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Items: 1 to 50 of 118

1.

A driving test for oncogenic mutations.

Heppner DE, Beyett TS, Eck MJ.

J Biol Chem. 2019 Jun 14;294(24):9390-9391. doi: 10.1074/jbc.H119.009452.

PMID:
31201242
2.

Single and dual targeting of mutant EGFR with an allosteric inhibitor.

To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, Eck MJ, Gray NS, Janne PA.

Cancer Discov. 2019 May 15. pii: CD-18-0903. doi: 10.1158/2159-8290.CD-18-0903. [Epub ahead of print]

PMID:
31092401
3.

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

McNally R, Li Q, Li K, Dekker C, Vangrevelinghe E, Jones M, Chène P, Machauer R, Radimerski T, Eck MJ.

ACS Chem Biol. 2019 Apr 19;14(4):587-593. doi: 10.1021/acschembio.8b00722. Epub 2019 Mar 11.

PMID:
30763067
4.

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.

Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS.

Angew Chem Int Ed Engl. 2018 Sep 3;57(36):11629-11633. doi: 10.1002/anie.201805187. Epub 2018 Aug 3.

5.

Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.

Wang Y, Li YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ.

Elife. 2018 Mar 12;7. pii: e36414. doi: 10.7554/eLife.36414. No abstract available.

6.

MELK is not necessary for the proliferation of basal-like breast cancer cells.

Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS.

Elife. 2017 Sep 19;6. pii: e26693. doi: 10.7554/eLife.26693.

7.

Crystal Structure of Leiomodin 2 in Complex with Actin: A Structural and Functional Reexamination.

Boczkowska M, Yurtsever Z, Rebowski G, Eck MJ, Dominguez R.

Biophys J. 2017 Aug 22;113(4):889-899. doi: 10.1016/j.bpj.2017.07.007.

8.

CRKL Mediates p110β-Dependent PI3K Signaling in PTEN-Deficient Cancer Cells.

Zhang J, Gao X, Schmit F, Adelmant G, Eck MJ, Marto JA, Zhao JJ, Roberts TM.

Cell Rep. 2017 Jul 18;20(3):549-557. doi: 10.1016/j.celrep.2017.06.054.

9.

Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors.

Kosaka T, Tanizaki J, Paranal RM, Endoh H, Lydon C, Capelletti M, Repellin CE, Choi J, Ogino A, Calles A, Ercan D, Redig AJ, Bahcall M, Oxnard GR, Eck MJ, Jänne PA.

Cancer Res. 2017 May 15;77(10):2712-2721. doi: 10.1158/0008-5472.CAN-16-3404. Epub 2017 Mar 31.

10.

Domain-dependent effects of insulin and IGF-1 receptors on signalling and gene expression.

Cai W, Sakaguchi M, Kleinridders A, Gonzalez-Del Pino G, Dreyfuss JM, O'Neill BT, Ramirez AK, Pan H, Winnay JN, Boucher J, Eck MJ, Kahn CR.

Nat Commun. 2017 Mar 27;8:14892. doi: 10.1038/ncomms14892.

11.

Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes.

Ficarro SB, Browne CM, Card JD, Alexander WM, Zhang T, Park E, McNally R, Dhe-Paganon S, Seo HS, Lamberto I, Eck MJ, Buhrlage SJ, Gray NS, Marto JA.

Anal Chem. 2016 Dec 20;88(24):12248-12254. doi: 10.1021/acs.analchem.6b03394. Epub 2016 Nov 30.

PMID:
28193034
12.

Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival.

Wang Y, Begley M, Li Q, Huang HT, Lako A, Eck MJ, Gray NS, Mitchison TJ, Cantley LC, Zhao JJ.

Proc Natl Acad Sci U S A. 2016 Aug 30;113(35):9810-5. doi: 10.1073/pnas.1606862113. Epub 2016 Aug 15.

13.

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.

Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ.

Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25.

14.

Crystal Structure of the FERM-SH2 Module of Human Jak2.

McNally R, Toms AV, Eck MJ.

PLoS One. 2016 May 26;11(5):e0156218. doi: 10.1371/journal.pone.0156218. eCollection 2016.

15.

Data publication with the structural biology data grid supports live analysis.

Meyer PA, Socias S, Key J, Ransey E, Tjon EC, Buschiazzo A, Lei M, Botka C, Withrow J, Neau D, Rajashankar K, Anderson KS, Baxter RH, Blacklow SC, Boggon TJ, Bonvin AM, Borek D, Brett TJ, Caflisch A, Chang CI, Chazin WJ, Corbett KD, Cosgrove MS, Crosson S, Dhe-Paganon S, Di Cera E, Drennan CL, Eck MJ, Eichman BF, Fan QR, Ferré-D'Amaré AR, Fromme JC, Garcia KC, Gaudet R, Gong P, Harrison SC, Heldwein EE, Jia Z, Keenan RJ, Kruse AC, Kvansakul M, McLellan JS, Modis Y, Nam Y, Otwinowski Z, Pai EF, Pereira PJ, Petosa C, Raman CS, Rapoport TA, Roll-Mecak A, Rosen MK, Rudenko G, Schlessinger J, Schwartz TU, Shamoo Y, Sondermann H, Tao YJ, Tolia NH, Tsodikov OV, Westover KD, Wu H, Foster I, Fraser JS, Maia FR, Gonen T, Kirchhausen T, Diederichs K, Crosas M, Sliz P.

Nat Commun. 2016 Mar 7;7:10882. doi: 10.1038/ncomms10882.

16.

SPLINTS: small-molecule protein ligand interface stabilizers.

Fischer ES, Park E, Eck MJ, Thomä NH.

Curr Opin Struct Biol. 2016 Apr;37:115-22. doi: 10.1016/j.sbi.2016.01.004. Epub 2016 Jan 30. Review.

17.

EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src.

Begley MJ, Yun CH, Gewinner CA, Asara JM, Johnson JL, Coyle AJ, Eck MJ, Apostolou I, Cantley LC.

Nat Struct Mol Biol. 2015 Dec;22(12):983-90. doi: 10.1038/nsmb.3117. Epub 2015 Nov 9.

18.

Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6.

Park E, Kim N, Ficarro SB, Zhang Y, Lee BI, Cho A, Kim K, Park AKJ, Park WY, Murray B, Meyerson M, Beroukhim R, Marto JA, Cho J, Eck MJ.

Nat Struct Mol Biol. 2015 Sep;22(9):703-711. doi: 10.1038/nsmb.3074. Epub 2015 Aug 17.

19.

Development of Selective Covalent Janus Kinase 3 Inhibitors.

Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella K, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, Look TA, Arthur JS, Eck MJ, Gray NS.

J Med Chem. 2015 Aug 27;58(16):6589-606. doi: 10.1021/acs.jmedchem.5b00710. Epub 2015 Aug 18.

20.

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

Wu SC, Li LS, Kopp N, Montero J, Chapuy B, Yoda A, Christie AL, Liu H, Christodoulou A, van Bodegom D, van der Zwet J, Layer JV, Tivey T, Lane AA, Ryan JA, Ng SY, DeAngelo DJ, Stone RM, Steensma D, Wadleigh M, Harris M, Mandon E, Ebel N, Andraos R, Romanet V, Dölemeyer A, Sterker D, Zender M, Rodig SJ, Murakami M, Hofmann F, Kuo F, Eck MJ, Silverman LB, Sallan SE, Letai A, Baffert F, Vangrevelinghe E, Radimerski T, Gaul C, Weinstock DM.

Cancer Cell. 2015 Jul 13;28(1):29-41. doi: 10.1016/j.ccell.2015.06.005.

21.

Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia.

Wu H, Hu C, Wang A, Weisberg EL, Chen Y, Yun CH, Wang W, Liu Y, Liu X, Tian B, Wang J, Zhao Z, Liang Y, Li B, Wang L, Wang B, Chen C, Buhrlage SJ, Qi Z, Zou F, Nonami A, Li Y, Fernandes SM, Adamia S, Stone RM, Galinsky IA, Wang X, Yang G, Griffin JD, Brown JR, Eck MJ, Liu J, Gray NS, Liu Q.

Leukemia. 2016 Jan;30(1):173-81. doi: 10.1038/leu.2015.180. Epub 2015 Jul 13.

22.

Structure of a Bud6/Actin Complex Reveals a Novel WH2-like Actin Monomer Recruitment Motif.

Park E, Graziano BR, Zheng W, Garabedian M, Goode BL, Eck MJ.

Structure. 2015 Aug 4;23(8):1492-1499. doi: 10.1016/j.str.2015.05.015. Epub 2015 Jun 25.

23.

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors.

Ercan D, Choi HG, Yun CH, Capelletti M, Xie T, Eck MJ, Gray NS, Jänne PA.

Clin Cancer Res. 2015 Sep 1;21(17):3913-23. doi: 10.1158/1078-0432.CCR-14-2789. Epub 2015 May 6.

24.

PARP1-driven poly-ADP-ribosylation regulates BRCA1 function in homologous recombination-mediated DNA repair.

Hu Y, Petit SA, Ficarro SB, Toomire KJ, Xie A, Lim E, Cao SA, Park E, Eck MJ, Scully R, Brown M, Marto JA, Livingston DM.

Cancer Discov. 2014 Dec;4(12):1430-47. doi: 10.1158/2159-8290.CD-13-0891. Epub 2014 Sep 24.

25.

Phosphatidylinositol 4,5-bisphosphate triggers activation of focal adhesion kinase by inducing clustering and conformational changes.

Goñi GM, Epifano C, Boskovic J, Camacho-Artacho M, Zhou J, Bronowska A, Martín MT, Eck MJ, Kremer L, Gräter F, Gervasio FL, Perez-Moreno M, Lietha D.

Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):E3177-86. doi: 10.1073/pnas.1317022111. Epub 2014 Jul 21.

26.

Colon cancer-derived oncogenic EGFR G724S mutant identified by whole genome sequence analysis is dependent on asymmetric dimerization and sensitive to cetuximab.

Cho J, Bass AJ, Lawrence MS, Cibulskis K, Cho A, Lee SN, Yamauchi M, Wagle N, Pochanard P, Kim N, Park AK, Won J, Hur HS, Greulich H, Ogino S, Sougnez C, Voet D, Tabernero J, Jimenez J, Baselga J, Gabriel SB, Lander ES, Getz G, Eck MJ, Park WY, Meyerson M.

Mol Cancer. 2014 Jun 4;13:141. doi: 10.1186/1476-4598-13-141.

27.

MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.

Wang Y, Lee YM, Baitsch L, Huang A, Xiang Y, Tong H, Lako A, Von T, Choi C, Lim E, Min J, Li L, Stegmeier F, Schlegel R, Eck MJ, Gray NS, Mitchison TJ, Zhao JJ.

Elife. 2014 May 20;3:e01763. doi: 10.7554/eLife.01763. Erratum in: Elife. 2018 Mar 12;7:.

28.

JAK-cytokine receptor recognition, unboxed.

McNally R, Eck MJ.

Nat Struct Mol Biol. 2014 May;21(5):431-3. doi: 10.1038/nsmb.2824. No abstract available.

PMID:
24799036
29.

Inhibition of KRAS-driven tumorigenicity by interruption of an autocrine cytokine circuit.

Zhu Z, Aref AR, Cohoon TJ, Barbie TU, Imamura Y, Yang S, Moody SE, Shen RR, Schinzel AC, Thai TC, Reibel JB, Tamayo P, Godfrey JT, Qian ZR, Page AN, Maciag K, Chan EM, Silkworth W, Labowsky MT, Rozhansky L, Mesirov JP, Gillanders WE, Ogino S, Hacohen N, Gaudet S, Eck MJ, Engelman JA, Corcoran RB, Wong KK, Hahn WC, Barbie DA.

Cancer Discov. 2014 Apr;4(4):452-65. doi: 10.1158/2159-8290.CD-13-0646. Epub 2014 Jan 20.

30.

Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer.

Yasuda H, Park E, Yun CH, Sng NJ, Lucena-Araujo AR, Yeo WL, Huberman MS, Cohen DW, Nakayama S, Ishioka K, Yamaguchi N, Hanna M, Oxnard GR, Lathan CS, Moran T, Sequist LV, Chaft JE, Riely GJ, Arcila ME, Soo RA, Meyerson M, Eck MJ, Kobayashi SS, Costa DB.

Sci Transl Med. 2013 Dec 18;5(216):216ra177. doi: 10.1126/scitranslmed.3007205. Erratum in: Sci Transl Med. 2014 Feb 26;6(225):225er1.

31.

Cetuximab response of lung cancer-derived EGF receptor mutants is associated with asymmetric dimerization.

Cho J, Chen L, Sangji N, Okabe T, Yonesaka K, Francis JM, Flavin RJ, Johnson W, Kwon J, Yu S, Greulich H, Johnson BE, Eck MJ, Jänne PA, Wong KK, Meyerson M.

Cancer Res. 2013 Nov 15;73(22):6770-9. doi: 10.1158/0008-5472.CAN-13-1145. Epub 2013 Sep 24.

32.

Mechanism for activation of mutated epidermal growth factor receptors in lung cancer.

Red Brewer M, Yun CH, Lai D, Lemmon MA, Eck MJ, Pao W.

Proc Natl Acad Sci U S A. 2013 Sep 17;110(38):E3595-604. doi: 10.1073/pnas.1220050110. Epub 2013 Sep 9. Erratum in: Proc Natl Acad Sci U S A. 2013 Dec 10;110(50):20344.

33.

Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases.

Toms AV, Deshpande A, McNally R, Jeong Y, Rogers JM, Kim CU, Gruner SM, Ficarro SB, Marto JA, Sattler M, Griffin JD, Eck MJ.

Nat Struct Mol Biol. 2013 Oct;20(10):1221-3. doi: 10.1038/nsmb.2673. Epub 2013 Sep 8.

34.

Structure-guided inhibitor design expands the scope of analog-sensitive kinase technology.

Zhang C, Lopez MS, Dar AC, Ladow E, Finkbeiner S, Yun CH, Eck MJ, Shokat KM.

ACS Chem Biol. 2013 Sep 20;8(9):1931-8. doi: 10.1021/cb400376p. Epub 2013 Jul 23.

35.

Structure and ubiquitination-dependent activation of TANK-binding kinase 1.

Tu D, Zhu Z, Zhou AY, Yun CH, Lee KE, Toms AV, Li Y, Dunn GP, Chan E, Thai T, Yang S, Ficarro SB, Marto JA, Jeon H, Hahn WC, Barbie DA, Eck MJ.

Cell Rep. 2013 Mar 28;3(3):747-58. doi: 10.1016/j.celrep.2013.01.033. Epub 2013 Feb 28.

36.

Structure of the formin-interaction domain of the actin nucleation-promoting factor Bud6.

Tu D, Graziano BR, Park E, Zheng W, Li Y, Goode BL, Eck MJ.

Proc Natl Acad Sci U S A. 2012 Dec 11;109(50):E3424-33. doi: 10.1073/pnas.1203035109. Epub 2012 Nov 16.

37.

Functional analysis of receptor tyrosine kinase mutations in lung cancer identifies oncogenic extracellular domain mutations of ERBB2.

Greulich H, Kaplan B, Mertins P, Chen TH, Tanaka KE, Yun CH, Zhang X, Lee SH, Cho J, Ambrogio L, Liao R, Imielinski M, Banerji S, Berger AH, Lawrence MS, Zhang J, Pho NH, Walker SR, Winckler W, Getz G, Frank D, Hahn WC, Eck MJ, Mani DR, Jaffe JD, Carr SA, Wong KK, Meyerson M.

Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14476-81. doi: 10.1073/pnas.1203201109. Epub 2012 Aug 20.

38.

Cyclic di-GMP sensing via the innate immune signaling protein STING.

Yin Q, Tian Y, Kabaleeswaran V, Jiang X, Tu D, Eck MJ, Chen ZJ, Wu H.

Mol Cell. 2012 Jun 29;46(6):735-45. doi: 10.1016/j.molcel.2012.05.029. Epub 2012 Jun 14.

39.

EGFR in limbo.

Eck MJ, Hahn WC.

Cell. 2012 May 11;149(4):735-7. doi: 10.1016/j.cell.2012.04.015.

40.

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer.

Hammerman PS, Sos ML, Ramos AH, Xu C, Dutt A, Zhou W, Brace LE, Woods BA, Lin W, Zhang J, Deng X, Lim SM, Heynck S, Peifer M, Simard JR, Lawrence MS, Onofrio RC, Salvesen HB, Seidel D, Zander T, Heuckmann JM, Soltermann A, Moch H, Koker M, Leenders F, Gabler F, Querings S, Ansén S, Brambilla E, Brambilla C, Lorimier P, Brustugun OT, Helland A, Petersen I, Clement JH, Groen H, Timens W, Sietsma H, Stoelben E, Wolf J, Beer DG, Tsao MS, Hanna M, Hatton C, Eck MJ, Janne PA, Johnson BE, Winckler W, Greulich H, Bass AJ, Cho J, Rauh D, Gray NS, Wong KK, Haura EB, Thomas RK, Meyerson M.

Cancer Discov. 2011 Jun;1(1):78-89. doi: 10.1158/2159-8274.CD-11-0005.

41.

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Weigert O, Lane AA, Bird L, Kopp N, Chapuy B, van Bodegom D, Toms AV, Marubayashi S, Christie AL, McKeown M, Paranal RM, Bradner JE, Yoda A, Gaul C, Vangrevelinghe E, Romanet V, Murakami M, Tiedt R, Ebel N, Evrot E, De Pover A, Régnier CH, Erdmann D, Hofmann F, Eck MJ, Sallan SE, Levine RL, Kung AL, Baffert F, Radimerski T, Weinstock DM.

J Exp Med. 2012 Feb 13;209(2):259-73. doi: 10.1084/jem.20111694. Epub 2012 Jan 23.

42.

EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.

He M, Capelletti M, Nafa K, Yun CH, Arcila ME, Miller VA, Ginsberg MS, Zhao B, Kris MG, Eck MJ, Jänne PA, Ladanyi M, Oxnard GR.

Clin Cancer Res. 2012 Mar 15;18(6):1790-7. doi: 10.1158/1078-0432.CCR-11-2361. Epub 2011 Dec 21.

43.

A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors.

Sasaki T, Koivunen J, Ogino A, Yanagita M, Nikiforow S, Zheng W, Lathan C, Marcoux JP, Du J, Okuda K, Capelletti M, Shimamura T, Ercan D, Stumpfova M, Xiao Y, Weremowicz S, Butaney M, Heon S, Wilner K, Christensen JG, Eck MJ, Wong KK, Lindeman N, Gray NS, Rodig SJ, Jänne PA.

Cancer Res. 2011 Sep 15;71(18):6051-60. doi: 10.1158/0008-5472.CAN-11-1340. Epub 2011 Jul 26.

44.

Structure and function of the interacting domains of Spire and Fmn-family formins.

Vizcarra CL, Kreutz B, Rodal AA, Toms AV, Lu J, Zheng W, Quinlan ME, Eck MJ.

Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):11884-9. doi: 10.1073/pnas.1105703108. Epub 2011 Jul 5.

45.

Crystal structure of a coiled-coil domain from human ROCK I.

Tu D, Li Y, Song HK, Toms AV, Gould CJ, Ficarro SB, Marto JA, Goode BL, Eck MJ.

PLoS One. 2011 Mar 21;6(3):e18080. doi: 10.1371/journal.pone.0018080.

46.

The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.

Sasaki T, Okuda K, Zheng W, Butrynski J, Capelletti M, Wang L, Gray NS, Wilner K, Christensen JG, Demetri G, Shapiro GI, Rodig SJ, Eck MJ, Jänne PA.

Cancer Res. 2010 Dec 15;70(24):10038-43. doi: 10.1158/0008-5472.CAN-10-2956. Epub 2010 Oct 28.

47.

The FERM domain: organizing the structure and function of FAK.

Frame MC, Patel H, Serrels B, Lietha D, Eck MJ.

Nat Rev Mol Cell Biol. 2010 Nov;11(11):802-14. doi: 10.1038/nrm2996. Review.

PMID:
20966971
48.

Crystal structure of a complex between amino and carboxy terminal fragments of mDia1: insights into autoinhibition of diaphanous-related formins.

Nezami A, Poy F, Toms A, Zheng W, Eck MJ.

PLoS One. 2010 Sep 30;5(9). pii: e12992. doi: 10.1371/journal.pone.0012992.

49.

Structural basis for the recognition of N-end rule substrates by the UBR box of ubiquitin ligases.

Choi WS, Jeong BC, Joo YJ, Lee MR, Kim J, Eck MJ, Song HK.

Nat Struct Mol Biol. 2010 Oct;17(10):1175-81. doi: 10.1038/nsmb.1907. Epub 2010 Sep 12.

PMID:
20835240
50.

Binucleine 2, an isoform-specific inhibitor of Drosophila Aurora B kinase, provides insights into the mechanism of cytokinesis.

Smurnyy Y, Toms AV, Hickson GR, Eck MJ, Eggert US.

ACS Chem Biol. 2010 Nov 19;5(11):1015-20. doi: 10.1021/cb1001685.

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