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Items: 1 to 50 of 122

1.

Direct Interaction of PP2A Phosphatase with GABAB Receptors Alters Functional Signaling.

Li X, Terunuma M, Deeb TG, Wiseman S, Pangalos MN, Nairn AC, Moss SJ, Slesinger PA.

J Neurosci. 2020 Apr 1;40(14):2808-2816. doi: 10.1523/JNEUROSCI.2654-19.2020. Epub 2020 Feb 28.

PMID:
32111696
2.

Clusterin Is Required for β-Amyloid Toxicity in Human iPSC-Derived Neurons.

Robbins JP, Perfect L, Ribe EM, Maresca M, Dangla-Valls A, Foster EM, Killick R, Nowosiad P, Reid MJ, Polit LD, Nevado AJ, Ebner D, Bohlooly-Y M, Buckley N, Pangalos MN, Price J, Lovestone S.

Front Neurosci. 2018 Jul 25;12:504. doi: 10.3389/fnins.2018.00504. eCollection 2018.

3.

Impact of a five-dimensional framework on R&D productivity at AstraZeneca.

Morgan P, Brown DG, Lennard S, Anderton MJ, Barrett JC, Eriksson U, Fidock M, Hamrén B, Johnson A, March RE, Matcham J, Mettetal J, Nicholls DJ, Platz S, Rees S, Snowden MA, Pangalos MN.

Nat Rev Drug Discov. 2018 Mar;17(3):167-181. doi: 10.1038/nrd.2017.244. Epub 2018 Jan 19.

PMID:
29348681
4.

Estradiol modulates the efficacy of synaptic inhibition by decreasing the dwell time of GABAA receptors at inhibitory synapses.

Mukherjee J, Cardarelli RA, Cantaut-Belarif Y, Deeb TZ, Srivastava DP, Tyagarajan SK, Pangalos MN, Triller A, Maguire J, Brandon NJ, Moss SJ.

Proc Natl Acad Sci U S A. 2017 Oct 31;114(44):11763-11768. doi: 10.1073/pnas.1705075114. Epub 2017 Oct 16.

5.

Deficits in the activity of presynaptic γ-aminobutyric acid type B receptors contribute to altered neuronal excitability in fragile X syndrome.

Kang JY, Chadchankar J, Vien TN, Mighdoll MI, Hyde TM, Mather RJ, Deeb TZ, Pangalos MN, Brandon NJ, Dunlop J, Moss SJ.

J Biol Chem. 2017 Apr 21;292(16):6621-6632. doi: 10.1074/jbc.M116.772541. Epub 2017 Feb 17.

6.

Pioneering government-sponsored drug repositioning collaborations: progress and learning.

Frail DE, Brady M, Escott KJ, Holt A, Sanganee HJ, Pangalos MN, Watkins C, Wegner CD.

Nat Rev Drug Discov. 2015 Dec;14(12):833-41. doi: 10.1038/nrd4707. Epub 2015 Nov 20. Review.

PMID:
26585533
7.

Purinergic receptor activation facilitates astrocytic GABAB receptor calcium signalling.

Terunuma M, Haydon PG, Pangalos MN, Moss SJ.

Neuropharmacology. 2015 Jan;88:74-81. doi: 10.1016/j.neuropharm.2014.09.015. Epub 2014 Sep 23.

8.

Glutamine synthetase stability and subcellular distribution in astrocytes are regulated by γ-aminobutyric type B receptors.

Huyghe D, Nakamura Y, Terunuma M, Faideau M, Haydon P, Pangalos MN, Moss SJ.

J Biol Chem. 2014 Oct 17;289(42):28808-15. doi: 10.1074/jbc.M114.583534. Epub 2014 Aug 29.

9.

Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework.

Cook D, Brown D, Alexander R, March R, Morgan P, Satterthwaite G, Pangalos MN.

Nat Rev Drug Discov. 2014 Jun;13(6):419-31. doi: 10.1038/nrd4309. Epub 2014 May 16. Review.

PMID:
24833294
10.

Postsynaptic GABAB receptor activity regulates excitatory neuronal architecture and spatial memory.

Terunuma M, Revilla-Sanchez R, Quadros IM, Deng Q, Deeb TZ, Lumb M, Sicinski P, Haydon PG, Pangalos MN, Moss SJ.

J Neurosci. 2014 Jan 15;34(3):804-16. doi: 10.1523/JNEUROSCI.3320-13.2013.

11.

Sodium channel cleavage is associated with aberrant neuronal activity and cognitive deficits in a mouse model of Alzheimer's disease.

Corbett BF, Leiser SC, Ling HP, Nagy R, Breysse N, Zhang X, Hazra A, Brown JT, Randall AD, Wood A, Pangalos MN, Reinhart PH, Chin J.

J Neurosci. 2013 Apr 17;33(16):7020-6. doi: 10.1523/JNEUROSCI.2325-12.2013. Erratum in: J Neurosci. 2013 Jun 26;33(26):10934. Brown, Jon T [added]; Randall, Andrew D [added].

12.

Treatment strategies targeting amyloid β-protein.

Schenk D, Basi GS, Pangalos MN.

Cold Spring Harb Perspect Med. 2012 Sep 1;2(9):a006387. doi: 10.1101/cshperspect.a006387. Review.

13.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31.

PMID:
22902656
14.

Methamphetamine-evoked depression of GABA(B) receptor signaling in GABA neurons of the VTA.

Padgett CL, Lalive AL, Tan KR, Terunuma M, Munoz MB, Pangalos MN, Martínez-Hernández J, Watanabe M, Moss SJ, Luján R, Lüscher C, Slesinger PA.

Neuron. 2012 Mar 8;73(5):978-89. doi: 10.1016/j.neuron.2011.12.031.

15.

Temporal proteomic profile of memory consolidation in the rat hippocampal dentate gyrus.

Monopoli MP, Raghnaill MN, Loscher JS, O'Sullivan NC, Pangalos MN, Ring RH, von Schack D, Dunn MJ, Regan CM, Pennington S, Murphy KJ.

Proteomics. 2011 Nov;11(21):4189-201. doi: 10.1002/pmic.201100072. Epub 2011 Oct 17.

PMID:
22002935
16.

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.

Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ.

J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11.

PMID:
21988093
17.

New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.

Malamas MS, Erdei J, Gunawan I, Barnes K, Hui Y, Johnson M, Robichaud A, Zhou P, Yan Y, Solvibile W, Turner J, Fan KY, Chopra R, Bard J, Pangalos MN.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5164-70. doi: 10.1016/j.bmcl.2011.07.057. Epub 2011 Jul 23.

PMID:
21835615
18.

Altered intrinsic neuronal excitability and reduced Na+ currents in a mouse model of Alzheimer's disease.

Brown JT, Chin J, Leiser SC, Pangalos MN, Randall AD.

Neurobiol Aging. 2011 Nov;32(11):2109.e1-14. doi: 10.1016/j.neurobiolaging.2011.05.025. Epub 2011 Jul 27.

PMID:
21794952
19.

Characterization of vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist.

Dunlop J, Watts SW, Barrett JE, Coupet J, Harrison B, Mazandarani H, Nawoschik S, Pangalos MN, Ramamoorthy S, Schechter L, Smith D, Stack G, Zhang J, Zhang G, Rosenzweig-Lipson S.

J Pharmacol Exp Ther. 2011 Jun;337(3):673-80. doi: 10.1124/jpet.111.179572. Epub 2011 Mar 14.

PMID:
21402690
20.

Monoacylglycerol lipase activity is a critical modulator of the tone and integrity of the endocannabinoid system.

Chanda PK, Gao Y, Mark L, Btesh J, Strassle BW, Lu P, Piesla MJ, Zhang MY, Bingham B, Uveges A, Kowal D, Garbe D, Kouranova EV, Ring RH, Bates B, Pangalos MN, Kennedy JD, Whiteside GT, Samad TA.

Mol Pharmacol. 2010 Dec;78(6):996-1003. doi: 10.1124/mol.110.068304. Epub 2010 Sep 20.

PMID:
20855465
21.

Introduction to the special issue on Alzheimer's disease.

Pangalos MN, Randall AD.

Neuropharmacology. 2010 Sep-Oct;59(4-5):219-20. doi: 10.1016/j.neuropharm.2010.07.021. No abstract available.

PMID:
20728692
22.

Functional modulation of GABAB receptors by protein kinases and receptor trafficking.

Terunuma M, Pangalos MN, Moss SJ.

Adv Pharmacol. 2010;58:113-22. doi: 10.1016/S1054-3589(10)58005-0. Review.

23.

Prolonged activation of NMDA receptors promotes dephosphorylation and alters postendocytic sorting of GABAB receptors.

Terunuma M, Vargas KJ, Wilkins ME, Ramírez OA, Jaureguiberry-Bravo M, Pangalos MN, Smart TG, Moss SJ, Couve A.

Proc Natl Acad Sci U S A. 2010 Aug 3;107(31):13918-23. doi: 10.1073/pnas.1000853107. Epub 2010 Jul 19.

24.

Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.

Höfgen N, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Tremmel P, Pangalos MN, Marquis KL, Hage T, Harrison BL, Malamas MS, Brandon NJ, Kronbach T.

J Med Chem. 2010 Jun 10;53(11):4399-411. doi: 10.1021/jm1002793.

PMID:
20450197
25.

Reduced reelin protein synthesis in ventral hippocampus of isolation reared Wistar rats accompanies impaired avoidance conditioning.

Cassidy AW, Mulvany SK, Pangalos MN, Murphy KJ, Regan CM.

Behav Brain Res. 2010 Nov 12;213(1):130-4. doi: 10.1016/j.bbr.2010.04.040. Epub 2010 May 8.

PMID:
20438765
26.

Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.

Malamas MS, Barnes K, Hui Y, Johnson M, Lovering F, Condon J, Fobare W, Solvibile W, Turner J, Hu Y, Manas ES, Fan K, Olland A, Chopra R, Bard J, Pangalos MN, Reinhart P, Robichaud AJ.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2068-73. doi: 10.1016/j.bmcl.2010.02.075. Epub 2010 Feb 23.

PMID:
20223661
27.

Social odor recognition: a novel behavioral model for cognitive dysfunction in Parkinson's disease.

Monaghan MM, Leddy L, Sung ML, Albinson K, Kubek K, Pangalos MN, Reinhart PH, Zaleska MM, Comery TA.

Neurodegener Dis. 2010;7(1-3):153-9. doi: 10.1159/000289227. Epub 2010 Mar 3.

PMID:
20197696
28.

Loss of retrograde endocannabinoid signaling and reduced adult neurogenesis in diacylglycerol lipase knock-out mice.

Gao Y, Vasilyev DV, Goncalves MB, Howell FV, Hobbs C, Reisenberg M, Shen R, Zhang MY, Strassle BW, Lu P, Mark L, Piesla MJ, Deng K, Kouranova EV, Ring RH, Whiteside GT, Bates B, Walsh FS, Williams G, Pangalos MN, Samad TA, Doherty P.

J Neurosci. 2010 Feb 10;30(6):2017-24. doi: 10.1523/JNEUROSCI.5693-09.2010.

29.

Temporal dysregulation of cortical gene expression in the isolation reared Wistar rat.

Murphy KJ, Ter Horst JP, Cassidy AW, DeSouza IE, Morgunova M, Li C, Connole LM, O'Sullivan NC, Loscher JS, Brady AT, Rombach N, Connellan J, McGettigan PA, Scully D, Fedriani R, Lukasz B, Moran MP, McCabe OM, Wantuch CM, Hughes ZA, Mulvany SK, Higgins DG, Pangalos MN, Marquis KL, O'Connor WT, Ring RH, von Schack D, Regan CM.

J Neurochem. 2010 May;113(3):601-14. doi: 10.1111/j.1471-4159.2010.06617.x. Epub 2010 Jan 24.

30.

Developmental emergence of reelin deficits in the prefrontal cortex of Wistar rats reared in social isolation.

Cassidy AW, Mulvany SK, Pangalos MN, Murphy KJ, Regan CM.

Neuroscience. 2010 Mar 17;166(2):377-85. doi: 10.1016/j.neuroscience.2009.12.045. Epub 2009 Dec 24.

PMID:
20035841
31.

Estrogen receptor neurobiology and its potential for translation into broad spectrum therapeutics for CNS disorders.

Hughes ZA, Liu F, Marquis K, Muniz L, Pangalos MN, Ring RH, Whiteside GT, Brandon NJ.

Curr Mol Pharmacol. 2009 Nov;2(3):215-36. Review.

PMID:
20021460
32.

AAV-mediated chronic over-expression of SNAP-25 in adult rat dorsal hippocampus impairs memory-associated synaptic plasticity.

McKee AG, Loscher JS, O'Sullivan NC, Chadderton N, Palfi A, Batti L, Sheridan GK, O'Shea S, Moran M, McCabe O, Fernández AB, Pangalos MN, O'Connor JJ, Regan CM, O'Connor WT, Humphries P, Farrar GJ, Murphy KJ.

J Neurochem. 2010 Feb;112(4):991-1004. doi: 10.1111/j.1471-4159.2009.06516.x. Epub 2009 Nov 30.

33.

Structural correlates of antibodies associated with acute reversal of amyloid beta-related behavioral deficits in a mouse model of Alzheimer disease.

Basi GS, Feinberg H, Oshidari F, Anderson J, Barbour R, Baker J, Comery TA, Diep L, Gill D, Johnson-Wood K, Goel A, Grantcharova K, Lee M, Li J, Partridge A, Griswold-Prenner I, Piot N, Walker D, Widom A, Pangalos MN, Seubert P, Jacobsen JS, Schenk D, Weis WI.

J Biol Chem. 2010 Jan 29;285(5):3417-27. doi: 10.1074/jbc.M109.045187. Epub 2009 Nov 18.

34.

GABA(B) receptor activation triggers BDNF release and promotes the maturation of GABAergic synapses.

Fiorentino H, Kuczewski N, Diabira D, Ferrand N, Pangalos MN, Porcher C, Gaiarsa JL.

J Neurosci. 2009 Sep 16;29(37):11650-61. doi: 10.1523/JNEUROSCI.3587-09.2009.

35.

Neuroprotective profile of novel SRC kinase inhibitors in rodent models of cerebral ischemia.

Liang S, Pong K, Gonzales C, Chen Y, Ling HP, Mark RJ, Boschelli F, Boschelli DH, Ye F, Barrios Sosa AC, Mansour TS, Frost P, Wood A, Pangalos MN, Zaleska MM.

J Pharmacol Exp Ther. 2009 Dec;331(3):827-35. doi: 10.1124/jpet.109.156562. Epub 2009 Sep 9.

PMID:
19741150
36.

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS.

J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11.

PMID:
19671883
37.

GABA(A) receptor membrane trafficking regulates spine maturity.

Jacob TC, Wan Q, Vithlani M, Saliba RS, Succol F, Pangalos MN, Moss SJ.

Proc Natl Acad Sci U S A. 2009 Jul 28;106(30):12500-5. doi: 10.1073/pnas.0903943106. Epub 2009 Jul 14.

38.

Preclinical characterization of WAY-211612: a dual 5-HT uptake inhibitor and 5-HT (1A) receptor antagonist and potential novel antidepressant.

Beyer CE, Lin Q, Platt B, Malberg J, Hornby G, Sullivan KM, Smith DL, Lock T, Mitchell PJ, Hatzenbuhler NT, Evrard DA, Harrison BL, Magolda R, Pangalos MN, Schechter LE, Rosenzweig-Lipson S, Andree TH.

Br J Pharmacol. 2009 May;157(2):307-19. doi: 10.1111/j.1476-5381.2009.00146.x. Epub 2009 Mar 26.

39.

Prodrugs of perzinfotel with improved oral bioavailability.

Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE Jr.

J Med Chem. 2009 Feb 12;52(3):771-8. doi: 10.1021/jm8011799.

PMID:
19146418
40.

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS.

J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w.

PMID:
19012391
41.

The development of stroke therapeutics: promising mechanisms and translational challenges.

Zaleska MM, Mercado ML, Chavez J, Feuerstein GZ, Pangalos MN, Wood A.

Neuropharmacology. 2009 Feb;56(2):329-41. doi: 10.1016/j.neuropharm.2008.10.006. Epub 2008 Nov 1. Review.

PMID:
19007799
42.

Impact of apolipoprotein E (ApoE) polymorphism on brain ApoE levels.

Riddell DR, Zhou H, Atchison K, Warwick HK, Atkinson PJ, Jefferson J, Xu L, Aschmies S, Kirksey Y, Hu Y, Wagner E, Parratt A, Xu J, Li Z, Zaleska MM, Jacobsen JS, Pangalos MN, Reinhart PH.

J Neurosci. 2008 Nov 5;28(45):11445-53. doi: 10.1523/JNEUROSCI.1972-08.2008.

43.

Multimodal magnetic resonance imaging for assessing evolution of ischemic penumbra: a key translational medicine strategy to manage the risk of developing novel therapies for acute ischemic stroke.

Chavez JC, Zaleska MM, Wang X, Wood A, Hurko O, Pangalos MN, Feuerstein GZ.

J Cereb Blood Flow Metab. 2009 Jan;29(1):217-9. doi: 10.1038/jcbfm.2008.103. Epub 2008 Sep 3.

PMID:
18766199
44.

The availability of surface GABA B receptors is independent of gamma-aminobutyric acid but controlled by glutamate in central neurons.

Vargas KJ, Terunuma M, Tello JA, Pangalos MN, Moss SJ, Couve A.

J Biol Chem. 2008 Sep 5;283(36):24641-8. doi: 10.1074/jbc.M802419200. Epub 2008 Jun 25.

45.

A diacylglycerol lipase-CB2 cannabinoid pathway regulates adult subventricular zone neurogenesis in an age-dependent manner.

Goncalves MB, Suetterlin P, Yip P, Molina-Holgado F, Walker DJ, Oudin MJ, Zentar MP, Pollard S, Yáñez-Muñoz RJ, Williams G, Walsh FS, Pangalos MN, Doherty P.

Mol Cell Neurosci. 2008 Aug;38(4):526-36. doi: 10.1016/j.mcn.2008.05.001. Epub 2008 May 15.

PMID:
18562209
46.

Enhanced clearance of Abeta in brain by sustaining the plasmin proteolysis cascade.

Jacobsen JS, Comery TA, Martone RL, Elokdah H, Crandall DL, Oganesian A, Aschmies S, Kirksey Y, Gonzales C, Xu J, Zhou H, Atchison K, Wagner E, Zaleska MM, Das I, Arias RL, Bard J, Riddell D, Gardell SJ, Abou-Gharbia M, Robichaud A, Magolda R, Vlasuk GP, Bjornsson T, Reinhart PH, Pangalos MN.

Proc Natl Acad Sci U S A. 2008 Jun 24;105(25):8754-9. doi: 10.1073/pnas.0710823105. Epub 2008 Jun 16.

47.

Ganglioside inhibition of neurite outgrowth requires Nogo receptor function: identification of interaction sites and development of novel antagonists.

Williams G, Wood A, Williams EJ, Gao Y, Mercado ML, Katz A, Joseph-McCarthy D, Bates B, Ling HP, Aulabaugh A, Zaccardi J, Xie Y, Pangalos MN, Walsh FS, Doherty P.

J Biol Chem. 2008 Jun 13;283(24):16641-52. doi: 10.1074/jbc.M802067200. Epub 2008 Apr 14.

48.

Activation of estrogen receptor-beta regulates hippocampal synaptic plasticity and improves memory.

Liu F, Day M, Muñiz LC, Bitran D, Arias R, Revilla-Sanchez R, Grauer S, Zhang G, Kelley C, Pulito V, Sung A, Mervis RF, Navarra R, Hirst WD, Reinhart PH, Marquis KL, Moss SJ, Pangalos MN, Brandon NJ.

Nat Neurosci. 2008 Mar;11(3):334-43. doi: 10.1038/nn2057. Epub 2008 Feb 24.

PMID:
18297067
49.

The clustering of GABA(A) receptor subtypes at inhibitory synapses is facilitated via the direct binding of receptor alpha 2 subunits to gephyrin.

Tretter V, Jacob TC, Mukherjee J, Fritschy JM, Pangalos MN, Moss SJ.

J Neurosci. 2008 Feb 6;28(6):1356-65. doi: 10.1523/JNEUROSCI.5050-07.2008.

50.

Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities.

Ruan B, Pong K, Jow F, Bowlby M, Crozier RA, Liu D, Liang S, Chen Y, Mercado ML, Feng X, Bennett F, von Schack D, McDonald L, Zaleska MM, Wood A, Reinhart PH, Magolda RL, Skotnicki J, Pangalos MN, Koehn FE, Carter GT, Abou-Gharbia M, Graziani EI.

Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8. Epub 2007 Dec 27.

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