JAK2 the future: Therapeutic strategies for JAK-dependent malignancies

Trends in Pharmacological Sciences

Volumn 33, Issue 11, 2012, Pages 574-582

  Lafave, Lindsay M ^a,b   Levine, Ross L ^a,b  

^a MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

^b Gerstner Sloan Kettering Graduate School of Biomedical Sciences   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (2,4 DIHYDROXY 5 ISOPROPYLPHENYL) 4 (4 MORPHOLINOMETHYLPHENYL) 3 ISOXAZOLECARBOXYLIC ACID ETHYLAMIDE; 5 CHLORO N2 [1 (5 FLUORO 2 PYRIMIDINYL)ETHYL] N4 (5 METHYL 1H PYRAZOL 3 YL) 2,4 PYRIMIDINEDIAMINE; BMS 911543; GANDOTINIB; GIVINOSTAT; HEAT SHOCK PROTEIN 90 INHIBITOR; HISTONE DEACETYLASE INHIBITOR; JANUS KINASE 2; JANUS KINASE 2 INHIBITOR; LESTAURTINIB; MOMELOTINIB; N BENZYL 2 CYANO 3 (3,4 DIHYDROXYPHENYL)ACRYLAMIDE; N TERT BUTYL 3 [5 METHYL 2 [4 (4 METHYL 1 PIPERAZINYL)PHENYLAMINO] 4 PYRIMIDINYLAMINO]BENZENESULFONAMIDE; N TERT BUTYL 3 [5 METHYL 2 [4 [2 (1 PYRROLIDINYL)ETHOXY]PHENYLAMINO] 4 PYRIMIDINYLAMINO]BENZENESULFONAMIDE; NS 018; PACRITINIB; PANOBINOSTAT; PLACEBO; RUXOLITINIB; STAT PROTEIN; TANESPIMYCIN; TOFACITINIB; UNCLASSIFIED DRUG;

ACUTE LYMPHOBLASTIC LEUKEMIA; ANEMIA; APOPTOSIS; DIARRHEA; DIZZINESS; DRUG EFFICACY; DRUG MECHANISM; ENZYME ACTIVITY; ENZYME PHOSPHORYLATION; EPIGENETICS; GASTROINTESTINAL SYMPTOM; HUMAN; LEUKOCYTOSIS; MYELOPROLIFERATIVE NEOPLASM; NAUSEA; NAUSEA AND VOMITING; NONHUMAN; PERIPHERAL NEUROPATHY; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; REVIEW; SIDE EFFECT; SIGNAL TRANSDUCTION; THROMBOCYTOPENIA; THROMBOCYTOSIS; THROMBOSIS;

ANIMALS; HUMANS; JANUS KINASES; MYELOPROLIFERATIVE DISORDERS; PROTEIN KINASE INHIBITORS; SIGNAL TRANSDUCTION;

EID: 84867851649     PISSN: 01656147     EISSN: 18733735     Source Type: Journal    
DOI: 10.1016/j.tips.2012.08.005     Document Type: Review

References (70)

1. R.L. Levine, and D.G. Gilliland Myeloproliferative disorders Blood 112 2008 2190 2198
2. E. Vakil, and A. Tefferi BCR-ABL1-negative myeloproliferative neoplasms: a review of molecular biology, diagnosis, and treatment Clin. Lymphoma Myeloma Leuk. 11 Suppl. 1 2011 S37 S45
3. J. Gora-Tybor Emerging therapies in chronic myeloid leukemia Curr. Cancer Drug Targets 12 2012 458 470
4. E. Weisberg Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia Nat. Rev. Cancer 7 2007 345 356
5. R.L. Levine Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis Cancer Cell 7 2005 387 397
6. E.J. Baxter Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders Lancet 365 2005 1054 1061
7. R. Kralovics A gain-of-function mutation of JAK2 in myeloproliferative disorders N. Engl. J. Med. 352 2005 1779 1790
8. C. James A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera Nature 434 2005 1144 1148
9. L.M. Scott JAK2 exon 12 mutations in polycythemia vera and idiopathic erythrocytosis N. Engl. J. Med. 356 2007 459 468
10. D. Pietra Somatic mutations of JAK2 exon 12 in patients with JAK2 (V617F)-negative myeloproliferative disorders Blood 111 2008 1686 1689
11. Y. Pikman MPLW515L is a novel somatic activating mutation in myelofibrosis with myeloid metaplasia PLoS Med. 3 2006 e270
12. D. Bercovich Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome Lancet 372 2008 1484 1492
13. E. Flex Somatically acquired JAK1 mutations in adult acute lymphoblastic leukemia J. Exp. Med. 205 2008 751 758
14. C. Harrison JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis N. Engl. J. Med. 366 2012 787 798
15. C.G. Mullighan Rearrangement of CRLF2 in B-progenitor- and Down syndrome-associated acute lymphoblastic leukemia Nat. Genet. 41 2009 1243 1246
16. A. Yoda Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia Proc. Natl. Acad. Sci. U.S.A. 107 2010 252 257
17. L. Hertzberg Down syndrome acute lymphoblastic leukemia, a highly heterogeneous disease in which aberrant expression of CRLF2 is associated with mutated JAK2: a report from the International BFM Study Group Blood 115 2010 1006 1017
18. C.G. Mullighan JAK mutations in high-risk childhood acute lymphoblastic leukemia Proc. Natl. Acad. Sci. U.S.A. 106 2009 9414 9418
19. C. Shochat Gain-of-function mutations in interleukin-7 receptor-alpha (IL7R) in childhood acute lymphoblastic leukemias J. Exp. Med. 208 2011 901 908
20. J. Zhang The genetic basis of early T-cell precursor acute lymphoblastic leukaemia Nature 481 2012 157 163
21. P.P. Zenatti Oncogenic IL7R gain-of-function mutations in childhood T-cell acute lymphoblastic leukemia Nat. Genet. 43 2011 932 939
22. R.C. Harvey Rearrangement of CRLF2 is associated with mutation of JAK kinases, alteration of IKZF1, Hispanic/Latino ethnicity, and a poor outcome in pediatric B-progenitor acute lymphoblastic leukemia Blood 115 2010 5312 5321
23. J. Feng Activation of Jak2 catalytic activity requires phosphorylation of Y1007 in the kinase activation loop Mol. Cell. Biol. 17 1997 2497 2501
24. P. Saharinen Regulation of the Jak2 tyrosine kinase by its pseudokinase domain Mol. Cell. Biol. 20 2000 3387 3395
25. K. Gnanasambandan The constitutive activation of Jak2-V617F is mediated by a pi stacking mechanism involving phenylalanines 595 and 617 Biochemistry 49 2010 9972 9984
26. D. Ungureanu The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling Nat. Struct. Mol. Biol. 18 2011 971 976
27. R.M. Bandaranayake Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F Nat. Struct. Mol. Biol. 9 2012 754 759
28. I.S. Lucet The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor Blood 107 2006 176 183
29. T.J. Boggon Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog Blood 106 2005 996 1002
30. M.A. Dawson JAK2 phosphorylates histone H3Y41 and excludes HP1alpha from chromatin Nature 461 2009 819 822
31. L. Rui Cooperative epigenetic modulation by cancer amplicon genes Cancer Cell 18 2010 590 605
32. A.M. Mazurkiewicz-Munoz Phosphorylation of JAK2 at serine 523: a negative regulator of JAK2 that is stimulated by growth hormone and epidermal growth factor Mol. Cell. Biol. 26 2006 4052 4062
33. S.A. Robertson Regulation of Jak2 function by phosphorylation of Tyr317 and Tyr637 during cytokine signaling Mol. Cell. Biol. 29 2009 3367 3378
34. E.P. Feener Tyrosine phosphorylation of Jak2 in the JH2 domain inhibits cytokine signaling Mol. Cell. Biol. 24 2004 4968 4978
35. L.S. Argetsinger Autophosphorylation of JAK2 on tyrosines 221 and 570 regulates its activity Mol. Cell. Biol. 24 2004 4955 4967
36. L.S. Argetsinger Tyrosines 868, 966, and 972 in the kinase domain of JAK2 are autophosphorylated and required for maximal JAK2 kinase activity Mol. Endocrinol. 24 2010 1062 1076
37. A.K. Samanta Janus kinase 2: a critical target in chronic myelogenous leukemia Cancer Res. 66 2006 6468 6472
38. Y. Liu, and N.S. Gray Rational design of inhibitors that bind to inactive kinase conformations Nat. Chem. Biol. 2 2006 358 364
39. E. Weisberg Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl Cancer Cell 7 2005 129 141
40. N.P. Shah Overriding imatinib resistance with a novel ABL kinase inhibitor Science 305 2004 399 401
41. T. O'Hare In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants Cancer Res. 65 2005 4500 4505
42. H.G. Choi A type-II kinase inhibitor capable of inhibiting the T315I 'gatekeeper' mutant of Bcr-Abl J. Med. Chem. 53 2010 5439 5448
43. E. Weisberg Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants Blood 115 2010 4206 4216
44. B.L. Harry JAK2 inhibition for the treatment of hematologic and solid malignancies Expert Opin. Investig. Drugs 21 2012 637 655
45. R. Fleischmann Placebo-controlled trial of tofacitinib monotherapy in rheumatoid arthritis N. Engl. J. Med. 367 2012 495 507
46. A. Quintas-Cardama Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms Blood 115 2010 3109 3117
47. P. Koppikar Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis Blood 115 2010 2919 2927
48. S. Verstovsek Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis N. Engl. J. Med. 363 2010 1117 1127
49. S. Verstovsek A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis N. Engl. J. Med. 366 2012 799 807
50. S.K. Tasian Aberrant STAT5 and PI3K/mTOR pathway signaling occurs in human CRLF2-rearranged B-precursor acute lymphoblastic leukemia Blood 120 2012 833 842
51. A. Pardanani Safety and efficacy of TG101348, a selective JAK2 inhibitor, in myelofibrosis J. Clin. Oncol. 29 2011 789 796
52. R. Andraos Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent Cancer Discov. 2 2012 512 523
53. M. Azam Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL Cell 112 2003 831 843
54. M.R. Burgess Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance Proc. Natl. Acad. Sci. U.S.A. 102 2005 3395 3400
55. A. Deshpande Kinase domain mutations confer resistance to novel inhibitors targeting JAK2 V617F in myeloproliferative neoplasms Leukemia 26 2012 708 715
56. O. Weigert Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition J. Exp. Med. 209 2012 259 273
57. J.W. Tyner CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms Blood 115 2010 5232 5240
58. K. Jhaveri Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers Biochim. Biophys. Acta 1823 2012 742 755
59. D.B. Solit, and G. Chiosis Development and application of Hsp90 inhibitors Drug Discov. Today 13 2008 38 43
60. L. Neckers, and K. Neckers Heat-shock protein 90 inhibitors as novel cancer chemotherapeutics - an update Expert Opin. Emerg. Drugs 10 2005 137 149
61. J. Bareng A potential role for HSP90 inhibitors in the treatment of JAK2 mutant-positive diseases as demonstrated using quantitative flow cytometry Leuk. Lymphoma 48 2007 2189 2195
62. H. He Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90 J. Med. Chem. 49 2006 381 390
63. S. Marubayashi HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans J. Clin. Invest. 120 2010 3578 3593
64. W. Fiskus Heat shock protein 90 inhibitor is synergistic with JAK2 inhibitor and overcomes resistance to JAK2-TKI in human myeloproliferative neoplasm cells Clin. Cancer Res. 17 2011 7347 7358
65. P. Koppikar Heterodimeric JAK-STAT activation as mechanism of persistence to JAK2 inhibitor therapy Nature 2012 10.1038/nature11303
66. P. Bali Inhibition of histone deacetylase 6 acetylates and disrupts the chaperone function of heat shock protein 90: a novel basis for antileukemia activity of histone deacetylase inhibitors J. Biol. Chem. 280 2005 26729 26734
67. Y. Wang Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells Blood 114 2009 5024 5033
68. W. Fiskus Molecular and biologic characterization and drug sensitivity of pan-histone deacetylase inhibitor-resistant acute myeloid leukemia cells Blood 112 2008 2896 2905
69. V617F myeloproliferative neoplasm cells Exp. Hematol. 40 2012 634 645
70. V617F positive chronic myeloproliferative neoplasms Br. J. Haematol. 150 2010 446 455