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JAK2 V617F Constitutive Activation Requires JH2 Residue F595: A Pseudokinase Domain Target for Specific Inhibitors

Bibliographic reference Dusa, Alexandra ; Mouton, Céline ; Pecquet, Christian ; Herman, Murielle ; Constantinescu, Stefan N.. JAK2 V617F Constitutive Activation Requires JH2 Residue F595: A Pseudokinase Domain Target for Specific Inhibitors. In: PLoS One, Vol. 5, no. 6, p. e11157 (2010)
Permanent URL http://hdl.handle.net/2078.1/33759
  1. Ziemiecki Andrew, Harpur Ailsa G., Wilks Andrew F., JAK protein tyrosine kinases: their role in cytokine signalling, 10.1016/0962-8924(94)90143-0
  2. JA Girault, Mol Med, 4, 751 (1998)
  3. Huang Lily Jun-shen, Constantinescu Stefan N., Lodish Harvey F., The N-Terminal Domain of Janus Kinase 2 Is Required for Golgi Processing and Cell Surface Expression of Erythropoietin Receptor, 10.1016/s1097-2765(01)00401-4
  4. Radtke Simone, Hermanns Heike M., Haan Claude, Schmitz-Van de Leur Hildegard, Gascan Hugues, Heinrich Peter C., Behrmann Iris, Novel Role of Janus Kinase 1 in the Regulation of Oncostatin M Receptor Surface Expression, 10.1074/jbc.m100822200
  5. Royer Yohan, Staerk Judith, Costuleanu Marcel, Courtoy Pierre J., Constantinescu Stefan N., Janus Kinases Affect Thrombopoietin Receptor Cell Surface Localization and Stability, 10.1074/jbc.m501376200
  6. Radtke Simone, Haan Serge, Jörissen Angela, Hermanns Heike M., Diefenbach Sandra, Smyczek Tanya, Schmitz-VandeLeur Hildegard, Heinrich Peter C., Behrmann Iris, Haan Claude, The Jak1 SH2 Domain Does Not Fulfill a Classical SH2 Function in Jak/STAT Signaling but Plays a Structural Role for Receptor Interaction and Up-regulation of Receptor Surface Expression, 10.1074/jbc.m500822200
  7. AG Harpur, Oncogene, 7, 1347 (1992)
  8. Saharinen Pipsa, Silvennoinen Olli, The Pseudokinase Domain Is Required for Suppression of Basal Activity of Jak2 and Jak3 Tyrosine Kinases and for Cytokine-inducible Activation of Signal Transduction, 10.1074/jbc.m205156200
  9. Saharinen P., Autoinhibition of Jak2 Tyrosine Kinase Is Dependent on Specific Regions in Its Pseudokinase Domain, 10.1091/mbc.e02-06-0342
  10. Lucet I. S., The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor, 10.1182/blood-2005-06-2413
  11. Boggon T. J., Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog, 10.1182/blood-2005-02-0707
  12. NK Williams, J Mol Biol (2009)
  13. Sicheri Frank, Moarefi Ismail, Kuriyan John, Crystal structure of the Src family tyrosine kinase Hck, 10.1038/385602a0
  14. De Bondt Hendrik L., Rosenblatt Jody, Jancarik Jarmila, Jones Heather D., Morgant David O., Kim Sung-Hou, Crystal structure of cyclin-dependent kinase 2, 10.1038/363595a0
  15. James Chloé, Ugo Valérie, Le Couédic Jean-Pierre, Staerk Judith, Delhommeau François, Lacout Catherine, Garçon Loïc, Raslova Hana, Berger Roland, Bennaceur-Griscelli Annelise, Villeval Jean Luc, Constantinescu Stefan N., Casadevall Nicole, Vainchenker William, A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera, 10.1038/nature03546
  16. BAXTER E, SCOTT L, CAMPBELL P, EAST C, FOUROUCLAS N, SWANTON S, VASSILIOU G, BENCH A, BOYD E, CURTIN N, Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders, 10.1016/s0140-6736(05)74230-6
  17. Levine Ross L., Wadleigh Martha, Cools Jan, Ebert Benjamin L., Wernig Gerlinde, Huntly Brian J.P., Boggon Titus J., Wlodarska Iwona, Clark Jennifer J., Moore Sandra, Adelsperger Jennifer, Koo Sumin, Lee Jeffrey C., Gabriel Stacey, Mercher Thomas, D’Andrea Alan, Fröhling Stefan, Döhner Konstanze, Marynen Peter, Vandenberghe Peter, Mesa Ruben A., Tefferi Ayalew, Griffin James D., Eck Michael J., Sellers William R., Meyerson Matthew, Golub Todd R., Lee Stephanie J., Gilliland D. Gary, Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis, 10.1016/j.ccr.2005.03.023
  18. Kralovics Robert, Passamonti Francesco, Buser Andreas S., Teo Soon-Siong, Tiedt Ralph, Passweg Jakob R., Tichelli Andre, Cazzola Mario, Skoda Radek C., A Gain-of-Function Mutation ofJAK2in Myeloproliferative Disorders, 10.1056/nejmoa051113
  19. Lindauer Klaus, Loerting Thomas, Liedl Klaus R., Kroemer Romano T., Prediction of the structure of human Janus kinase 2 (JAK2) comprising the two carboxy-terminal domains reveals a mechanism for autoregulation, 10.1093/protein/14.1.27
  20. Williams John C, Weijland Albert, Gonfloni Stefania, Thompson Andy, Courtneidge Sara A, Superti-Furga Giulio, Wierenga Rik K, The 2.35 å crystal structure of the inactivated form of chicken src: a dynamic molecule with multiple regulatory interactions, 10.1006/jmbi.1997.1426
  21. Filippakopoulos Panagis, Kofler Michael, Hantschel Oliver, Gish Gerald D., Grebien Florian, Salah Eidarus, Neudecker Philipp, Kay Lewis E., Turk Benjamin E., Superti-Furga Giulio, Pawson Tony, Knapp Stefan, Structural Coupling of SH2-Kinase Domains Links Fes and Abl Substrate Recognition and Kinase Activation, 10.1016/j.cell.2008.07.047
  22. Huse Morgan, Kuriyan John, The Conformational Plasticity of Protein Kinases, 10.1016/s0092-8674(02)00741-9
  23. Xu Wenqing, Harrison Stephen C., Eck Michael J., Three-dimensional structure of the tyrosine kinase c-Src, 10.1038/385595a0
  24. Superti-Furga Giulio, Gonfloni Stefania, Frischknecht Friedrich, Way Michael, 10.1038/11537
  25. Deindl Sebastian, Kadlecek Theresa A., Brdicka Tomas, Cao Xiaoxian, Weiss Arthur, Kuriyan John, Structural Basis for the Inhibition of Tyrosine Kinase Activity of ZAP-70, 10.1016/j.cell.2007.03.039
  26. Dusa Alexandra, Staerk Judith, Elliott Joanne, Pecquet Christian, Poirel Hélène A., Johnston James A., Constantinescu Stefan N., Substitution of Pseudokinase Domain Residue Val-617 by Large Non-polar Amino Acids Causes Activation of JAK2, 10.1074/jbc.m709302200
  27. Kohlhuber F, Rogers N C, Watling D, Feng J, Guschin D, Briscoe J, Witthuhn B A, Kotenko S V, Pestka S, Stark G R, Ihle J N, Kerr I M, A JAK1/JAK2 chimera can sustain alpha and gamma interferon responses., 10.1128/mcb.17.2.695
  28. Scott Linda M., Tong Wei, Levine Ross L., Scott Mike A., Beer Philip A., Stratton Michael R., Futreal P. Andrew, Erber Wendy N., McMullin Mary Frances, Harrison Claire N., Warren Alan J., Gilliland D. Gary, Lodish Harvey F., Green Anthony R., JAK2Exon 12 Mutations in Polycythemia Vera and Idiopathic Erythrocytosis, 10.1056/nejmoa065202
  29. Mercher T., Wernig G., Moore S. A., Levine R. L., Gu T.-L., Frohling S., Cullen D., Polakiewicz R. D., Bernard O. A., Boggon T. J., Lee B. H., Gilliland D. G., JAK2T875N is a novel activating mutation that results in myeloproliferative disease with features of megakaryoblastic leukemia in a murine bone marrow transplantation model, 10.1182/blood-2006-04-014712
  30. Mullighan C. G., Zhang J., Harvey R. C., Collins-Underwood J. R., Schulman B. A., Phillips L. A., Tasian S. K., Loh M. L., Su X., Liu W., Devidas M., Atlas S. R., Chen I-M., Clifford R. J., Gerhard D. S., Carroll W. L., Reaman G. H., Smith M., Downing J. R., Hunger S. P., Willman C. L., JAK mutations in high-risk childhood acute lymphoblastic leukemia, 10.1073/pnas.0811761106
  31. Staerk Judith, Kallin Anders, Demoulin Jean-Baptiste, Vainchenker William, Constantinescu Stefan N., JAK1 and Tyk2 Activation by the Homologous Polycythemia Vera JAK2 V617F Mutation : CROSS-TALK WITH IGF1 RECEPTOR, 10.1074/jbc.c500358200
  32. Jeong E. G., Kim M. S., Nam H. K., Min C. K., Lee S., Chung Y. J., Yoo N. J., Lee S. H., Somatic Mutations of JAK1 and JAK3 in Acute Leukemias and Solid Cancers, 10.1158/1078-0432.ccr-07-4839
  33. Flex Elisabetta, Petrangeli Valentina, Stella Lorenzo, Chiaretti Sabina, Hornakova Tekla, Knoops Laurent, Ariola Cristina, Fodale Valentina, Clappier Emmanuelle, Paoloni Francesca, Martinelli Simone, Fragale Alessandra, Sanchez Massimo, Tavolaro Simona, Messina Monica, Cazzaniga Giovanni, Camera Andrea, Pizzolo Giovanni, Tornesello Assunta, Vignetti Marco, Battistini Angela, Cavé Hélène, Gelb Bruce D., Renauld Jean-Christophe, Biondi Andrea, Constantinescu Stefan N., Foà Robin, Tartaglia Marco, Somatically acquiredJAK1mutations in adult acute lymphoblastic leukemia, 10.1084/jem.20072182
  34. Seubert Nadine, Royer Yohan, Staerk Judith, Kubatzky Katharina F, Moucadel Virginie, Krishnakumar Shyam, Smith Steven O, Constantinescu Stefan N, Active and Inactive Orientations of the Transmembrane and Cytosolic Domains of the Erythropoietin Receptor Dimer, 10.1016/s1097-2765(03)00389-7
  35. Kubatzky Katharina F., Liu Wei, Goldgraben Kerri, Simmerling Carlos, Smith Steven O., Constantinescu Stefan N., Structural Requirements of the Extracellular to Transmembrane Domain Junction for Erythropoietin Receptor Function, 10.1074/jbc.m411251200
  36. Lu X., Levine R., Tong W., Wernig G., Pikman Y., Zarnegar S., Gilliland D. G., Lodish H., Expression of a homodimeric type I cytokine receptor is required for JAK2V617F-mediated transformation, 10.1073/pnas.0509714102
  37. Lu Xiaohui, Huang Lily Jun-Shen, Lodish Harvey F., Dimerization by a Cytokine Receptor Is Necessary for Constitutive Activation of JAK2V617F, 10.1074/jbc.m707125200
  38. Lee Tai-Sung, Ma Wanlong, Zhang Xi, Giles Francis, Kantarjian Hagop, Albitar Maher, Mechanisms of constitutive activation of Janus kinase 2-V617F revealed at the atomic level through molecular dynamics simulations, 10.1002/cncr.24183
  39. Remy I., Wilson I. A., Michnick S. W., Erythropoietin Receptor Activation by a Ligand-Induced Conformation Change, 10.1126/science.283.5404.990
  40. Mukherjee Konark, Sharma Manu, Urlaub Henning, Bourenkov Gleb P., Jahn Reinhard, Südhof Thomas C., Wahl Markus C., CASK Functions as a Mg2+-Independent Neurexin Kinase, 10.1016/j.cell.2008.02.036
  41. Zeqiraj Elton, Filippi Beatrice Maria, Goldie Simon, Navratilova Iva, Boudeau Jérôme, Deak Maria, Alessi Dario R., van Aalten Daan M. F., ATP and MO25α Regulate the Conformational State of the STRADα Pseudokinase and Activation of the LKB1 Tumour Suppressor, 10.1371/journal.pbio.1000126
  42. Wernig Gerlinde, Kharas Michael G., Okabe Rachel, Moore Sandra A., Leeman Dena S., Cullen Dana E., Gozo Maricel, McDowell Elizabeth P., Levine Ross L., Doukas John, Mak Chi Ching, Noronha Glenn, Martin Michael, Ko Yon D., Lee Benjamin H., Soll Richard M., Tefferi Ayalew, Hood John D., Gilliland D. Gary, Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera, 10.1016/j.ccr.2008.02.009
  43. Mesa Ruben A, Tefferi Ayalew, Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis, 10.1517/14728210903066809
  44. Müller Mathias, Briscoe James, Laxton Carl, Guschin Dmitry, Ziemiecki Andrew, Silvennoinen Olli, Harpur Ailsa G., Barbieri Giovanna, Witthuhn Bruce A., Schindler Chris, Pellegrini Sandra, Wilks Andrew F., Ihle James N., Stark George R., Kerr lan M., The protein tyrosine kinase JAK1 complements defects in interferon-α/β and -γ signal transduction, 10.1038/366129a0
  45. Dumoutier L., Van Roost E., Colau D., Renauld J.-C., Human interleukin-10-related T cell-derived inducible factor: Molecular cloning and functional characterization as an hepatocyte-stimulating factor, 10.1073/pnas.170291697
  46. Pettersen Eric F., Goddard Thomas D., Huang Conrad C., Couch Gregory S., Greenblatt Daniel M., Meng Elaine C., Ferrin Thomas E., UCSF Chimera?A visualization system for exploratory research and analysis, 10.1002/jcc.20084