Janus kinase inhibitors for the treatment of myeloproliferative neoplasias and beyond

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

(2010) R. A. Mesa et al.   BLOOD

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

(2010) S. T. Oh et al.   BLOOD

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

(2010) J. W. Tyner et al.   BLOOD

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

(2010) H. Akada et al.   BLOOD

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

(2010) A. Quintas-Cardama et al.   BLOOD

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

(2010) W A Stewart et al.   BONE MARROW TRANSPLANTATION

Physiological Jak2V617F Expression Causes a Lethal Myeloproliferative Neoplasm with Differential Effects on Hematopoietic Stem and Progenitor Cells

(2010) Ann Mullally et al.   CANCER CELL

Genetic Analysis of Transforming Events That Convert Chronic Myeloproliferative Neoplasms to Leukemias

(2010) O. Abdel-Wahab et al.   CANCER RESEARCH

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

(2010) Sachie Marubayashi et al.   JOURNAL OF CLINICAL INVESTIGATION

Lnk constrains myeloproliferative diseases in mice

(2010) Alexey Bersenev et al.   JOURNAL OF CLINICAL INVESTIGATION

Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050

(2010) J. S. Fridman et al.   JOURNAL OF IMMUNOLOGY

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

(2010) A Tefferi et al.   LEUKEMIA

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

(2010) A Pardanani et al.   LEUKEMIA

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

(2010) A Tefferi   LEUKEMIA

Deletions of the transcription factor Ikaros in myeloproliferative neoplasms

(2010) R Jäger et al.   LEUKEMIA

Potent and Selective Inhibition of Polycythemia by the Quinoxaline JAK2 Inhibitor NVP-BSK805

(2010) F. Baffert et al.   MOLECULAR CANCER THERAPEUTICS

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

(2010) Shinsuke Ito et al.   NATURE

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

(2010) Thomas Ernst et al.   NATURE GENETICS

Somatic Mutations ofIDH1andIDH2in the Leukemic Transformation of Myeloproliferative Neoplasms

(2010) Anthony Green et al.   NEW ENGLAND JOURNAL OF MEDICINE

LNKMutations inJAK2Mutation–Negative Erythrocytosis

(2010) Terra L. Lasho et al.   NEW ENGLAND JOURNAL OF MEDICINE

Safety and Efficacy of INCB018424, a JAK1 and JAK2 Inhibitor, in Myelofibrosis

(2010) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

Calcineurin-Inhibitor-Free Immunosuppression Based on the JAK Inhibitor CP-690,550: A Pilot Study inDe NovoKidney Allograft Recipients

(2009) S. Busque et al.   AMERICAN JOURNAL OF TRANSPLANTATION

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

(2009) J H Coombs et al.   ANNALS OF THE RHEUMATIC DISEASES

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

(2009) R. M. Fleischmann   ARTHRITIS AND RHEUMATISM

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

(2009) Joel M. Kremer et al.   ARTHRITIS AND RHEUMATISM

How I treat symptomatic splenomegaly in patients with myelofibrosis

(2009) R. A. Mesa   BLOOD

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

(2009) G. Barosi et al.   BLOOD

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

(2009) N. Kroger et al.   BLOOD

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

(2009) F. P. S. Santos et al.   BLOOD

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

(2009) Y. Wang et al.   BLOOD

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

(2009) F. H. Grand et al.   BLOOD

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)

(2009) F. Passamonti et al.   BLOOD

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

(2009) A Bacigalupo et al.   BONE MARROW TRANSPLANTATION

The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors

(2009) Michael Hedvat et al.   CANCER CELL

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

(2009) P. C.C. Liu et al.   CLINICAL CANCER RESEARCH

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

(2009) Roberto H. Nussenzveig et al.   INTERNATIONAL JOURNAL OF HEMATOLOGY

Lenalidomide Plus Prednisone Results in Durable Clinical, Histopathologic, and Molecular Responses in Patients With Myelofibrosis

(2009) Alfonso Quintás-Cardama et al.   JOURNAL OF CLINICAL ONCOLOGY

Dissecting Specificity in the Janus Kinases: The Structures of JAK-Specific Inhibitors Complexed to the JAK1 and JAK2 Protein Tyrosine Kinase Domains

(2009) Neal K. Williams et al.   JOURNAL OF MOLECULAR BIOLOGY

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

(2009) A Pardanani et al.   LEUKEMIA

Mutations of ASXL1 gene in myeloproliferative neoplasms

(2009) N Carbuccia et al.   LEUKEMIA

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

(2009) A Tefferi et al.   LEUKEMIA

JAK2 phosphorylates histone H3Y41 and excludes HP1α from chromatin

(2009) Mark A. Dawson et al.   NATURE

A common JAK2 haplotype confers susceptibility to myeloproliferative neoplasms

(2009) Damla Olcaydu et al.   NATURE GENETICS

A germline JAK2 SNP is associated with predisposition to the development of JAK2V617F-positive myeloproliferative neoplasms

(2009) Outi Kilpivaara et al.   NATURE GENETICS

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

(2009) Amy V Jones et al.   NATURE GENETICS

Mutation inTET2in Myeloid Cancers

(2009) François Delhommeau et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2009) A K Samanta et al.   ONCOGENE

JAK mutations in high-risk childhood acute lymphoblastic leukemia

(2009) C. G. Mullighan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conversion of 5-Methylcytosine to 5-Hydroxymethylcytosine in Mammalian DNA by MLL Partner TET1

(2009) M. Tahiliani et al.   SCIENCE

The Effect of the JAK Inhibitor CP-690,550 on Peripheral Immune Parameters in Stable Kidney Allograft Patients

(2009) Evelien A. F. J. van Gurp et al.   TRANSPLANTATION

Monitoring of the Immunomodulatory Effect of CP-690,550 by Analysis of the JAK/STAT Pathway in Kidney Transplant Patients

(2009) Monique E. Quaedackers et al.   TRANSPLANTATION

Pathogenesis and management of essential thrombocythemia

(2009) P. A. Beer et al.   Hematology-American Society of Hematology Education Program

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

(2008) E. van Gurp et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Myeloproliferative disorders

(2008) R. L. Levine et al.   BLOOD

Transgenic expression of JAK2V617F causes myeloproliferative disorders in mice

(2008) S. Xing et al.   BLOOD

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

(2008) A. M. Vannucchi et al.   BLOOD

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

(2008) P. A. Beer et al.   BLOOD

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

(2008) F. Cervantes et al.   BLOOD

Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera

(2008) Gerlinde Wernig et al.   CANCER CELL

The JAK kinase inhibitor CP-690,550 supresses the growth of human polycythemia vera cells carrying the JAK2V617Fmutation

(2008) Taghi Manshouri et al.   CANCER SCIENCE

Substitution of Pseudokinase Domain Residue Val-617 by Large Non-polar Amino Acids Causes Activation of JAK2

(2008) Alexandra Dusa et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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)

(2008) Jian-kang Jiang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Miscreant myeloproliferative disorder stem cells

(2008) C H M Jamieson et al.   LEUKEMIA

Aberrant signal transduction pathways in myeloproliferative neoplasms

(2008) J Kota et al.   LEUKEMIA

Choosing between stem cell therapy and drugs in myelofibrosis

(2008) N Kröger et al.   LEUKEMIA

A Role for JAK2 Mutations in Myeloproliferative Diseases

(2007) Kelly J. Morgan et al.   Annual Review of Medicine

Identification of somatic JAK1 mutations in patients with acute myeloid leukemia

(2007) Z. Xiang et al.   BLOOD

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

(2007) R. Tiedt et al.   BLOOD