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Items: 1 to 50 of 158

1.

Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.

Bueno O, Gargantilla M, Estévez-Gallego J, Martins S, Díaz JF, Camarasa MJ, Liekens S, Pérez-Pérez MJ, Priego EM.

Eur J Med Chem. 2019 Jun 1;171:195-208. doi: 10.1016/j.ejmech.2019.03.045. Epub 2019 Mar 21.

PMID:
30921759
2.

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands.

Balaguer FA, Mühlethaler T, Estévez-Gallego J, Calvo E, Giménez-Abián JF, Risinger AL, Sorensen EJ, Vanderwal CD, Altmann KH, Mooberry SL, Steinmetz MO, Oliva MÁ, Prota AE, Díaz JF.

Int J Mol Sci. 2019 Mar 20;20(6). pii: E1392. doi: 10.3390/ijms20061392.

3.

Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate.

Gaugaz FZ, Chicca A, Redondo-Horcajo M, Barasoain I, Díaz JF, Altmann KH.

Int J Mol Sci. 2019 Mar 5;20(5). pii: E1113. doi: 10.3390/ijms20051113.

4.

Klebsiella oxytoca enterotoxins tilimycin and tilivalline have distinct host DNA-damaging and microtubule-stabilizing activities.

Unterhauser K, Pöltl L, Schneditz G, Kienesberger S, Glabonjat RA, Kitsera M, Pletz J, Josa-Prado F, Dornisch E, Lembacher-Fadum C, Roier S, Gorkiewicz G, Lucena D, Barasoain I, Kroutil W, Wiedner M, Loizou JI, Breinbauer R, Díaz JF, Schild S, Högenauer C, Zechner EL.

Proc Natl Acad Sci U S A. 2019 Feb 26;116(9):3774-3783. doi: 10.1073/pnas.1819154116. Epub 2019 Feb 11.

5.

Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents.

Brindisi M, Ulivieri C, Alfano G, Gemma S, de Asís Balaguer F, Khan T, Grillo A, Chemi G, Menchon G, Prota AE, Olieric N, Lucena-Agell D, Barasoain I, Diaz JF, Nebbioso A, Conte M, Lopresti L, Magnano S, Amet R, Kinsella P, Zisterer DM, Ibrahim O, O'Sullivan J, Morbidelli L, Spaccapelo R, Baldari C, Butini S, Novellino E, Campiani G, Altucci L, Steinmetz MO, Brogi S.

Eur J Med Chem. 2019 Jan 15;162:290-320. doi: 10.1016/j.ejmech.2018.11.004. Epub 2018 Nov 3.

PMID:
30448418
6.

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.

Menchon G, Prota AE, Lucena-Agell D, Bucher P, Jansen R, Irschik H, Müller R, Paterson I, Díaz JF, Altmann KH, Steinmetz MO.

Nat Commun. 2018 May 29;9(1):2106. doi: 10.1038/s41467-018-04535-8.

7.

Gallic acid sensitizes paclitaxel-resistant human ovarian carcinoma cells through an increase in reactive oxygen species and subsequent downregulation of ERK activation.

Sánchez-Carranza JN, Díaz JF, Redondo-Horcajo M, Barasoain I, Alvarez L, Lastres P, Romero-Estrada A, Aller P, González-Maya L.

Oncol Rep. 2018 Jun;39(6):3007-3014. doi: 10.3892/or.2018.6382. Epub 2018 Apr 18.

PMID:
29693189
8.

High-affinity ligands of the colchicine domain in tubulin based on a structure-guided design.

Bueno O, Estévez Gallego J, Martins S, Prota AE, Gago F, Gómez-SanJuan A, Camarasa MJ, Barasoain I, Steinmetz MO, Díaz JF, Pérez-Pérez MJ, Liekens S, Priego EM.

Sci Rep. 2018 Mar 9;8(1):4242. doi: 10.1038/s41598-018-22382-x.

9.

Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.

Bueno O, Tobajas G, Quesada E, Estévez-Gallego J, Noppen S, Camarasa MJ, Díaz JF, Liekens S, Priego EM, Pérez-Pérez MJ.

Eur J Med Chem. 2018 Mar 25;148:337-348. doi: 10.1016/j.ejmech.2018.02.019. Epub 2018 Feb 10.

PMID:
29471122
10.

Au@p4VP core@shell pH-sensitive nanocomposites suitable for drug entrapment.

Clara-Rahola J, Moscoso A, Belén Ruiz-Muelle A, Laurenti M, Formanek P, Lopez-Romero JM, Fernández I, Diaz JF, Rubio-Retama J, Fery A, Contreras-Cáceres R.

J Colloid Interface Sci. 2018 Mar 15;514:704-714. doi: 10.1016/j.jcis.2017.12.072. Epub 2017 Dec 31. Review.

PMID:
29310100
11.

Review of 494 Consecutive Breast Augmentation Patients: System to Improve Patient Outcomes and Satisfaction.

Diaz JF.

Plast Reconstr Surg Glob Open. 2017 Oct 20;5(10):e1526. doi: 10.1097/GOX.0000000000001526. eCollection 2017 Oct.

12.

Self-Organization of FtsZ Polymers in Solution Reveals Spacer Role of the Disordered C-Terminal Tail.

Huecas S, Ramírez-Aportela E, Vergoñós A, Núñez-Ramírez R, Llorca O, Díaz JF, Juan-Rodríguez D, Oliva MA, Castellen P, Andreu JM.

Biophys J. 2017 Oct 17;113(8):1831-1844. doi: 10.1016/j.bpj.2017.08.046.

13.

Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites.

Field JJ, Pera B, Gallego JE, Calvo E, Rodríguez-Salarichs J, Sáez-Calvo G, Zuwerra D, Jordi M, Andreu JM, Prota AE, Ménchon G, Miller JH, Altmann KH, Díaz JF.

J Nat Prod. 2018 Mar 23;81(3):494-505. doi: 10.1021/acs.jnatprod.7b00704. Epub 2017 Oct 12.

PMID:
29023132
14.

Quinolin-6-Yloxyacetamides Are Microtubule Destabilizing Agents That Bind to the Colchicine Site of Tubulin.

Sharma A, Sáez-Calvo G, Olieric N, de Asís Balaguer F, Barasoain I, Lamberth C, Díaz JF, Steinmetz MO.

Int J Mol Sci. 2017 Jun 22;18(7). pii: E1336. doi: 10.3390/ijms18071336.

15.

Modification of C-seco taxoids through ring tethering and substituent replacement leading to effective agents against tumor drug resistance mediated by βIII-Tubulin and P-glycoprotein (P-gp) overexpressions.

Tang Y, Rodríguez-Salarichs J, Zhao Y, Cai P, Estévez-Gallego J, Balaguer-Pérez F, Redondo Horcajo M, Lucena-Agell D, Barasoain I, Díaz JF, Fang WS.

Eur J Med Chem. 2017 Sep 8;137:488-503. doi: 10.1016/j.ejmech.2017.06.001. Epub 2017 Jun 3.

PMID:
28624703
16.

Triazolopyrimidines Are Microtubule-Stabilizing Agents that Bind the Vinca Inhibitor Site of Tubulin.

Sáez-Calvo G, Sharma A, Balaguer FA, Barasoain I, Rodríguez-Salarichs J, Olieric N, Muñoz-Hernández H, Berbís MÁ, Wendeborn S, Peñalva MA, Matesanz R, Canales Á, Prota AE, Jímenez-Barbero J, Andreu JM, Lamberth C, Steinmetz MO, Díaz JF.

Cell Chem Biol. 2017 Jun 22;24(6):737-750.e6. doi: 10.1016/j.chembiol.2017.05.016. Epub 2017 Jun 1.

17.

Zampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration.

Field JJ, Northcote PT, Paterson I, Altmann KH, Díaz JF, Miller JH.

Int J Mol Sci. 2017 May 3;18(5). pii: E971. doi: 10.3390/ijms18050971.

18.

Angina and Ischemia at 2 Years With Bioresorbable Vascular Scaffolds and Metallic Drug-eluting Stents. ESTROFA Ischemia BVS-mDES Study.

de la Torre Hernández JM, Rumoroso JR, Ojeda S, Brugaletta S, Cascón JD, Ruisánchez C, Sánchez Gila J, Roa J, Tizón H, Gutiérrez H, Larman M, García Camarero T, Pinar E, Díaz JF, Pan M, Morillas Bueno M, Oyonarte JM, Ruiz Guerrero L, Ble M, Rubio Patón R, Arnold R, Echegaray K, de la Morena G, Sabate M.

Rev Esp Cardiol (Engl Ed). 2018 May;71(5):327-334. doi: 10.1016/j.rec.2017.03.024. Epub 2017 Apr 29. English, Spanish.

PMID:
28461150
19.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention.

Bohnacker T, Prota AE, Beaufils F, Burke JE, Melone A, Inglis AJ, Rageot D, Sele AM, Cmiljanovic V, Cmiljanovic N, Bargsten K, Aher A, Akhmanova A, Díaz JF, Fabbro D, Zvelebil M, Williams RL, Steinmetz MO, Wymann MP.

Nat Commun. 2017 Mar 9;8:14683. doi: 10.1038/ncomms14683.

20.

Insights into the Distinct Mechanisms of Action of Taxane and Non-Taxane Microtubule Stabilizers from Cryo-EM Structures.

Kellogg EH, Hejab NMA, Howes S, Northcote P, Miller JH, Díaz JF, Downing KH, Nogales E.

J Mol Biol. 2017 Mar 10;429(5):633-646. doi: 10.1016/j.jmb.2017.01.001. Epub 2017 Jan 17.

21.

Structural Determinants of the Dictyostatin Chemotype for Tubulin Binding Affinity and Antitumor Activity Against Taxane- and Epothilone-Resistant Cancer Cells.

Trigili C, Barasoain I, Sánchez-Murcia PA, Bargsten K, Redondo-Horcajo M, Nogales A, Gardner NM, Meyer A, Naylor GJ, Gómez-Rubio E, Gago F, Steinmetz MO, Paterson I, Prota AE, Díaz JF.

ACS Omega. 2016 Dec 31;1(6):1192-1204. doi: 10.1021/acsomega.6b00317. Epub 2016 Dec 13.

22.

Outcomes and predictors of success and complications for paravalvular leak closure: an analysis of the SpanisH real-wOrld paravalvular LEaks closure (HOLE) registry.

García E, Arzamendi D, Jimenez-Quevedo P, Sarnago F, Martí G, Sanchez-Recalde A, Lasa-Larraya G, Sancho M, Iñiguez A, Goicolea J, Garcia-San Roman K, Alonso-Briales JH, Molina E, Calabuig J, Freixa X, Berenguer A, Valdes-Chavarri M, Vazquez N, Diaz JF, Cruz-Gonzalez I.

EuroIntervention. 2017 Mar 20;12(16):1962-1968. doi: 10.4244/EIJ-D-16-00581.

23.

Aggregated Compound Biological Signatures Facilitate Phenotypic Drug Discovery and Target Elucidation.

Cortes Cabrera A, Lucena-Agell D, Redondo-Horcajo M, Barasoain I, Díaz JF, Fasching B, Petrone PM.

ACS Chem Biol. 2016 Nov 18;11(11):3024-3034. Epub 2016 Sep 14.

PMID:
27564241
24.

Synthesis, Biological Profiling and Determination of the Tubulin-Bound Conformation of 12-Aza-Epothilones (Azathilones).

Jantsch A, Nieto L, Gertsch J, Rodríguez-Salarichs J, Matesanz R, Jiménez-Barbero J, Díaz JF, Canales Á, Altmann KH.

Molecules. 2016 Aug 3;21(8). pii: E1010. doi: 10.3390/molecules21081010.

25.

Structural and Biochemical Characterization of the Interaction of Tubulin with Potent Natural Analogues of Podophyllotoxin.

Antúnez-Mojica M, Rodríguez-Salarichs J, Redondo-Horcajo M, León A, Barasoain I, Canales Á, Cañada FJ, Jiménez-Barbero J, Alvarez L, Díaz JF.

J Nat Prod. 2016 Aug 26;79(8):2113-21. doi: 10.1021/acs.jnatprod.6b00428. Epub 2016 Aug 12.

PMID:
27518758
26.

Synthesis and Anti-Proliferative Activity of Sulfanyltriazolylnaphthalenols and Sulfanyltriazolylnaphthalene-1,4-diones.

Chaaban I, El Khawass el SM, Abd El Razik HA, El Salamouni NS, Redondo-Horcajo M, Barasoain I, Díaz JF, Yli-Kauhaluoma J, Moreira VM.

Arch Pharm (Weinheim). 2016 Sep;349(9):749-61. doi: 10.1002/ardp.201600134. Epub 2016 Jul 12.

PMID:
27404773
27.

Pironetin Binds Covalently to αCys316 and Perturbs a Major Loop and Helix of α-Tubulin to Inhibit Microtubule Formation.

Prota AE, Setter J, Waight AB, Bargsten K, Murga J, Diaz JF, Steinmetz MO.

J Mol Biol. 2016 Jul 31;428(15):2981-8. doi: 10.1016/j.jmb.2016.06.023. Epub 2016 Jul 6.

28.

Puncture Versus Surgical Cutdown Complications of Transfemoral Aortic Valve Implantation (from the Spanish TAVI Registry).

Hernández-Enriquez M, Andrea R, Brugaletta S, Jiménez-Quevedo P, Hernández-García JM, Trillo R, Larman M, Fernández-Avilés F, Vázquez-González N, Iñiguez A, Zueco J, Ruiz-Salmerón R, Del Valle R, Molina E, García Del Blanco B, Berenguer A, Valdés M, Moreno R, Urbano-Carrillo C, Hernández-Antolín R, Gimeno F, Cequier Á, Cruz I, López-Mínguez JR, Aramendi JI, Sánchez Á, Goicolea J, Albarrán A, Díaz JF, Navarro F, Moreu J, Morist A, Fernández-Nofrerías E, Fernández-Vázquez F, Ten F, Mainar V, Mari B, Saenz A, Alfonso F, Diarte JA, Sancho M, Lezáun R, Arzamendi D, Sabaté M.

Am J Cardiol. 2016 Aug 15;118(4):578-84. doi: 10.1016/j.amjcard.2016.05.054. Epub 2016 May 29.

PMID:
27378142
29.

Antivascular and antitumor properties of the tubulin-binding chalcone TUB091.

Canela MD, Noppen S, Bueno O, Prota AE, Bargsten K, Sáez-Calvo G, Jimeno ML, Benkheil M, Ribatti D, Velázquez S, Camarasa MJ, Díaz JF, Steinmetz MO, Priego EM, Pérez-Pérez MJ, Liekens S.

Oncotarget. 2017 Feb 28;8(9):14325-14342. doi: 10.18632/oncotarget.9527.

30.

Restoration of Microtubule Interaction and Cytotoxicity in D-seco Taxanes upon Incorporation of 20-Hydroxymethyl-4-allyloxy Groups.

Wang SR, Yang CG, Sánchez-Murcia PA, Snyder JP, Yan N, Sáez-Calvo G, Díaz JF, Gago F, Fang WS.

Org Lett. 2015 Dec 18;17(24):6098-101. doi: 10.1021/acs.orglett.5b03119. Epub 2015 Dec 9.

PMID:
26649936
31.

High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells.

Pera B, Calvo-Vidal MN, Ambati S, Jordi M, Kahn A, Díaz JF, Fang W, Altmann KH, Cerchietti L, Moore MAS.

Cancer Lett. 2015 Nov 1;368(1):97-104. doi: 10.1016/j.canlet.2015.07.038. Epub 2015 Aug 12.

32.

Cytotoxic Activity and Chemical Composition of the Root Extract from the Mexican Species Linum scabrellum: Mechanism of Action of the Active Compound 6-Methoxypodophyllotoxin.

Alejandre-García I, Álvarez L, Cardoso-Taketa A, González-Maya L, Antúnez M, Salas-Vidal E, Díaz JF, Marquina-Bahena S, Villarreal ML.

Evid Based Complement Alternat Med. 2015;2015:298463. doi: 10.1155/2015/298463. Epub 2015 Jul 12.

33.

Secretory meningioma with KLF4 K409Q mutation in collision with glioma.

Ruiz J, Capilla E, Díaz JF, Ruiz JA, Andrade J, Hernández T, Mollejo M, Meléndez B.

Clin Neuropathol. 2015 Nov-Dec;34(6):322-9. doi: 10.5414/NP300860.

PMID:
26227255
34.

Synthesis, Characterization, and Application in HeLa Cells of an NIR Light Responsive Doxorubicin Delivery System Based on NaYF4:Yb,Tm@SiO2-PEG Nanoparticles.

Alonso-Cristobal P, Oton-Fernandez O, Mendez-Gonzalez D, Díaz JF, Lopez-Cabarcos E, Barasoain I, Rubio-Retama J.

ACS Appl Mater Interfaces. 2015 Jul 15;7(27):14992-9. doi: 10.1021/acsami.5b03881. Epub 2015 Jul 6.

PMID:
26094748
35.

The Mechanism of the Interactions of Pironetin Analog/Combretastatin A-4 Hybrids with Tubulin.

Torijano-Gutiérrez S, Vilanova C, Díaz-Oltra S, Murga J, Falomir E, Carda M, Redondo-Horcajo M, Díaz JF, Barasoain I, Marco JA.

Arch Pharm (Weinheim). 2015 Aug;348(8):541-7. doi: 10.1002/ardp.201500106. Epub 2015 Jun 17.

PMID:
26085125
36.

Total Synthesis of Amphidinolide K, a Macrolide That Stabilizes F-Actin.

Sánchez D, Andreou T, Costa AM, Meyer KG, Williams DR, Barasoain I, Díaz JF, Lucena-Agell D, Vilarrasa J.

J Org Chem. 2015 Sep 4;80(17):8511-9. doi: 10.1021/acs.joc.5b00966. Epub 2015 Jun 23.

PMID:
26079383
37.

TRAPPII regulates exocytic Golgi exit by mediating nucleotide exchange on the Ypt31 ortholog RabERAB11.

Pinar M, Arst HN Jr, Pantazopoulou A, Tagua VG, de los Ríos V, Rodríguez-Salarichs J, Díaz JF, Peñalva MA.

Proc Natl Acad Sci U S A. 2015 Apr 7;112(14):4346-51. doi: 10.1073/pnas.1419168112. Epub 2015 Mar 23.

38.

Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents.

Chaaban I, El Khawass el SM, Abd El Razik HA, El Salamouni NS, Redondo-Horcajo M, Barasoain I, Díaz JF, Yli-Kauhaluoma J, Moreira VM.

Eur J Med Chem. 2014 Nov 24;87:805-13. doi: 10.1016/j.ejmech.2014.10.015. Epub 2014 Oct 13.

PMID:
25440882
39.

Design and synthesis of pironetin analogue/colchicine hybrids and study of their cytotoxic activity and mechanisms of interaction with tubulin.

Vilanova C, Díaz-Oltra S, Murga J, Falomir E, Carda M, Redondo-Horcajo M, Díaz JF, Barasoain I, Marco JA.

J Med Chem. 2014 Dec 26;57(24):10391-403. doi: 10.1021/jm501112q. Epub 2014 Dec 12.

PMID:
25426924
40.

Edge vascular response after polymer-free vs. polymer-based paclitaxel-eluting stent implantation.

Otsuki S, Shiratori Y, Brugaletta S, Cola C, García Del Blanco B, Ruiz-Salmeron R, Díaz JF, Pinar E, Martí V, García-Picart J, Martín-Yuste V, Sabaté M.

Circ J. 2014;78(11):2657-64. Epub 2014 Sep 22.

41.

A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs.

Prota AE, Bargsten K, Diaz JF, Marsh M, Cuevas C, Liniger M, Neuhaus C, Andreu JM, Altmann KH, Steinmetz MO.

Proc Natl Acad Sci U S A. 2014 Sep 23;111(38):13817-21. doi: 10.1073/pnas.1408124111. Epub 2014 Aug 11.

42.

Taxanes with high potency inducing tubulin assembly overcome tumoural cell resistances.

Matesanz R, Trigili C, Rodríguez-Salarichs J, Zanardi I, Pera B, Nogales A, Fang WS, Jímenez-Barbero J, Canales A, Barasoain I, Ojima I, Díaz JF.

Bioorg Med Chem. 2014 Sep 15;22(18):5078-90. doi: 10.1016/j.bmc.2014.05.048. Epub 2014 Jun 19.

43.

The impact of cyclopropane configuration on the biological activity of cyclopropyl-epothilones.

Gaugaz FZ, Redondo-Horcajo M, Barasoain I, Díaz JF, Cobos-Correa A, Kaufmann M, Altmann KH.

ChemMedChem. 2014 Oct;9(10):2227-32. doi: 10.1002/cmdc.201402129. Epub 2014 Jul 8.

PMID:
25045073
44.

Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach.

Canela MD, Pérez-Pérez MJ, Noppen S, Sáez-Calvo G, Díaz JF, Camarasa MJ, Liekens S, Priego EM.

J Med Chem. 2014 May 22;57(10):3924-38. doi: 10.1021/jm401939g. Epub 2014 May 9.

45.

The diamagnetic susceptibility of the tubulin dimer.

Bras W, Torbet J, Diakun GP, Rikken GL, Diaz JF.

J Biophys. 2014;2014:985082. doi: 10.1155/2014/985082. Epub 2014 Feb 18.

46.

Molecular recognition of epothilones by microtubules and tubulin dimers revealed by biochemical and NMR approaches.

Canales A, Nieto L, Rodríguez-Salarichs J, Sánchez-Murcia PA, Coderch C, Cortés-Cabrera A, Paterson I, Carlomagno T, Gago F, Andreu JM, Altmann KH, Jiménez-Barbero J, Díaz JF.

ACS Chem Biol. 2014 Apr 18;9(4):1033-43. doi: 10.1021/cb400673h. Epub 2014 Feb 25.

47.

PM060184, a new tubulin binding agent with potent antitumor activity including P-glycoprotein over-expressing tumors.

Martínez-Díez M, Guillén-Navarro MJ, Pera B, Bouchet BP, Martínez-Leal JF, Barasoain I, Cuevas C, Andreu JM, García-Fernández LF, Díaz JF, Avilés P, Galmarini CM.

Biochem Pharmacol. 2014 Apr 1;88(3):291-302. doi: 10.1016/j.bcp.2014.01.026. Epub 2014 Jan 31.

PMID:
24486569
48.

Structural basis of microtubule stabilization by laulimalide and peloruside A.

Prota AE, Bargsten K, Northcote PT, Marsh M, Altmann KH, Miller JH, Díaz JF, Steinmetz MO.

Angew Chem Int Ed Engl. 2014 Feb 3;53(6):1621-5. doi: 10.1002/anie.201307749. Epub 2014 Jan 27.

PMID:
24470331
49.

Optimally designed quantum transport across disordered networks.

Walschaers M, Diaz JF, Mulet R, Buchleitner A.

Phys Rev Lett. 2013 Nov 1;111(18):180601. Epub 2013 Oct 29.

PMID:
24237498
50.

Methods for studying microtubule binding site interactions: zampanolide as a covalent binding agent.

Field JJ, Calvo E, Northcote PT, Miller JH, Altmann KH, Díaz JF.

Methods Cell Biol. 2013;115:303-25. doi: 10.1016/B978-0-12-407757-7.00019-0.

PMID:
23973080

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