-
1
-
-
0025117392
-
Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome
-
Daley, G. Q., Van Etten, R. A., Baltimore, D. Induction of chronic myelogenous leukemia in mice by the P210bcr/abl gene of the Philadelphia chromosome. Science 247, 824-830 (1990).
-
(1990)
Science
, vol.247
, pp. 824-830
-
-
Daley, G.Q.1
Van Etten, R.A.2
Baltimore, D.3
-
2
-
-
70350450778
-
Perspectives on the development of imatinib and the future of cancer research
-
Druker, B. J. Perspectives on the development of imatinib and the future of cancer research. Nat Med 15, 1149-1152 (2009).
-
(2009)
Nat Med
, vol.15
, pp. 1149-1152
-
-
Druker, B.J.1
-
3
-
-
0029947186
-
Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells
-
Druker, B. J. et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 2, 561-566 (1996).
-
(1996)
Nat Med
, vol.2
, pp. 561-566
-
-
Druker, B.J.1
-
4
-
-
9244222261
-
Targeted cancer therapy
-
Sawyers, C. Targeted cancer therapy. Nature 432, 294-297 (2004).
-
(2004)
Nature
, vol.432
, pp. 294-297
-
-
Sawyers, C.1
-
5
-
-
20244369569
-
Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis
-
Levine, R. L. et al. Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis. Cancer Cell 7, 387-397 (2005).
-
(2005)
Cancer Cell
, vol.7
, pp. 387-397
-
-
Levine, R.L.1
-
6
-
-
20144363192
-
Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders
-
Baxter, E. J. et al. Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders. Lancet 365, 1054-1061 (2005).
-
(2005)
Lancet
, vol.365
, pp. 1054-1061
-
-
Baxter, E.J.1
-
7
-
-
17644424955
-
A gain-of-function mutation of JAK2 in myeloproliferative disorders
-
Kralovics, R. et al. A gain-of-function mutation of JAK2 in myeloproliferative disorders. N Engl J Med 352, 1779-1790 (2005).
-
(2005)
N Engl J Med
, vol.352
, pp. 1779-1790
-
-
Kralovics, R.1
-
8
-
-
17844383458
-
A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera
-
James, C. et al. A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera. Nature 434, 1144-1148 (2005).
-
(2005)
Nature
, vol.434
, pp. 1144-1148
-
-
James, C.1
-
9
-
-
33846216449
-
Jak2: Normal function and role in hematopoietic disorders
-
Ihle, J. N., Gilliland, D. G. Jak2: normal function and role in hematopoietic disorders. Curr Opin Genet Dev 17, 8-14 (2007).
-
(2007)
Curr Opin Genet Dev
, vol.17
, pp. 8-14
-
-
Ihle, J.N.1
Gilliland, D.G.2
-
10
-
-
84865118132
-
Genetic alterations activating kinase and cytokine receptor signaling in high-risk acute lymphoblastic leukemia
-
Roberts, K. G. et al. Genetic alterations activating kinase and cytokine receptor signaling in high-risk acute lymphoblastic leukemia. Cancer Cell 22, 153-166 (2012).
-
(2012)
Cancer Cell
, vol.22
, pp. 153-166
-
-
Roberts, K.G.1
-
11
-
-
84867851649
-
JAK2 the future: Therapeutic strategies for JAK-dependent malignancies
-
LaFave, L. M., Levine, R. L. JAK2 the future: therapeutic strategies for JAK-dependent malignancies. Trends in pharmacological sciences 33, 574-582 (2012).
-
(2012)
Trends in Pharmacological Sciences
, vol.33
, pp. 574-582
-
-
LaFave, L.M.1
Levine, R.L.2
-
12
-
-
77951759127
-
Conditional expression of heterozygous or homozygous Jak2V617F from its endogenous promoter induces a polycythemia vera-like disease
-
Akada, H. et al. Conditional expression of heterozygous or homozygous Jak2V617F from its endogenous promoter induces a polycythemia vera-like disease. Blood 115, 3589-3597 (2010).
-
(2010)
Blood
, vol.115
, pp. 3589-3597
-
-
Akada, H.1
-
13
-
-
77953274727
-
Physiological Jak2V617F expression causes a lethal myeloproliferative neoplasm with differential effects on hematopoietic stem and progenitor cells
-
Mullally, A. et al. Physiological Jak2V617F expression causes a lethal myeloproliferative neoplasm with differential effects on hematopoietic stem and progenitor cells. Cancer Cell 17, 584-596 (2010).
-
(2010)
Cancer Cell
, vol.17
, pp. 584-596
-
-
Mullally, A.1
-
14
-
-
34447642422
-
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F
-
Zaleskas, V. M. et al. Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. PLoS One 1, e18 (2006).
-
(2006)
PLoS One
, vol.1
, pp. e18
-
-
Zaleskas, V.M.1
-
15
-
-
77950684805
-
Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: Therapeutic implications for the treatment of myeloproliferative neoplasms
-
Quintas-Cardama, A. et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115, 3109-3117 (2010).
-
(2010)
Blood
, vol.115
, pp. 3109-3117
-
-
Quintas-Cardama, A.1
-
16
-
-
41249099841
-
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera
-
Wernig, G. et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell 13, 311-320 (2008).
-
(2008)
Cancer Cell
, vol.13
, pp. 311-320
-
-
Wernig, G.1
-
17
-
-
77954680141
-
CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms
-
Tyner, J. W. et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 115, 5232-5240 (2010).
-
(2010)
Blood
, vol.115
, pp. 5232-5240
-
-
Tyner, J.W.1
-
18
-
-
84858855487
-
JAK inhibitors for myeloproliferative neoplasms: Clarifying facts from myths
-
Tefferi, A. JAK inhibitors for myeloproliferative neoplasms: clarifying facts from myths. Blood 119, 2721-2730 (2012).
-
(2012)
Blood
, vol.119
, pp. 2721-2730
-
-
Tefferi, A.1
-
19
-
-
84861216420
-
Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia
-
Eghtedar, A. et al. Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia. Blood 119, 4614-4618 (2012).
-
(2012)
Blood
, vol.119
, pp. 4614-4618
-
-
Eghtedar, A.1
-
20
-
-
77956696835
-
Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis
-
Verstovsek, S. et al. Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis. N Engl J Med 363, 1117-1127 (2010).
-
(2010)
N Engl J Med
, vol.363
, pp. 1117-1127
-
-
Verstovsek, S.1
-
21
-
-
84865192181
-
Long-term outcomes of 107 patients with myelofibrosis receiving JAK1/JAK2 inhibitor ruxolitinib: Survival advantage in comparison to matched historical controls
-
Verstovsek, S. et al. Long-term outcomes of 107 patients with myelofibrosis receiving JAK1/JAK2 inhibitor ruxolitinib: survival advantage in comparison to matched historical controls. Blood 120, 1202-1209 (2012).
-
(2012)
Blood
, vol.120
, pp. 1202-1209
-
-
Verstovsek, S.1
-
22
-
-
84924061466
-
Oncogene addiction: Pathways of therapeutic response, resistance, and road maps toward a cure
-
Pagliarini, R., Shao, W., Sellers, W. R. Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure. EMBO reports (2015).
-
(2015)
EMBO Reports
-
-
Pagliarini, R.1
Shao, W.2
Sellers, W.R.3
-
23
-
-
44849093562
-
Oncogene addiction
-
discussion 3080
-
Weinstein, I. B., Joe, A. Oncogene addiction. Cancer Res 68, 3077-3080; discussion 3080 (2008).
-
(2008)
Cancer Res
, vol.68
, pp. 3077-3080
-
-
Weinstein, I.B.1
Joe, A.2
-
24
-
-
84916201113
-
Therapy for myeloproliferative neoplasms: When which agent, and how
-
Geyer, H. L., Mesa, R. A. Therapy for myeloproliferative neoplasms: when, which agent, and how? Blood 124, 3529-3537 (2014).
-
(2014)
Blood
, vol.124
, pp. 3529-3537
-
-
Geyer, H.L.1
Mesa, R.A.2
-
25
-
-
30144436273
-
The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor
-
Lucet, I. S. et al. The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor. Blood 107, 176-183 (2006).
-
(2006)
Blood
, vol.107
, pp. 176-183
-
-
Lucet, I.S.1
-
26
-
-
84864668290
-
Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F
-
Bandaranayake, R. M. et al. Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F. Nat Struct Mol Biol 19, 754-759 (2012).
-
(2012)
Nat Struct Mol Biol
, vol.19
, pp. 754-759
-
-
Bandaranayake, R.M.1
-
27
-
-
32144432437
-
The SWISS-MODEL workspace: A web-based environment for protein structure homology modelling
-
Arnold, K., Bordoli, L., Kopp, J., Schwede, T. The SWISS-MODEL workspace: a web-based environment for protein structure homology modelling. Bioinformatics 22, 195-201 (2006).
-
(2006)
Bioinformatics
, vol.22
, pp. 195-201
-
-
Arnold, K.1
Bordoli, L.2
Kopp, J.3
Schwede, T.4
-
28
-
-
0037459344
-
Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL
-
Azam, M., Latek, R. R., Daley, G. Q. Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL. Cell 112, 831-843 (2003).
-
(2003)
Cell
, vol.112
, pp. 831-843
-
-
Azam, M.1
Latek, R.R.2
Daley, G.Q.3
-
29
-
-
0001686739
-
Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia
-
Shah, N. P. et al. Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2, 117-125 (2002).
-
(2002)
Cancer Cell
, vol.2
, pp. 117-125
-
-
Shah, N.P.1
-
30
-
-
40749093314
-
Jak2 FERM domain interaction with the erythropoietin receptor regulates Jak2 kinase activity
-
Funakoshi-Tago, M., Pelletier, S., Moritake, H., Parganas, E., Ihle, J. N. Jak2 FERM domain interaction with the erythropoietin receptor regulates Jak2 kinase activity. Mol Cell Biol 28, 1792-1801 (2008).
-
(2008)
Mol Cell Biol
, vol.28
, pp. 1792-1801
-
-
Funakoshi-Tago, M.1
Pelletier, S.2
Moritake, H.3
Parganas, E.4
Ihle, J.N.5
-
31
-
-
13844317894
-
EGFR mutation and resistance of non-small-cell lung cancer to gefitinib
-
Kobayashi, S. et al. EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med 352, 786-792 (2005).
-
(2005)
N Engl J Med
, vol.352
, pp. 786-792
-
-
Kobayashi, S.1
-
32
-
-
53549104402
-
Activation of tyrosine kinases by mutation of the gatekeeper threonine
-
Azam, M., Seeliger, M. A., Gray, N. S., Kuriyan, J., Daley, G. Q. Activation of tyrosine kinases by mutation of the gatekeeper threonine. Nat Struct Mol Biol 15, 1109-1118 (2008).
-
(2008)
Nat Struct Mol Biol
, vol.15
, pp. 1109-1118
-
-
Azam, M.1
Seeliger, M.A.2
Gray, N.S.3
Kuriyan, J.4
Daley, G.Q.5
-
33
-
-
18244393495
-
Unexpected effects of FERM domain mutations on catalytic activity of Jak3: Structural implication for Janus kinases
-
Zhou, Y. J. et al. Unexpected effects of FERM domain mutations on catalytic activity of Jak3: structural implication for Janus kinases. Mol Cell 8, 959-969 (2001).
-
(2001)
Mol Cell
, vol.8
, pp. 959-969
-
-
Zhou, Y.J.1
-
34
-
-
80052492285
-
The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling
-
Ungureanu, D. et al. The pseudokinase domain of JAK2 is a dual-specificity protein kinase that negatively regulates cytokine signaling. Nat Struct Mol Biol 18, 971-976.
-
Nat Struct Mol Biol
, vol.18
, pp. 971-976
-
-
Ungureanu, D.1
-
35
-
-
79960029361
-
SwissDock a protein-small molecule docking web service based on EADock DSS
-
Grosdidier, A., Zoete, V., Michielin, O. SwissDock, a protein-small molecule docking web service based on EADock DSS. Nucleic Acids Res 39, W270-277 (2011).
-
(2011)
Nucleic Acids Res
, vol.39
, pp. W270-277
-
-
Grosdidier, A.1
Zoete, V.2
Michielin, O.3
-
36
-
-
33646755174
-
A Src-like inactive conformation in the abl tyrosine kinase domain
-
Levinson, N. M. et al. A Src-like inactive conformation in the abl tyrosine kinase domain. PLoS Biol 4, e144 (2006).
-
(2006)
PLoS Biol
, vol.4
, pp. e144
-
-
Levinson, N.M.1
-
37
-
-
79953308071
-
Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms
-
Jura, N. et al. Catalytic control in the EGF receptor and its connection to general kinase regulatory mechanisms. Mol Cell 42, 9-22 (2011).
-
(2011)
Mol Cell
, vol.42
, pp. 9-22
-
-
Jura, N.1
-
38
-
-
33745164854
-
Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance
-
Azam, M. et al. Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci USA 103, 9244-9249 (2006).
-
(2006)
Proc Natl Acad Sci USA
, vol.103
, pp. 9244-9249
-
-
Azam, M.1
-
39
-
-
84865735256
-
Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy
-
Koppikar, P. et al. Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy. Nature 489, 155-159 (2012).
-
(2012)
Nature
, vol.489
, pp. 155-159
-
-
Koppikar, P.1
-
40
-
-
0030954172
-
A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket
-
Tong, L. et al. A highly specific inhibitor of human p38 MAP kinase binds in the ATP pocket. Nature structural biology 4, 311-316 (1997).
-
(1997)
Nature Structural Biology
, vol.4
, pp. 311-316
-
-
Tong, L.1
-
41
-
-
79955136973
-
Analysis of Jak2 catalytic function by peptide microarrays: The role of the JH2 domain and V617F mutation
-
Sanz, A. et al. Analysis of Jak2 catalytic function by peptide microarrays: the role of the JH2 domain and V617F mutation. PLoS One 6, e18522 (2011).
-
(2011)
PLoS One
, vol.6
, pp. e18522
-
-
Sanz, A.1
-
42
-
-
84858424089
-
Converting cancer therapies into cures: Lessons from infectious diseases
-
Glickman, M. S., Sawyers, C. L. Converting cancer therapies into cures: lessons from infectious diseases. Cell 148, 1089-1098 (2012).
-
(2012)
Cell
, vol.148
, pp. 1089-1098
-
-
Glickman, M.S.1
Sawyers, C.L.2
-
43
-
-
22044442973
-
Tyrosine kinases as targets for cancer therapy
-
Krause, D. S., Van Etten, R. A. Tyrosine kinases as targets for cancer therapy. N Engl J Med 353, 172-187 (2005).
-
(2005)
N Engl J Med
, vol.353
, pp. 172-187
-
-
Krause, D.S.1
Van Etten, R.A.2
-
44
-
-
84859643082
-
Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms
-
Deshpande, A. et al. Kinase domain mutations confer resistance to novel inhibitors targeting JAK2V617F in myeloproliferative neoplasms. Leukemia 26, 708-715 (2012).
-
(2012)
Leukemia
, vol.26
, pp. 708-715
-
-
Deshpande, A.1
-
45
-
-
84865062499
-
Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor
-
Marit, M. R. et al. Random mutagenesis reveals residues of JAK2 critical in evading inhibition by a tyrosine kinase inhibitor. PLoS One 7, e43437 (2012).
-
(2012)
PLoS One
, vol.7
, pp. e43437
-
-
Marit, M.R.1
-
46
-
-
84856932936
-
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition
-
Weigert, O. et al. Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition. The Journal of experimental medicine 209, 259-273 (2012).
-
(2012)
The Journal of Experimental Medicine
, vol.209
, pp. 259-273
-
-
Weigert, O.1
-
47
-
-
52949090018
-
SOCS regulation of the JAK/STAT signalling pathway
-
Croker, B. A., Kiu, H., Nicholson, S. E. SOCS regulation of the JAK/STAT signalling pathway. Seminars in cell & developmental biology 19, 414-422 (2008).
-
(2008)
Seminars in Cell & Developmental Biology
, vol.19
, pp. 414-422
-
-
Croker, B.A.1
Kiu, H.2
Nicholson, S.E.3
-
48
-
-
13844261144
-
A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance
-
Gumireddy, K. et al. A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance. Proc Natl Acad Sci USA 102, 1992-1997 (2005).
-
(2005)
Proc Natl Acad Sci USA
, vol.102
, pp. 1992-1997
-
-
Gumireddy, K.1
-
49
-
-
84887193830
-
The JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivo
-
Heine, A. et al. The JAK-inhibitor ruxolitinib impairs dendritic cell function in vitro and in vivo. Blood 122, 1192-1202 (2013).
-
(2013)
Blood
, vol.122
, pp. 1192-1202
-
-
Heine, A.1
-
50
-
-
84879728130
-
Depletion of Jak2V617F myeloproliferative neoplasm-propagating stem cells by interferon-alpha in a murine model of polycythemia vera
-
Mullally, A. et al. Depletion of Jak2V617F myeloproliferative neoplasm-propagating stem cells by interferon-alpha in a murine model of polycythemia vera. Blood 121, 3692-3702 (2013).
-
(2013)
Blood
, vol.121
, pp. 3692-3702
-
-
Mullally, A.1
-
51
-
-
80053014000
-
The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers
-
Shi, J. G. et al. The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers. Journal of clinical pharmacology 51, 1644-1654 (2011).
-
(2011)
Journal of Clinical Pharmacology
, vol.51
, pp. 1644-1654
-
-
Shi, J.G.1
-
52
-
-
3142676436
-
Overriding imatinib resistance with a novel ABL kinase inhibitor
-
Shah, N. P. et al. Overriding imatinib resistance with a novel ABL kinase inhibitor. Science 305, 399-401 (2004).
-
(2004)
Science
, vol.305
, pp. 399-401
-
-
Shah, N.P.1
-
53
-
-
74549122017
-
AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance
-
Azam, M. et al. AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance. Chem Biol Drug Des 75, 223-227 (2010).
-
(2010)
Chem Biol Drug des
, vol.75
, pp. 223-227
-
-
Azam, M.1
-
54
-
-
70350507997
-
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance
-
O'Hare, T. et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 16, 401-412 (2009).
-
(2009)
Cancer Cell
, vol.16
, pp. 401-412
-
-
O'Hare, T.1
-
55
-
-
79953765304
-
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036
-
Chan, W. W. et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell 19, 556-568.
-
Cancer Cell
, vol.19
, pp. 556-568
-
-
Chan, W.W.1
-
56
-
-
75749146563
-
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors
-
Zhang, J. et al. Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature 463, 501-506 (2010).
-
(2010)
Nature
, vol.463
, pp. 501-506
-
-
Zhang, J.1
|