Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond (Q37833893)

24 August 2017

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title

Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond (English)

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24 August 2017

2

Hagop Kantarjian

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24 August 2017

4

Srdan Verstovsek

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24 August 2017

3

Jorge Cortes

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24 August 2017

Alfonso Quintás-Cardama

series ordinal

1

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24 August 2017

1 February 2011

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Nature Reviews Drug Discovery

24 August 2017

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24 August 2017

10

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24 August 2017

127-140

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24 August 2017

2

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https://scigraph.springernature.com/pub.10.1038/nrd3264

24 August 2017

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Jak2 deficiency defines an essential developmental checkpoint in definitive hematopoiesis

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Jak2 is essential for signaling through a variety of cytokine receptors

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Role of JAK2 in the pathogenesis and therapy of myeloproliferative disorders

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Acquired mutation of the tyrosine kinase JAK2 in human myeloproliferative disorders

21 January 2018

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A unique clonal JAK2 mutation leading to constitutive signalling causes polycythaemia vera

21 January 2018

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A gain-of-function mutation of JAK2 in myeloproliferative disorders

21 January 2018

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Activating mutation in the tyrosine kinase JAK2 in polycythemia vera, essential thrombocythemia, and myeloid metaplasia with myelofibrosis

21 January 2018

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Identification of an acquired JAK2 mutation in polycythemia vera

21 January 2018

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Expression of a homodimeric type I cytokine receptor is required for JAK2V617F-mediated transformation

21 January 2018

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Substitution of pseudokinase domain residue Val-617 by large non-polar amino acids causes activation of JAK2.

21 January 2018

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JAK2 exon 12 mutations in polycythemia vera and idiopathic erythrocytosis

21 January 2018

1 reference

Somatic mutations of JAK2 exon 12 in patients with JAK2 (V617F)-negative myeloproliferative disorders

21 January 2018

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Prevalence and clinicopathologic correlates of JAK2 exon 12 mutations in JAK2V617F-negative polycythemia vera.

21 January 2018

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JAK2 haplotype is a major risk factor for the development of myeloproliferative neoplasms

21 January 2018

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A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms

21 January 2018

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A common JAK2 haplotype confers susceptibility to myeloproliferative neoplasms.

21 January 2018

1 reference

Regulation of the Jak2 tyrosine kinase by its pseudokinase domain

21 January 2018

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The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor

21 January 2018

1 reference

Expression of Bcl-x in erythroid precursors from patients with polycythemia vera

21 January 2018

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The JAK2 V617F mutation occurs in hematopoietic stem cells in polycythemia vera and predisposes toward erythroid differentiation

21 January 2018

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Involvement of various hematopoietic-cell lineages by the JAK2V617F mutation in polycythemia vera.

21 January 2018

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Evidence that the JAK2 G1849T (V617F) mutation occurs in a lymphomyeloid progenitor in polycythemia vera and idiopathic myelofibrosis.

21 January 2018

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JAK2V617F expression in murine hematopoietic cells leads to MPD mimicking human PV with secondary myelofibrosis.

21 January 2018

1 reference

Expression of Jak2V617F causes a polycythemia vera-like disease with associated myelofibrosis in a murine bone marrow transplant model

21 January 2018

1 reference

Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F.

21 January 2018

1 reference

Ratio of mutant JAK2-V617F to wild-type Jak2 determines the MPD phenotypes in transgenic mice

21 January 2018

1 reference

Imatinib mesylate therapy for polycythemia vera: final result of a phase II study initiated in 2001

21 January 2018

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Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis

21 January 2018

1 reference

Response criteria for essential thrombocythemia and polycythemia vera: result of a European LeukemiaNet consensus conference.

21 January 2018

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Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.

21 January 2018

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JAK2 inhibitor therapy in myeloproliferative disorders: rationale, preclinical studies and ongoing clinical trials

21 January 2018

1 reference

TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations

21 January 2018

1 reference

Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders

21 January 2018

1 reference

A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy

21 January 2018

1 reference

Single-agent CEP-701, a novel FLT3 inhibitor, shows biologic and clinical activity in patients with relapsed or refractory acute myeloid leukemia

21 January 2018

1 reference

Phase 2 study of CEP-701, an orally available JAK2 inhibitor, in patients with primary or post-polycythemia vera/essential thrombocythemia myelofibrosis

21 January 2018

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The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors

21 January 2018

1 reference

CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients

21 January 2018

1 reference

CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms

21 January 2018

1 reference

Prevention of Organ Allograft Rejection by a Specific Janus Kinase 3 Inhibitor

21 January 2018

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Dissecting specificity in the Janus kinases: the structures of JAK-specific inhibitors complexed to the JAK1 and JAK2 protein tyrosine kinase domains

21 January 2018

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Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550)

21 January 2018

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Novel immunosuppression: small molecules and biologics

21 January 2018

1 reference

The JAK kinase inhibitor CP-690,550 suppresses the growth of human polycythemia vera cells carrying the JAK2V617F mutation

21 January 2018

1 reference

A TEL-JAK2 fusion protein with constitutive kinase activity in human leukemia

21 January 2018

1 reference

Transformation of hematopoietic cell lines to growth-factor independence and induction of a fatal myelo- and lymphoproliferative disease in mice by retrovirally transduced TEL/JAK2 fusion genes

21 January 2018

1 reference

JAK mutations in high-risk childhood acute lymphoblastic leukemia

21 January 2018

1 reference

Identification of somatic JAK1 mutations in patients with acute myeloid leukemia

21 January 2018

1 reference

Activating alleles of JAK3 in acute megakaryoblastic leukemia

21 January 2018

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The JAK2 V617F mutation in de novo acute myelogenous leukemias.

21 January 2018

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JAK2 mutation 1849G>T is rare in acute leukemias but can be found in CMML, Philadelphia chromosome-negative CML, and megakaryocytic leukemia

21 January 2018

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Arf gene loss enhances oncogenicity and limits imatinib response in mouse models of Bcr-Abl-induced acute lymphoblastic leukemia

21 January 2018

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Jak2 inhibition deactivates Lyn kinase through the SET-PP2A-SHP1 pathway, causing apoptosis in drug-resistant cells from chronic myelogenous leukemia patients

21 January 2018

1 reference

Cytokines and immunodeficiency diseases

21 January 2018

1 reference

Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes

21 January 2018

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A new modality for immunosuppression: targeting the JAK/STAT pathway

21 January 2018

1 reference

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

21 January 2018

1 reference

The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo

21 January 2018

1 reference

Improved pain, physical functioning and health status in patients with rheumatoid arthritis treated with CP-690,550, an orally active Janus kinase (JAK) inhibitor: results from a randomised, double-blind, placebo-controlled trial.

21 January 2018

1 reference

Progressive multifocal leukoencephalopathy following rituximab treatment in a patient with rheumatoid arthritis.

21 January 2018

1 reference

Jak3, severe combined immunodeficiency, and a new class of immunosuppressive drugs.

21 January 2018

1 reference

Monitoring of the immunomodulatory effect of CP-690,550 by analysis of the JAK/STAT pathway in kidney transplant patients

21 January 2018

1 reference

Calcineurin-inhibitor-free immunosuppression based on the JAK inhibitor CP-690,550: a pilot study in de novo kidney allograft recipients

21 January 2018

1 reference

The effect of the JAK inhibitor CP-690,550 on peripheral immune parameters in stable kidney allograft patients

21 January 2018

1 reference

Phase 1 dose-escalation study of CP-690 550 in stable renal allograft recipients: preliminary findings of safety, tolerability, effects on lymphocyte subsets and pharmacokinetics

21 January 2018

1 reference

Combined use of the JAK3 inhibitor CP-690,550 with mycophenolate mofetil to prevent kidney allograft rejection in nonhuman primates

21 January 2018

1 reference

Novel mutations and their functional and clinical relevance in myeloproliferative neoplasms: JAK2, MPL, TET2, ASXL1, CBL, IDH and IKZF1

21 January 2018

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JAK2 phosphorylates histone H3Y41 and excludes HP1alpha from chromatin

21 January 2018

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Cotreatment with panobinostat and JAK2 inhibitor TG101209 attenuates JAK2V617F levels and signaling and exerts synergistic cytotoxic effects against human myeloproliferative neoplastic cells.

21 January 2018

1 reference

HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans

21 January 2018

1 reference

The haematocrit and platelet target in polycythemia vera

21 January 2018

1 reference

Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia

21 January 2018

1 reference

Advances in the therapy of chronic idiopathic myelofibrosis

21 January 2018

1 reference

How I treat symptomatic splenomegaly in patients with myelofibrosis

21 January 2018

1 reference

Lenalidomide plus prednisone results in durable clinical, histopathologic, and molecular responses in patients with myelofibrosis

21 January 2018

1 reference

Lenalidomide and prednisone for myelofibrosis: Eastern Cooperative Oncology Group (ECOG) phase 2 trial E4903.

21 January 2018

1 reference

Allogeneic hemopoietic SCT for patients with primary myelofibrosis: a predictive transplant score based on transfusion requirement, spleen size and donor type

21 January 2018

1 reference

The role of allogeneic SCT in primary myelofibrosis: a British Society for Blood and Marrow Transplantation study.

21 January 2018

1 reference

Allogeneic stem cell transplantation after reduced-intensity conditioning in patients with myelofibrosis: a prospective, multicenter study of the Chronic Leukemia Working Party of the European Group for Blood and Marrow Transplantation

21 January 2018

1 reference

Choosing between stem cell therapy and drugs in myelofibrosis

21 January 2018

1 reference

Disruption of the Jak1 gene demonstrates obligatory and nonredundant roles of the Jaks in cytokine-induced biologic responses

21 January 2018

1 reference

Partial impairment of cytokine responses in Tyk2-deficient mice

21 January 2018

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Tyk2 plays a restricted role in IFN alpha signaling, although it is required for IL-12-mediated T cell function

21 January 2018

1 reference

A genome-wide association study identifies IL23R as an inflammatory bowel disease gene

21 January 2018

1 reference

Association scan of 14,500 nonsynonymous SNPs in four diseases identifies autoimmunity variants

21 January 2018

1 reference

MPLW515L is a novel somatic activating mutation in myelofibrosis with myeloid metaplasia

21 January 2018

1 reference

MPL515 mutations in myeloproliferative and other myeloid disorders: a study of 1182 patients

21 January 2018

1 reference

Characteristics and clinical correlates of MPL 515W>L/K mutation in essential thrombocythemia

21 January 2018

1 reference

MPL mutations in myeloproliferative disorders: analysis of the PT-1 cohort.

21 January 2018

1 reference

Lnk constrains myeloproliferative diseases in mice

21 January 2018

1 reference

Novel mutations in the inhibitory adaptor protein LNK drive JAK-STAT signaling in patients with myeloproliferative neoplasms.

21 January 2018

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LNK mutations in JAK2 mutation-negative erythrocytosis.

21 January 2018

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Leukemic blasts in transformed JAK2-V617F-positive myeloproliferative disorders are frequently negative for the JAK2-V617F mutation.

21 January 2018

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Acquisition of the V617F mutation of JAK2 is a late genetic event in a subset of patients with myeloproliferative disorders.

21 January 2018

1 reference

Mutation in TET2 in myeloid cancers

21 January 2018

1 reference

Conversion of 5-methylcytosine to 5-hydroxymethylcytosine in mammalian DNA by MLL partner TET1

21 January 2018

1 reference

Role of Tet proteins in 5mC to 5hmC conversion, ES-cell self-renewal and inner cell mass specification

21 January 2018

1 reference

TET2 mutations and their clinical correlates in polycythemia vera, essential thrombocythemia and myelofibrosis

21 January 2018

1 reference

Mutations of ASXL1 gene in myeloproliferative neoplasms.

21 January 2018

1 reference

Genetic analysis of transforming events that convert chronic myeloproliferative neoplasms to leukemias

21 January 2018

1 reference

Frequent CBL mutations associated with 11q acquired uniparental disomy in myeloproliferative neoplasms.

21 January 2018

1 reference

Taxing sugar-sweetened beverages

21 January 2018

1 reference

IDH1 and IDH2 mutation analysis in chronic- and blast-phase myeloproliferative neoplasms.

21 January 2018

1 reference

IDH1 and IDH2 mutation studies in 1473 patients with chronic-, fibrotic- or blast-phase essential thrombocythemia, polycythemia vera or myelofibrosis.

21 January 2018

1 reference

Deletions of the transcription factor Ikaros in myeloproliferative neoplasms.

21 January 2018

1 reference

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

21 January 2018

1 reference

Characterization of murine JAK2V617F-positive myeloproliferative disease

21 January 2018

1 reference

Transgenic expression of JAK2V617F causes myeloproliferative disorders in mice

21 January 2018

1 reference

Physiological Jak2V617F expression causes a lethal myeloproliferative neoplasm with differential effects on hematopoietic stem and progenitor cells

21 January 2018

1 reference

Conditional expression of heterozygous or homozygous Jak2V617F from its endogenous promoter induces a polycythemia vera-like disease

21 January 2018

1 reference

A role for JAK2 mutations in myeloproliferative diseases

21 January 2018

1 reference

STAT3 is constitutively active in some patients with Polycythemia rubra vera

21 January 2018

1 reference

Spontaneous STAT5 activation induces growth factor independence in idiopathic myelofibrosis: possible relationship with FKBP51 overexpression.

21 January 2018

1 reference

Miscreant myeloproliferative disorder stem cells

21 January 2018

1 reference

Aberrant signal transduction pathways in myeloproliferative neoplasms

21 January 2018

1 reference

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

21 January 2018

1 reference

Multiple signaling pathways are involved in erythropoietin-independent differentiation of erythroid progenitors in polycythemia vera.

21 January 2018

1 reference

JAK signaling globally counteracts heterochromatic gene silencing

21 January 2018

1 reference

Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells and improvements in measures of disease severity

21 January 2018

1 reference

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805

21 January 2018

1 reference

JAK2 Mutations are present in all cases of polycythemia vera

21 January 2018

1 reference

A dynamic prognostic model to predict survival in primary myelofibrosis: a study by the IWG-MRT (International Working Group for Myeloproliferative Neoplasms Research and Treatment).

21 January 2018

1 reference

Clonal analysis of haemopoietic cells in essential thrombocythaemia

31 March 2020

1 reference

Clonality in chronic myeloproliferative disorders defined by X-chromosome linked probes: demonstration of heterogeneity in lineage involvement

31 March 2020

1 reference

Impaired expression of the thrombopoietin receptor by platelets from patients with polycythemia vera

31 March 2020

1 reference

The JAK2-V617F mutation is frequently present at diagnosis in patients with essential thrombocythemia and polycythemia vera

31 March 2020

1 reference

Phase I trial of orally administered CEP-701, a novel neurotrophin receptor-linked tyrosine kinase inhibitor

31 March 2020

1 reference

Clinical profile of homozygous JAK2 617V>F mutation in patients with polycythemia vera or essential thrombocythemia

31 March 2020

1 reference

Hydroxyurea for patients with essential thrombocythemia and a high risk of thrombosis

31 March 2020

1 reference

New prognostic scoring system for primary myelofibrosis based on a study of the International Working Group for Myelofibrosis Research and Treatment

31 March 2020

1 reference

Defective lymphoid development in mice lacking Jak3

31 March 2020

1 reference

Evidence for MPL W515L/K mutations in hematopoietic stem cells in primitive myelofibrosis

31 March 2020

1 reference

The JAK2 617V>F mutation triggers erythropoietin hypersensitivity and terminal erythroid amplification in primary cells from patients with polycythemia vera

31 March 2020

1 reference

Somatic mutations of IDH1 and IDH2 in the leukemic transformation of myeloproliferative neoplasms

31 March 2020

1 reference

Myeloproliferative disorders

31 March 2020

1 reference

Molecular and clinical features of the myeloproliferative neoplasm associated with JAK2 exon 12 mutations.

31 March 2020

1 reference

Letter: Bone-marrow responses in polycythemia vera.

31 March 2020

1 reference

12 December 2020

Fusion of the ets transcription factor TEL to Jak2 results in constitutive Jak-Stat signaling

1 reference

12 December 2020

Treatment of polycythemia vera: use of 32P alone or in combination with maintenance therapy using hydroxyurea in 461 patients greater than 65 years of age. The French Polycythemia Study Group

1 reference

12 December 2020

Fusion of TEL, the ETS-variant gene 6 (ETV6), to the receptor-associated kinase JAK2 as a result of t(9;12) in a lymphoid and t(9;15;12) in a myeloid leukemia

1 reference

12 December 2020

The Jak-Stat pathway in normal and perturbed hematopoiesis

1 reference

12 December 2020

Practice guidelines for the therapy of essential thrombocythemia. A statement from the Italian Society of Hematology, the Italian Society of Experimental Hematology and the Italian Group for Bone Marrow Transplantation.

1 reference

12 December 2020

Identifiers

DOI

10.1038/NRD3264

1 reference

24 August 2017

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PubMed ID

21283107