Emerging therapeutic paradigms to target the dysregulated Janus kinase/signal transducer and activator of transcription pathway in hematological malignancies

INCB16562, a JAK1/2 Selective Inhibitor, Is Efficacious against Multiple Myeloma Cells and Reverses the Protective Effects of Cytokine and Stromal Cell Support

(2015) Jun Li et al.   NEOPLASIA

A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenstrom macroglobulinemia

(2013) G. Yang et al.   BLOOD

Lymphoid malignancies: Another face to the Janus kinases

(2013) Linda M. Scott   BLOOD REVIEWS

Inhibition of related JAK/STAT pathways with molecular targeted drugs shows strong synergy with ruxolitinib in chronic myeloproliferative neoplasm

(2013) Santiago Barrio et al.   BRITISH JOURNAL OF HAEMATOLOGY

Molecular Pathways: JAK/STAT Pathway: Mutations, Inhibitors, and Resistance

(2013) A. Quintas-Cardama et al.   CLINICAL CANCER RESEARCH

Targeting the JAK-STAT pathway in lymphoma: a focus on pacritinib

(2013) Enrico Derenzini et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Targeting Primitive Chronic Myeloid Leukemia Cells by Effective Inhibition of a New AHI-1–BCR-ABL–JAK2 Complex

(2013) Min Chen et al.   JNCI-Journal of the National Cancer Institute

Oncogenic CSF3R Mutations in Chronic Neutrophilic Leukemia and Atypical CML

(2013) Julia E. Maxson et al.   NEW ENGLAND JOURNAL OF MEDICINE

JAKs and STATs in Immunity, Immunodeficiency, and Cancer

(2013) John J. O'Shea et al.   NEW ENGLAND JOURNAL OF MEDICINE

TYK2–STAT1–BCL2 Pathway Dependence in T-cell Acute Lymphoblastic Leukemia

(2013) Takaomi Sanda et al.   Cancer Discovery

Unraveling the genetic underpinnings of myeloproliferative neoplasms and understanding their effect on disease course and response to therapy: Proceedings from the 6th international post-ASH symposium

(2012) Omar Abdel-Wahab et al.   AMERICAN JOURNAL OF HEMATOLOGY

Combined gene expression and DNA occupancy profiling identifies potential therapeutic targets of t(8;21) AML

(2012) M.-C. Lo et al.   BLOOD

JAKing up AML1-ETO

(2012) J. D. Crispino   BLOOD

Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia

(2012) A. Eghtedar et al.   BLOOD

The thrombopoietin/MPL/Bcl-xL pathway is essential for survival and self-renewal in human preleukemia induced by AML1-ETO

(2012) F.-S. Chou et al.   BLOOD

Thrombopoietin/MPL participates in initiating and maintaining RUNX1-ETO acute myeloid leukemia via PI3K/AKT signaling

(2012) J. A. Pulikkan et al.   BLOOD

Elevated serum IL-10 levels in diffuse large B-cell lymphoma: a mechanism of aberrant JAK2 activation

(2012) M. Gupta et al.   BLOOD

MYD88 somatic mutations in MALT lymphomas

(2012) Zhi-Ming Li et al.   BRITISH JOURNAL OF HAEMATOLOGY

Genetic Alterations Activating Kinase and Cytokine Receptor Signaling in High-Risk Acute Lymphoblastic Leukemia

(2012) Kathryn G. Roberts et al.   CANCER CELL

STAT5 Is Crucial to Maintain Leukemic Stem Cells in Acute Myelogenous Leukemias Induced by MOZ-TIF2

(2012) W. F. Tam et al.   CANCER RESEARCH

The Role of JAK Pathway Dysregulation in the Pathogenesis and Treatment of Acute Myeloid Leukemia

(2012) H. J. Lee et al.   CLINICAL CANCER RESEARCH

Janus Kinase Deregulation in Leukemia and Lymphoma

(2012) Edwin Chen et al.   IMMUNITY

The JAK-STAT Pathway at Twenty

(2012) George R. Stark et al.   IMMUNITY

Janus Reveals Another Face: The Biologic Rationale for Targeting Janus Kinase 2 in Lymphoma

(2012) Ann Mullally et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I Study of a Novel Oral Janus Kinase 2 Inhibitor, SB1518, in Patients With Relapsed Lymphoma: Evidence of Clinical and Biologic Activity in Multiple Lymphoma Subtypes

(2012) Anas Younes et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting the Interleukin-6/Jak/Stat Pathway in Human Malignancies

(2012) Pasquale Sansone et al.   JOURNAL OF CLINICAL ONCOLOGY

Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors

(2012) E Weisberg et al.   LEUKEMIA

Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

(2012) Priya Koppikar et al.   NATURE

The genetic basis of early T-cell precursor acute lymphoblastic leukaemia

(2012) Jinghui Zhang et al.   NATURE

A new STATus in CML

(2012) Doriano Fabbro   Nature Chemical Biology

BCR-ABL uncouples canonical JAK2-STAT5 signaling in chronic myeloid leukemia

(2012) Oliver Hantschel et al.   Nature Chemical Biology

Challenges Facing JAK Inhibitor Therapy for Myeloproliferative Neoplasms

(2012) Ayalew Tefferi   NEW ENGLAND JOURNAL OF MEDICINE

A Double-Blind, Placebo-Controlled Trial of Ruxolitinib for Myelofibrosis

(2012) Srdan Verstovsek et al.   NEW ENGLAND JOURNAL OF MEDICINE

JAK Inhibition with Ruxolitinib versus Best Available Therapy for Myelofibrosis

(2012) Claire Harrison et al.   NEW ENGLAND JOURNAL OF MEDICINE

MYD88 L265P Somatic Mutation in Waldenström's Macroglobulinemia

(2012) Steven P. Treon et al.   NEW ENGLAND JOURNAL OF MEDICINE

JAK/STAT signaling in hematological malignancies

(2012) W Vainchenker et al.   ONCOGENE

Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing

(2012) J. G. Lohr et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Janus Kinase 3–Activating Mutations Identified in Natural Killer/T-cell Lymphoma

(2012) Ghee Chong Koo et al.   Cancer Discovery

Activating L265P mutations of the MYD88 gene are common in primary central nervous system lymphoma

(2011) Manuel Montesinos-Rongen et al.   ACTA NEUROPATHOLOGICA

JAK2 rearrangements, including the novel SEC31A-JAK2 fusion, are recurrent in classical Hodgkin lymphoma

(2011) K. Van Roosbroeck et al.   BLOOD

FERM domain mutations induce gain of function in JAK3 in adult T-cell leukemia/lymphoma

(2011) N. E. Elliott et al.   BLOOD

High STAT5 levels mediate imatinib resistance and indicate disease progression in chronic myeloid leukemia

(2011) W. Warsch et al.   BLOOD

The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors

(2011) E. A. Nelson et al.   BLOOD

MicroRNA-21: A novel therapeutic target in human cancer

(2011) Xuan Pan et al.   CANCER BIOLOGY & THERAPY

Gain-of-function mutations ininterleukin-7 receptor-α(IL7R) in childhood acute lymphoblastic leukemias

(2011) Chen Shochat et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Potentiation of Nilotinib-mediated cell death in the context of the bone marrow microenvironment requires a promiscuous JAK inhibitor in CML

(2011) Rajesh R. Nair et al.   LEUKEMIA RESEARCH

Oncogenic IL7R gain-of-function mutations in childhood T-cell acute lymphoblastic leukemia

(2011) Priscila P Zenatti et al.   NATURE GENETICS

Genomics and the Multifactorial Nature of Human Autoimmune Disease

(2011) Judy H. Cho et al.   NEW ENGLAND JOURNAL OF MEDICINE

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells

(2010) Vijay Ramakrishnan et al.   AMERICAN JOURNAL OF HEMATOLOGY

Stat5a serine 725 and 779 phosphorylation is a prerequisite for hematopoietic transformation

(2010) K. Friedbichler 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

Integrative analysis reveals selective 9p24.1 amplification, increased PD-1 ligand expression, and further induction via JAK2 in nodular sclerosing Hodgkin lymphoma and primary mediastinal large B-cell lymphoma

(2010) M. R. Green et al.   BLOOD

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

(2010) R. C. Harvey et al.   BLOOD

First report of phase 2 study of dasatinib with hyper-CVAD for the frontline treatment of patients with Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia

(2010) F. Ravandi et al.   BLOOD

Distinct Clinical Phenotypes Associated with JAK2V617F Reflect Differential STAT1 Signaling

(2010) Edwin Chen et al.   CANCER CELL

Cooperative Epigenetic Modulation by Cancer Amplicon Genes

(2010) Lixin Rui et al.   CANCER CELL

Chromosome 9p24 abnormalities: prevalence, description of novel JAK2 translocations, JAK2V617F mutation analysis and clinicopathologic correlates

(2010) Mrinal M. Patnaik et al.   EUROPEAN JOURNAL OF HAEMATOLOGY

Janus kinase 2 regulates Bcr–Abl signaling in chronic myeloid leukemia

(2010) A Samanta et al.   LEUKEMIA

A novel small molecule inhibits STAT3 phosphorylation and DNA binding activity and exhibits potent growth suppressive activity in human cancer cells

(2010) Li Lin et al.   Molecular Cancer

Oncogenically active MYD88 mutations in human lymphoma

(2010) Vu N. Ngo et al.   NATURE

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

(2009) L. Hertzberg et al.   BLOOD

Deregulated expression of cytokine receptor gene, CRLF2, is involved in lymphoid transformation in B-cell precursor acute lymphoblastic leukemia

(2009) L. J. Russell et al.   BLOOD

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

(2009) F. H. Grand et al.   BLOOD

JAK1 mutations are not frequent events in adult T-ALL: a GRAALL study

(2009) Vahid Asnafi et al.   BRITISH JOURNAL OF HAEMATOLOGY

High expression ofBCL3in human myeloma cells is associated with increased proliferation and inferior prognosis

(2009) Anne-Tove Brenne et al.   EUROPEAN JOURNAL OF HAEMATOLOGY

Janus kinase inhibitor INCB20 has antiproliferative and apoptotic effects on human myeloma cells in vitro and in vivo

(2009) R. Burger et al.   MOLECULAR CANCER THERAPEUTICS

JAK2 phosphorylates histone H3Y41 and excludes HP1α from chromatin

(2009) Mark A. Dawson et al.   NATURE

Rearrangement of CRLF2 in B-progenitor– and Down syndrome–associated acute lymphoblastic leukemia

(2009) Charles G Mullighan 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

Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia

(2009) A. Yoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Mitochondrial STAT3 Supports Ras-Dependent Oncogenic Transformation

(2009) D. J. Gough et al.   SCIENCE

Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3

(2008) E. A. Nelson et al.   BLOOD

Specific JAK2 mutation (JAK2R683) and multiple gene deletions in Down syndrome acute lymphoblastic leukemia

(2008) L. Kearney et al.   BLOOD

Somatic Mutations of JAK1 and JAK3 in Acute Leukemias and Solid Cancers

(2008) E. G. Jeong et al.   CLINICAL CANCER RESEARCH

NovelSSBP2-JAK2fusion gene resulting from a t(5;9)(q14.1;p24.1) in pre-B acute lymphocytic leukemia

(2008) Jennifer L. Poitras et al.   GENES CHROMOSOMES & CANCER

Somatically acquiredJAK1mutations in adult acute lymphoblastic leukemia

(2008) Elisabetta Flex et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Mutations of JAK2 in acute lymphoblastic leukaemias associated with Down's syndrome

(2008) Dani Bercovich et al.   LANCET

Comparison of mutated ABL1 and JAK2 as oncogenes and drug targets in myeloproliferative disorders

(2008) C Walz et al.   LEUKEMIA

Incidence and diversity of PAX5 fusion genes in childhood acute lymphoblastic leukemia

(2008) K Nebral et al.   LEUKEMIA

Epigenetic regulation of signal transducer and activator of transcription 3 in acute myeloid leukemia

(2008) Sampa Ghoshal (Gupta) et al.   LEUKEMIA RESEARCH

Mining for JAK–STAT mutations in cancer

(2008) Stefan N. Constantinescu et al.   TRENDS IN BIOCHEMICAL SCIENCES

Identification of somatic JAK1 mutations in patients with acute myeloid leukemia

(2007) Z. Xiang et al.   BLOOD

Cooperative signaling through the signal transducer and activator of transcription 3 and nuclear factor- B pathways in subtypes of diffuse large B-cell lymphoma

(2007) L. T. Lam et al.   BLOOD