-130599.

PMID:
23948925
23.

Design and synthesis of bicyclic heterocycles as potent γ-secretase modulators.

Oehlrich D, Rombouts FJ, Berthelot D, Bischoff FP, De Cleyn MA, Jaroskova L, Macdonald G, Mercken M, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter AI, Wu T, Gijsen HJ.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4794-800. doi: 10.1016/j.bmcl.2013.06.100. Epub 2013 Jul 11.

PMID:
23890837
24.

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.

25.

Soluble amyloid precursor protein α and β in CSF in Alzheimer's disease.

Brinkmalm G, Brinkmalm A, Bourgeois P, Persson R, Hansson O, Portelius E, Mercken M, Andreasson U, Parent S, Lipari F, Ohrfelt A, Bjerke M, Minthon L, Zetterberg H, Blennow K, Nutu M.

Brain Res. 2013 Jun 4;1513:117-26. doi: 10.1016/j.brainres.2013.03.019. Epub 2013 Mar 27.

PMID:
23541617
26.

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.

27.

γ-Secretase Modulators: Can We Combine Potency with Safety?

Gijsen HJ, Mercken M.

Int J Alzheimers Dis. 2012;2012:295207. doi: 10.1155/2012/295207. Epub 2012 Dec 17.

28.

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].

29.

Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators.

Bischoff F, Berthelot D, De Cleyn M, Macdonald G, Minne G, Oehlrich D, Pieters S, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter I, Zaja M, Borghys H, Masungi C, Mercken M, Gijsen HJ.

J Med Chem. 2012 Nov 8;55(21):9089-106. doi: 10.1021/jm201710f. Epub 2012 Jun 8.

PMID:
22650177
30.

BACE1 inhibition induces a specific cerebrospinal fluid β-amyloid pattern that identifies drug effects in the central nervous system.

Mattsson N, Rajendran L, Zetterberg H, Gustavsson M, Andreasson U, Olsson M, Brinkmalm G, Lundkvist J, Jacobson LH, Perrot L, Neumann U, Borghys H, Mercken M, Dhuyvetter D, Jeppsson F, Blennow K, Portelius E.

PLoS One. 2012;7(2):e31084. doi: 10.1371/journal.pone.0031084. Epub 2012 Feb 6.

31.

Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.

Gijsen HJ, Berthelot D, De Cleyn MA, Geuens I, Brône B, Mercken M.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):797-800. doi: 10.1016/j.bmcl.2011.12.068. Epub 2011 Dec 22.

PMID:
22222037
32.

A canine model to evaluate efficacy and safety of γ-secretase inhibitors and modulators.

Borghys H, Tuefferd M, Van Broeck B, Clessens E, Dillen L, Cools W, Vinken P, Straetemans R, De Ridder F, Gijsen H, Mercken M.

J Alzheimers Dis. 2012;28(4):809-22. doi: 10.3233/JAD-2011-111475.

PMID:
22072214
33.

The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics.

Karran E, Mercken M, De Strooper B.

Nat Rev Drug Discov. 2011 Aug 19;10(9):698-712. doi: 10.1038/nrd3505. Review.

PMID:
21852788
34.

The Alzheimer's Association external quality control program for cerebrospinal fluid biomarkers.

Mattsson N, Andreasson U, Persson S, Arai H, Batish SD, Bernardini S, Bocchio-Chiavetto L, Blankenstein MA, Carrillo MC, Chalbot S, Coart E, Chiasserini D, Cutler N, Dahlfors G, Duller S, Fagan AM, Forlenza O, Frisoni GB, Galasko D, Galimberti D, Hampel H, Handberg A, Heneka MT, Herskovits AZ, Herukka SK, Holtzman DM, Humpel C, Hyman BT, Iqbal K, Jucker M, Kaeser SA, Kaiser E, Kapaki E, Kidd D, Klivenyi P, Knudsen CS, Kummer MP, Lui J, Lladó A, Lewczuk P, Li QX, Martins R, Masters C, McAuliffe J, Mercken M, Moghekar A, Molinuevo JL, Montine TJ, Nowatzke W, O'Brien R, Otto M, Paraskevas GP, Parnetti L, Petersen RC, Prvulovic D, de Reus HP, Rissman RA, Scarpini E, Stefani A, Soininen H, Schröder J, Shaw LM, Skinningsrud A, Skrogstad B, Spreer A, Talib L, Teunissen C, Trojanowski JQ, Tumani H, Umek RM, Van Broeck B, Vanderstichele H, Vecsei L, Verbeek MM, Windisch M, Zhang J, Zetterberg H, Blennow K.

Alzheimers Dement. 2011 Jul;7(4):386-395.e6. doi: 10.1016/j.jalz.2011.05.2243. Erratum in: Alzheimers Dement. 2011 Sep;7(5):556.

35.

Amyloid precursor protein mutation E682K at the alternative β-secretase cleavage β'-site increases Aβ generation.

Zhou L, Brouwers N, Benilova I, Vandersteen A, Mercken M, Van Laere K, Van Damme P, Demedts D, Van Leuven F, Sleegers K, Broersen K, Van Broeckhoven C, Vandenberghe R, De Strooper B.

EMBO Mol Med. 2011 May;3(5):291-302. doi: 10.1002/emmm.201100138. Epub 2011 Apr 15.

36.

Endogenous amyloid-β is necessary for hippocampal synaptic plasticity and memory.

Puzzo D, Privitera L, Fa' M, Staniszewski A, Hashimoto G, Aziz F, Sakurai M, Ribe EM, Troy CM, Mercken M, Jung SS, Palmeri A, Arancio O.

Ann Neurol. 2011 May;69(5):819-30. doi: 10.1002/ana.22313. Epub 2011 Apr 6.

37.

Chronic treatment with a novel γ-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease.

Van Broeck B, Chen JM, Tréton G, Desmidt M, Hopf C, Ramsden N, Karran E, Mercken M, Rowley A.

Br J Pharmacol. 2011 May;163(2):375-89. doi: 10.1111/j.1476-5381.2011.01207.x.

38.

Analogues of morphanthridine and the tear gas dibenz[b,f][1,4]oxazepine (CR) as extremely potent activators of the human transient receptor potential ankyrin 1 (TRPA1) channel.

Gijsen HJ, Berthelot D, Zaja M, Brône B, Geuens I, Mercken M.

J Med Chem. 2010 Oct 14;53(19):7011-20. doi: 10.1021/jm100477n.

PMID:
20806939
39.

Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.

Portelius E, Van Broeck B, Andreasson U, Gustavsson MK, Mercken M, Zetterberg H, Borghys H, Blennow K.

J Alzheimers Dis. 2010;21(3):1005-12. doi: 10.3233/JAD-2010-100573.

PMID:
20634579
40.

Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.

Huang Y, Strobel ED, Ho CY, Reynolds CH, Conway KA, Piesvaux JA, Brenneman DE, Yohrling GJ, Moore Arnold H, Rosenthal D, Alexander RS, Tounge BA, Mercken M, Vandermeeren M, Parker MH, Reitz AB, Baxter EW.

Bioorg Med Chem Lett. 2010 May 15;20(10):3158-60. doi: 10.1016/j.bmcl.2010.03.097. Epub 2010 Mar 30.

PMID:
20399652
41.

Tear gasses CN, CR, and CS are potent activators of the human TRPA1 receptor.

Brône B, Peeters PJ, Marrannes R, Mercken M, Nuydens R, Meert T, Gijsen HJ.

Toxicol Appl Pharmacol. 2008 Sep 1;231(2):150-6. doi: 10.1016/j.taap.2008.04.005. Epub 2008 Apr 20.

PMID:
18501939
42.

P2X currents in peritoneal macrophages of wild type and P2X4 -/- mice.

Brône B, Moechars D, Marrannes R, Mercken M, Meert T.

Immunol Lett. 2007 Nov 15;113(2):83-9. Epub 2007 Aug 22.

PMID:
17825926
43.

2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.

Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, Winter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SM, Berthelot DJ, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz AB.

J Med Chem. 2007 Sep 6;50(18):4261-4. Epub 2007 Aug 8.

PMID:
17685503
44.

Lack of neprilysin suffices to generate murine amyloid-like deposits in the brain and behavioral deficit in vivo.

Madani R, Poirier R, Wolfer DP, Welzl H, Groscurth P, Lipp HP, Lu B, El Mouedden M, Mercken M, Nitsch RM, Mohajeri MH.

J Neurosci Res. 2006 Dec;84(8):1871-8.

PMID:
16998901
45.
47.

Macroautophagy--a novel Beta-amyloid peptide-generating pathway activated in Alzheimer's disease.

Yu WH, Cuervo AM, Kumar A, Peterhoff CM, Schmidt SD, Lee JH, Mohan PS, Mercken M, Farmery MR, Tjernberg LO, Jiang Y, Duff K, Uchiyama Y, Näslund J, Mathews PM, Cataldo AM, Nixon RA.

J Cell Biol. 2005 Oct 10;171(1):87-98. Epub 2005 Oct 3.

48.

Method for the determination of the levels of beta-amyloid peptide in the CSF sampled from freely moving rats.

El Mouedden M, Haseldonckx M, Mackie C, Meert T, Mercken M.

J Pharmacol Toxicol Methods. 2005 Sep-Oct;52(2):229-33. Epub 2005 Apr 14.

PMID:
16125620
49.

Development of a specific ELISA for the quantitative study of amino-terminally truncated beta-amyloid peptides.

El Mouedden M, Vandermeeren M, Meert T, Mercken M.

J Neurosci Methods. 2005 Jun 30;145(1-2):97-105. Epub 2005 Jan 8.

PMID:
15922029
50.

Abeta localization in abnormal endosomes: association with earliest Abeta elevations in AD and Down syndrome.

Cataldo AM, Petanceska S, Terio NB, Peterhoff CM, Durham R, Mercken M, Mehta PD, Buxbaum J, Haroutunian V, Nixon RA.

Neurobiol Aging. 2004 Nov-Dec;25(10):1263-72.

PMID:
15465622

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