Pharmacological Inhibition of Oncogenic STAT3 and STAT5 Signaling in Hematopoietic Cancers

Targeting FLT3 mutations in AML: review of current knowledge and evidence

(2019) Naval Daver et al.   LEUKEMIA

Antimalarial drug pyrimethamine plays a dual role in anti-tumor proliferation and metastasis through targeting DHFR and TP

(2019) Huijuan Liu et al.   MOLECULAR CANCER THERAPEUTICS

Clinical resistance to crenolanib in acute myeloid leukemia due to diverse molecular mechanisms

(2019) Haijiao Zhang et al.   Nature Communications

Decoration of Anti-CD38 on Nanoparticles Carrying a STAT3 Inhibitor Can Improve the Therapeutic Efficacy Against Myeloma

(2019) Yung-Hsing Huang et al.   Cancers

Phase II trial of Lestaurtinib, a JAK2 inhibitor, in patients with myelofibrosis

(2019) John Mascarenhas et al.   LEUKEMIA & LYMPHOMA

Twins with different personalities: STAT5B—but not STAT5A—has a key role in BCR/ABL-induced leukemia

(2019) Sebastian Kollmann et al.   LEUKEMIA

Hematopoietic niche drives FLT3-ITD acute myeloid leukemia resistance to quizartinib via STAT5- and hypoxia- dependent up-regulation of AXL

(2019) Pierre-Yves Dumas et al.   HAEMATOLOGICA

STAT5BN642H drives transformation of NKT cells: a novel mouse model for CD56+ T-LGL leukemia

(2019) Klara Klein et al.   LEUKEMIA

JAK3/STAT3 oncogenic pathway and PRDM1 expression stratify clinicopathologic features of extranodal NK/T‑cell lymphoma, nasal type

(2019) Jumei Liu et al.   ONCOLOGY REPORTS

Quizartinib (AC220): a promising option for acute myeloid leukemia

(2019) Fang Zhou et al.   Drug Design Development and Therapy

STAT3: A Promising Therapeutic Target in Multiple Myeloma

(2019) Chong et al.   Cancers

Structural and functional consequences of the STAT5BN642H driver mutation

(2019) Elvin D. de Araujo et al.   Nature Communications

Oncogenic KIT mutations induce STAT3-dependent autophagy to support cell proliferation in acute myeloid leukemia

(2019) Clément Larrue et al.   Oncogenesis

Fedratinib: First Approval

(2019) Hannah A. Blair   DRUGS

STAT3 and STAT5 Activation in Solid Cancers

(2019) Sebastian Igelmann et al.   Cancers

A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo

(2019) Longchuan Bai et al.   CANCER CELL

A Novel Inhibitor of STAT5 Signaling Overcomes Chemotherapy Resistance in Myeloid Leukemia Cells

(2019) Marie Brachet-Botineau et al.   Cancers

Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma

(2018) Tycel J. Phillips et al.   BLOOD

Pacritinib and its use in the treatment of patients with myelofibrosis who have thrombocytopenia

(2018) Adolfo Enrique Diaz et al.   Future Oncology

A phase II study of the oral JAK1/JAK2 inhibitor ruxolitinib in advanced relapsed/refractory Hodgkin lymphoma

(2018) Eric Van Den Neste et al.   HAEMATOLOGICA

Pharmacologic inhibition of STAT5 in acute myeloid leukemia

(2018) Bettina Wingelhofer et al.   LEUKEMIA

Implications of STAT3 and STAT5 signaling on gene regulation and chromatin remodeling in hematopoietic cancer

(2018) Bettina Wingelhofer et al.   LEUKEMIA

Phase 2 study of gandotinib (LY2784544) in patients with myeloproliferative neoplasms

(2018) J. Berdeja et al.   LEUKEMIA RESEARCH

B Cell Lymphoma Immunotherapy Using TLR9-Targeted Oligonucleotide STAT3 Inhibitors

(2018) Xingli Zhao et al.   MOLECULAR THERAPY

Two decades of research in discovery of anticancer drugs targeting STAT3, how close are we?

(2018) Jenny D. Beebe et al.   PHARMACOLOGY & THERAPEUTICS

NS-018 reduces myeloma cell proliferation and suppresses osteolysis through inhibition of the JAK2 and Src signaling pathways

(2018) Ayumi Honda et al.   Blood Cancer Journal

A phase II study of the oral JAK1/JAK2 inhibitor ruxolitinib in advanced relapsed/refractory Hodgkin lymphoma

(2018) Eric Van Den Neste et al.   HAEMATOLOGICA

Momelotinib versus best available therapy in patients with myelofibrosis previously treated with ruxolitinib (SIMPLIFY 2): a randomised, open-label, phase 3 trial

(2018) Claire N Harrison et al.   Lancet Haematology

Constitutive Activation of STAT3 in Myeloma Cells Cultured in a Three-Dimensional, Reconstructed Bone Marrow Model

(2018) Yung-Hsing Huang et al.   Cancers

Oncogenic activation of the STAT3 pathway drives PD-L1 expression in natural killer/T-cell lymphoma

(2018) Tammy Linlin Song et al.   BLOOD

Targeting STAT5 or STAT5-regulated pathways suppresses leukemogenesis of Ph+ acute lymphoblastic leukemia

(2018) Valentina Minieri et al.   CANCER RESEARCH

STAT3 localizes to the ER, acting as a gatekeeper for ER-mitochondrion Ca2+ fluxes and apoptotic responses

(2018) Lidia Avalle et al.   CELL DEATH AND DIFFERENTIATION

Nucleus, Mitochondrion, or Reticulum? STAT3 à La Carte

(2018) Lidia Avalle et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

STAT3-coordinated migration facilitates the dissemination of diffuse large B-cell lymphomas

(2018) Yi-Ru Pan et al.   Nature Communications

STAT3 is constitutively acetylated on lysine 685 residues in chronic lymphocytic leukemia cells

(2018) Uri Rozovski et al.   Oncotarget

Clinical Validation of KIT Inhibition in Advanced Systemic Mastocytosis

(2018) John H. Baird et al.   Current Hematologic Malignancy Reports

Genetic Hierarchy of Acute Myeloid Leukemia: From Clonal Hematopoiesis to Molecular Residual Disease

(2018) Jean-Alain Martignoles et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Antisense STAT3 inhibitor decreases viability of myelodysplastic and leukemic stem cells

(2018) Aditi Shastri et al.   JOURNAL OF CLINICAL INVESTIGATION

Clinical use of FLT3 inhibitors in acute myeloid leukemia

(2018) Grerk Sutamtewagul et al.   OncoTargets and Therapy

Sinomenine derivative YL064: a novel STAT3 inhibitor with promising anti-myeloma activity

(2018) Yingying Wang et al.   Cell Death & Disease

STAT3 antisense oligonucleotide AZD9150 in a subset of patients with heavily pretreated lymphoma: results of a phase 1b trial

(2018) Matthew J. Reilley et al.   Journal for ImmunoTherapy of Cancer

Combined targeting of STAT3 and STAT5: a novel approach to overcome drug resistance in chronic myeloid leukemia

(2017) Karoline V. Gleixner et al.   HAEMATOLOGICA

Mechanisms of Resistance to FLT3 Inhibitors and the Role of the Bone Marrow Microenvironment

(2017) Gabriel Ghiaur et al.   HEMATOLOGY-ONCOLOGY CLINICS OF NORTH AMERICA

STAT5BN642H is a driver mutation for T cell neoplasia

(2017) Ha Thi Thanh Pham et al.   JOURNAL OF CLINICAL INVESTIGATION

SIMPLIFY-1: A Phase III Randomized Trial of Momelotinib Versus Ruxolitinib in Janus Kinase Inhibitor–Naïve Patients With Myelofibrosis

(2017) Ruben A. Mesa et al.   JOURNAL OF CLINICAL ONCOLOGY

New Inhibitor Targeting Signal Transducer and Activator of Transcription 5 (STAT5) Signaling in Myeloid Leukemias

(2017) Ludovic Juen et al.   JOURNAL OF MEDICINAL CHEMISTRY

O-GlcNAcylation of STAT5 controls tyrosine phosphorylation and oncogenic transcription in STAT5-dependent malignancies

(2017) P Freund et al.   LEUKEMIA

STAT5A/5B-specific expansion and transformation of hematopoietic stem cells

(2017) S Ghanem et al.   Blood Cancer Journal

The effect of the JAK2 inhibitor TG101209 against T cell acute lymphoblastic leukemia (T-ALL) is mediated by inhibition of JAK-STAT signaling and activation of the crosstalk between apoptosis and autophagy signaling

(2017) Zhao Cheng et al.   Oncotarget

Crenolanib is a type I tyrosine kinase inhibitor that inhibits mutant KIT D816 isoforms prevalent in systemic mastocytosis and core binding factor leukemia

(2017) Kerstin Maria Kampa-Schittenhelm et al.   Oncotarget

Combined targeting of STAT3 and STAT5: a novel approach to overcome drug resistance in chronic myeloid leukemia

(2017) Karoline V. Gleixner et al.   HAEMATOLOGICA

Abnormal repression of SHP-1, SHP-2 and SOCS-1 transcription sustains the activation of the JAK/STAT3 pathway and the progression of the disease in multiple myeloma

(2017) Asma Beldi-Ferchiou et al.   PLoS One

Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b

(2017) Nagarajan Elumalai et al.   Scientific Reports

STAT3-induced long noncoding RNAs in multiple myeloma cells display different properties in cancer

(2017) Stefanie Binder et al.   Scientific Reports

Serum-resistant CpG-STAT3 decoy for targeting survival and immune checkpoint signaling in acute myeloid leukemia

(2016) Q. Zhang et al.   BLOOD

Genetic basis and molecular pathophysiology of classical myeloproliferative neoplasms

(2016) William Vainchenker et al.   BLOOD

STAT3 mutations are not sufficient to induce large granular lymphocytic leukaemia in mice

(2016) Avik Dutta et al.   BRITISH JOURNAL OF HAEMATOLOGY

Pioglitazone together with imatinib in chronic myeloid leukemia: A proof of concept study

(2016) Philippe Rousselot et al.   CANCER

Pyrimethamine as a Potent and Selective Inhibitor of Acute Myeloid Leukemia Identified by High-throughput Drug Screening

(2016) Amit Sharma et al.   CURRENT CANCER DRUG TARGETS

Stat3 promotes mitochondrial transcription and oxidative respiration during maintenance and induction of naive pluripotency

(2016) Elena Carbognin et al.   EMBO JOURNAL

Primary analysis of a phase II open-label trial of INCB039110, a selective JAK1 inhibitor, in patients with myelofibrosis

(2016) John O. Mascarenhas et al.   HAEMATOLOGICA

At High Levels, Constitutively Activated STAT3 Induces Apoptosis of Chronic Lymphocytic Leukemia Cells

(2016) Uri Rozovski et al.   JOURNAL OF IMMUNOLOGY

Multiple myeloma exosomes establish a favourable bone marrow microenvironment with enhanced angiogenesis and immunosuppression

(2016) Jinheng Wang et al.   JOURNAL OF PATHOLOGY

A phase I, open-label, dose-escalation, multicenter study of the JAK2 inhibitor NS-018 in patients with myelofibrosis

(2016) S Verstovsek et al.   LEUKEMIA

Lineage-specific STAT5 target gene activation in hematopoietic progenitor cells predicts the FLT3+-mediated leukemic phenotype

(2016) T A Müller et al.   LEUKEMIA

STAT3 inhibitor has potent antitumor activity in B-lineage acute lymphoblastic leukemia cells overexpressing the high mobility group A1 (HMGA1)–STAT3 pathway

(2016) Amy Belton et al.   LEUKEMIA & LYMPHOMA

SUMOylation and SENP3 regulate STAT3 activation in head and neck cancer

(2016) Z Zhou et al.   ONCOGENE

STAT5 Is a Key Regulator in NK Cells and Acts as a Molecular Switch from Tumor Surveillance to Tumor Promotion

(2016) D. Gotthardt et al.   Cancer Discovery

CM363, a novel naphthoquinone derivative which acts as multikinase modulator and overcomes imatinib resistance in chronic myelogenous leukemia

(2016) Borja Guerra et al.   Oncotarget

Oncogenic STAT5 signaling promotes oxidative stress in chronic myeloid leukemia cells by repressing antioxidant defenses

(2016) Jerome Bourgeais et al.   Oncotarget

Piperlongumine induces apoptosis and reduces bortezomib resistance by inhibiting STAT3 in multiple myeloma cells

(2016) Yao Yao et al.   Oncotarget

Leukemic stem cell persistence in chronic myeloid leukemia patients in deep molecular response induced by tyrosine kinase inhibitors and the impact of therapy discontinuation

(2016) Jean Claude Chomel et al.   Oncotarget

Primary analysis of a phase II open-label trial of INCB039110, a selective JAK1 inhibitor, in patients with myelofibrosis

(2016) John O. Mascarenhas et al.   HAEMATOLOGICA

STAT3 Undergoes Acetylation-dependent Mitochondrial Translocation to Regulate Pyruvate Metabolism

(2016) Yan S. Xu et al.   Scientific Reports

Nanomolar Inhibitors of the Transcription Factor STAT5b with High Selectivity over STAT5a

(2015) Nagarajan Elumalai et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Deletion of Stat3 in hematopoietic cells enhances thrombocytosis and shortens survival in a JAK2-V617F mouse model of MPN

(2015) J. Grisouard et al.   BLOOD

The effect of long-term ruxolitinib treatment on JAK2p.V617F allele burden in patients with myelofibrosis

(2015) M. Deininger et al.   BLOOD

A phase I/II study of sunitinib and intensive chemotherapy in patients over 60 years of age with acute myeloid leukaemia and activatingFLT3mutations

(2015) Walter Fiedler et al.   BRITISH JOURNAL OF HAEMATOLOGY

CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms

(2015) Sara C. Meyer et al.   CANCER CELL

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia

(2015) Shuo-Chieh Wu et al.   CANCER CELL

Phase I study of OPB-51602, an oral inhibitor of signal transducer and activator of transcription 3, in patients with relapsed/refractory hematological malignancies

(2015) Michinori Ogura et al.   CANCER SCIENCE

A Phase I/II Study of the Janus Kinase (JAK)1 and 2 Inhibitor Ruxolitinib in Patients With Relapsed or Refractory Acute Myeloid Leukemia

(2015) Naveen Pemmaraju et al.   Clinical Lymphoma Myeloma & Leukemia

Cytokine‐induced megakaryocytic differentiation is regulated by genome‐wide loss of a uSTAT transcriptional program

(2015) Hyun Jung Park et al.   EMBO JOURNAL

Deletion of Stat3 enhances myeloid cell expansion and increases the severity of myeloproliferative neoplasms in Jak2V617F knock-in mice

(2015) D Yan et al.   LEUKEMIA

A phase I, open-label, multi-center study of the JAK2 inhibitor AZD1480 in patients with myelofibrosis

(2015) Srdan Verstovsek et al.   LEUKEMIA RESEARCH

Impact of the N-Terminal Domain of STAT3 in STAT3-Dependent Transcriptional Activity

(2015) Tiancen Hu et al.   MOLECULAR AND CELLULAR BIOLOGY

Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia

(2015) Z. Liao et al.   MOLECULAR CANCER THERAPEUTICS

Hitting the right spot: Mechanism of action of OPB-31121, a novel and potent inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3)

(2015) Lara Brambilla et al.   Molecular Oncology

Erosion of the chronic myeloid leukaemia stem cell pool by PPARγ agonists

(2015) Stéphane Prost et al.   NATURE

STAT3-driven transcription depends upon the dimethylation of K49 by EZH2

(2015) Maupali Dasgupta et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

AZD9150, a next-generation antisense oligonucleotide inhibitor of STAT3 with early evidence of clinical activity in lymphoma and lung cancer

(2015) David Hong et al.   Science Translational Medicine

Honokiol Inhibits Constitutive and Inducible STAT3 Signaling via PU.1-Induced SHP1 Expression in Acute Myeloid Leukemia Cells

(2015) Laixi Bi et al.   TOHOKU JOURNAL OF EXPERIMENTAL MEDICINE

Activating mutations of STAT5B and STAT3 in lymphomas derived from γδ-T or NK cells

(2015) Can Küçük et al.   Nature Communications

Stat5-deficient hematopoiesis is permissive for Myc-induced B-cell leukemogenesis

(2015) Zhengqi Wang et al.   Oncotarget

Mitochondrial Ca2+ and membrane potential, an alternative pathway for Interleukin 6 to regulate CD4 cell effector function

(2015) Rui Yang et al.   eLife

Stat5 Exerts Distinct, Vital Functions in the Cytoplasm and Nucleus of Bcr-Abl+ K562 and Jak2(V617F)+ HEL Leukemia Cells

(2015) Axel Weber et al.   Cancers

A Chemical Biology Approach to Developing STAT Inhibitors: Molecular Strategies for Accelerating Clinical Translation

(2015) Erik A. Nelson et al.   Oncotarget

STAT5 triggers BCR-ABL1 mutation by mediating ROS production in chronic myeloid leukaemia

(2015) Wolfgang Warsch et al.   Oncotarget

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

S-Glutathionylation at Cys328 and Cys542 Impairs STAT3 Phosphorylation

(2014) Elena Butturini et al.   ACS Chemical Biology

Effects of Jak2 Type 1 Inhibitors NVP-BSK805 and NVP-BVB808 on Jak2 Mutation-Positive and Bcr-Abl-Positive Cell Lines

(2014) Frauke Ringel et al.   ACTA HAEMATOLOGICA

Uncovering the pathogenesis of large granular lymphocytic leukemia—novelSTAT3andSTAT5bmutations

(2014) Hanna L. M. Rajala et al.   ANNALS OF MEDICINE

JAK2/STAT5 inhibition by nilotinib with ruxolitinib contributes to the elimination of CML CD34+ cells in vitro and in vivo

(2014) P. Gallipoli et al.   BLOOD

STAT3 supports experimental K-RasG12D-induced murine myeloproliferative neoplasms dependent on serine phosphorylation

(2014) D. J. Gough et al.   BLOOD

Deregulation in STAT signaling is important for cutaneous T-cell lymphoma (CTCL) pathogenesis and cancer progression

(2014) Elena Netchiporouk et al.   CELL CYCLE

Selective JAK2 Inhibition Specifically Decreases Hodgkin Lymphoma and Mediastinal Large B-cell Lymphoma Growth In Vitro and In Vivo

(2014) Y. Hao et al.   CLINICAL CANCER RESEARCH

Resistance of Cancer Cells to Targeted Therapies Through the Activation of Compensating Signaling Loops

(2014) Viktoria Manstein et al.   Current Signal Transduction Therapy

The activating STAT5B N642H mutation is a common abnormality in pediatric T-cell acute lymphoblastic leukemia and confers a higher risk of relapse

(2014) O. R. Bandapalli et al.   HAEMATOLOGICA

Critical Role for Lysine 685 in Gene Expression Mediated by Transcription Factor Unphosphorylated STAT3

(2014) Maupali Dasgupta et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Combined STAT3 and BCR-ABL1 inhibition induces synthetic lethality in therapy-resistant chronic myeloid leukemia

(2014) A M Eiring et al.   LEUKEMIA

Frequent STAT5B mutations in γδ hepatosplenic T-cell lymphomas

(2014) A Nicolae et al.   LEUKEMIA

Phospho-flow detection of constitutive and cytokine-induced pSTAT3/5, pAKT and pERK expression highlights novel prognostic biomarkers for patients with multiple myeloma

(2014) R Brown et al.   LEUKEMIA

Novel activating STAT5B mutations as putative drivers of T-cell acute lymphoblastic leukemia

(2014) M Kontro et al.   LEUKEMIA

Targeting STAT5 in Hematologic Malignancies through Inhibition of the Bromodomain and Extra-Terminal (BET) Bromodomain Protein BRD2

(2014) S. Liu et al.   MOLECULAR CANCER THERAPEUTICS

Evaluation of the In Vitro and In Vivo Efficacy of the JAK Inhibitor AZD1480 against JAK-Mutated Acute Lymphoblastic Leukemia

(2014) S. Suryani et al.   MOLECULAR CANCER THERAPEUTICS

The Natural Chemopreventive Agent Sulforaphane Inhibits STAT5 Activity

(2014) Sophia Pinz et al.   PLoS One

BCR-ABL Affects STAT5A and STAT5B Differentially

(2014) Michael Schaller-Schönitz et al.   PLoS One

Viability and stress protection of chronic lymphoid leukemia cells involves overactivation of mitochondrial phosphoSTAT3Ser727

(2014) C Capron et al.   Cell Death & Disease

Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein

(2014) Abbarna A. Cumaraswamy et al.   ACS Medicinal Chemistry Letters

Regulation of Stat5 by FAK and PAK1 in Oncogenic FLT3- and KIT-Driven Leukemogenesis

(2014) Anindya Chatterjee et al.   Cell Reports

STAT3 in Cancer—Friend or Foe?

(2014) Hai-Feng Zhang et al.   Cancers

TLR9-mediated siRNA delivery for targeting of normal and malignant human hematopoietic cells in vivo

(2013) Q. Zhang et al.   BLOOD

Leukemia cell-targeted STAT3 silencing and TLR9 triggering generate systemic antitumor immunity

(2013) D. M. S. Hossain et al.   BLOOD

Discovery of somatic STAT5b mutations in large granular lymphocytic leukemia

(2013) H. L. M. Rajala et al.   BLOOD

Open-label study of oral CEP-701 (lestaurtinib) in patients with polycythaemia vera or essential thrombocythaemia withJAK2-V617F mutation

(2013) Elizabeth Hexner et al.   BRITISH JOURNAL OF HAEMATOLOGY

Phosphorylation of EZH2 Activates STAT3 Signaling via STAT3 Methylation and Promotes Tumorigenicity of Glioblastoma Stem-like Cells

(2013) Eunhee Kim et al.   CANCER CELL

A Novel Inhibitor of STAT3 Homodimerization Selectively Suppresses STAT3 Activity and Malignant Transformation

(2013) X. Zhang et al.   CANCER RESEARCH

Differential Contributions of STAT5A and STAT5B to Stress Protection and Tyrosine Kinase Inhibitor Resistance of Chronic Myeloid Leukemia Stem/Progenitor Cells

(2013) L. Casetti et al.   CANCER RESEARCH

Regulation of STAT signaling by acetylation

(2013) Shougang Zhuang   CELLULAR SIGNALLING

Inhibiting Aberrant Signal Transducer and Activator of Transcription Protein Activation with Tetrapodal, Small Molecule Src Homology 2 Domain Binders: Promising Agents against Multiple Myeloma

(2013) Brent D. G. Page et al.   JOURNAL OF MEDICINAL CHEMISTRY

STAT transcription factors in hematopoiesis and leukemogenesis: opportunities for therapeutic intervention

(2013) K A Dorritie et al.   LEUKEMIA

A role for reactive oxygen species in JAK2 V617F myeloproliferative neoplasm progression

(2013) C Marty et al.   LEUKEMIA

PAK-dependent STAT5 serine phosphorylation is required for BCR-ABL-induced leukemogenesis

(2013) A Berger et al.   LEUKEMIA

Nanoparticle delivery of inhibitory signal transducer and activator of transcription 3 G-quartet oligonucleotides blocks tumor growth inHMGA1transgenic model of T-cell leukemia

(2013) Joelle Hillion et al.   LEUKEMIA & LYMPHOMA

Combination of YM155, a survivin suppressant with a STAT3 inhibitor: A new strategy to treat diffuse large B-cell lymphoma

(2013) Naoki Kaneko et al.   LEUKEMIA RESEARCH

Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor

(2013) Srdan Verstovsek et al.   LEUKEMIA RESEARCH

STAT5 Outcompetes STAT3 To Regulate the Expression of the Oncogenic Transcriptional Modulator BCL6

(2013) S. R. Walker et al.   MOLECULAR AND CELLULAR BIOLOGY

Distinct roles of STAT3 and STAT5 in the pathogenesis and targeted therapy of breast cancer

(2013) Sarah R. Walker et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Correction: The MEK-ERK Pathway Is Necessary for Serine Phosphorylation of Mitochondrial STAT3 and Ras-Mediated Transformation

(2013) Daniel J. Gough et al.   PLoS One

STAT3 suppresses transcription of proapoptotic genes in cancer cells with the involvement of its N-terminal domain

(2013) Olga A. Timofeeva et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A novel STAT inhibitor, OPB-31121, has a significant antitumor effect on leukemia with STAT-addictive oncokinases

(2013) F Hayakawa et al.   Blood Cancer Journal

Peripheral T-Cell Lymphomas: A Review of Current Approaches and Hopes for the Future

(2013) Alan P. Skarbnik et al.   Frontiers in Oncology

Essential role for Stat5a/b in myeloproliferative neoplasms induced by BCR-ABL1 and JAK2V617F in mice

(2012) C. Walz et al.   BLOOD

STAT3 mutations unify the pathogenesis of chronic lymphoproliferative disorders of NK cells and T-cell large granular lymphocyte leukemia

(2012) A. Jerez et al.   BLOOD

Mouse hematopoietic cell-targeted STAT3 deletion: stem/progenitor cell defects, mitochondrial dysfunction, ROS overproduction, and a rapid aging-like phenotype

(2012) C. Mantel et al.   BLOOD

Biology and significance of the JAK/STAT signalling pathways

(2012) Hiu Kiu et al.   GROWTH FACTORS

Signal Transducer and Activator of Transcription 5b (Stat5b) Serine 193 Is a Novel Cytokine-induced Phospho-regulatory Site That Is Constitutively Activated in Primary Hematopoietic Malignancies

(2012) Abhisek Mitra et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Mechanisms of Unphosphorylated STAT3 Transcription Factor Binding to DNA

(2012) Olga A. Timofeeva et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Import of the Transcription Factor STAT3 into Mitochondria Depends on GRIM-19, a Component of the Electron Transport Chain

(2012) Prasad Tammineni et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

STAT3 mutations are highly specific for large granular lymphocytic leukemia

(2012) A Fasan et al.   LEUKEMIA

Evidence for a protective role of the STAT5 transcription factor against oxidative stress in human leukemic pre-B cells

(2012) E Cholez et al.   LEUKEMIA

Indirubin derivatives induce apoptosis of chronic myelogenous leukemia cells involving inhibition of Stat5 signaling

(2012) Sangkil Nam et al.   Molecular Oncology

SomaticSTAT3Mutations in Large Granular Lymphocytic Leukemia

(2012) Hanna L.M. Koskela et al.   NEW ENGLAND JOURNAL OF MEDICINE

Src family kinases mediate cytoplasmic retention of activated STAT5 in BCR–ABL-positive cells

(2012) N Chatain et al.   ONCOGENE

JAK/STAT signaling in hematological malignancies

(2012) W Vainchenker et al.   ONCOGENE

H2O2 Production Downstream of FLT3 Is Mediated by p22phox in the Endoplasmic Reticulum and Is Required for STAT5 Signalling

(2012) John F. Woolley et al.   PLoS One

Acetylated STAT3 is crucial for methylation of tumor-suppressor gene promoters and inhibition by resveratrol results in demethylation

(2012) H. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of PPARγLigands on Leukemia

(2012) Yoko Tabe et al.   PPAR Research

Nongenomic STAT5-dependent effects on Golgi apparatus and endoplasmic reticulum structure and function

(2011) Jason E. Lee et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Identification of a non-phosphorylated, cell permeable, small molecule ligand for the Stat3 SH2 domain

(2011) Brent D.G. Page et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Critical requirement for Stat5 in a mouse model of polycythemia vera

(2011) D. Yan et al.   BLOOD

Stat3 signaling in acute myeloid leukemia: ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitor

(2011) M. S. Redell 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

Celastrol inhibits proliferation and induces chemosensitization through down-regulation of NF-κB and STAT3 regulated gene products in multiple myeloma cells

(2011) Radhamani Kannaiyan et al.   BRITISH JOURNAL OF PHARMACOLOGY

Antagonism of the Stat3-Stat3 Protein Dimer with Salicylic Acid Based Small Molecules

(2011) Steven Fletcher et al.   ChemMedChem

The Ph-positive and Ph-negative myeloproliferative neoplasms: some topical pre-clinical and clinical issues

(2011) R. A. Van Etten et al.   HAEMATOLOGICA

A small molecule, LLL12 inhibits constitutive STAT3 and IL-6-induced STAT3 signaling and exhibits potent growth suppressive activity in human multiple myeloma cells

(2011) Li Lin et al.   INTERNATIONAL JOURNAL OF CANCER

The role of the N-terminal domain in dimerization and nucleocytoplasmic shuttling of latent STAT3

(2011) M. Vogt et al.   JOURNAL OF CELL SCIENCE

Ebf1orPax5haploinsufficiency synergizes with STAT5 activation to initiate acute lymphoblastic leukemia

(2011) Lynn M. Heltemes-Harris et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Small Molecule STAT5-SH2 Domain Inhibitors Exhibit Potent Antileukemia Activity

(2011) Brent D. G. Page et al.   JOURNAL OF MEDICINAL CHEMISTRY

The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells

(2011) K A Monaghan et al.   LEUKEMIA

Dual inhibition of Jak2 and STAT5 enhances killing of myeloproliferative neoplasia cells

(2011) M Bar-Natan et al.   LEUKEMIA

Epigenetic repression of the Igk locus by STAT5-mediated recruitment of the histone methyltransferase Ezh2

(2011) Malay Mandal et al.   NATURE IMMUNOLOGY

Opposing regulation of the locus encoding IL-17 through direct, reciprocal actions of STAT3 and STAT5

(2011) Xiang-Ping Yang et al.   NATURE IMMUNOLOGY

Challenging issues in pediatric oncology

(2011) Ching-Hon Pui et al.   Nature Reviews Clinical Oncology

Redeployment-based drug screening identifies the anti-helminthic niclosamide as anti-myeloma therapy that also reduces free light chain production

(2011) F L Khanim et al.   Blood Cancer Journal

The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma

(2011) E Derenzini et al.   Blood Cancer Journal

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

Expression of pSTAT5 predicts FLT3 internal tandem duplications in acute myeloid leukemia

(2010) Ellen Christina Obermann et al.   ANNALS OF HEMATOLOGY

Mitochondrial translocation of signal transducer and activator of transcription 5 (STAT5) in leukemic T cells and cytokine-stimulated cells

(2010) Fu-Yu Chueh et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The role of Stat5 transcription factors as tumor suppressors or oncogenes

(2010) G. Ferbeyre et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

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

(2010) K. Friedbichler et al.   BLOOD

STAT3 is constitutively phosphorylated on serine 727 residues, binds DNA, and activates transcription in CLL cells

(2010) I. Hazan-Halevy et al.   BLOOD

Modulation of Gene Expression and Tumor Cell Growth by Redox Modification of STAT3

(2010) L. Li et al.   CANCER RESEARCH

Targeted Blockage of Signal Transducer and Activator of Transcription 5 Signaling Pathway with Decoy Oligodeoxynucleotides Suppresses Leukemic K562 Cell Growth

(2010) Xiaozhong Wang et al.   DNA AND CELL BIOLOGY

Stat5 is indispensable for the maintenance ofbcr/abl-positive leukaemia

(2010) Andrea Hoelbl et al.   EMBO Molecular Medicine

Phase I study of sorafenib in patients with refractory or relapsed acute leukemias

(2010) G. Borthakur et al.   HAEMATOLOGICA

Preclinical characterization of atiprimod, a novel JAK2 AND JAK3 inhibitor

(2010) Alfonso Quintás-Cardama et al.   INVESTIGATIONAL NEW DRUGS

Mechanisms of STAT Protein Activation by Oncogenic KIT Mutants in Neoplastic Mast Cells

(2010) Amandine Chaix et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Phase I/II Study of Combination Therapy With Sorafenib, Idarubicin, and Cytarabine in Younger Patients With Acute Myeloid Leukemia

(2010) Farhad Ravandi et al.   JOURNAL OF CLINICAL ONCOLOGY

Effective targeting of STAT5-mediated survival in myeloproliferative neoplasms using ABT-737 combined with rapamycin

(2010) G Li et al.   LEUKEMIA

The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival

(2010) A Scuto et al.   LEUKEMIA

A randomized phase I clinical and biologic study of two schedules of sorafenib in patients with myelodysplastic syndrome or acute myeloid leukemia: a NCIC (National Cancer Institute of Canada) Clinical Trials Group Study

(2010) Michael Crump et al.   LEUKEMIA & LYMPHOMA

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

AZ960, a Novel Jak2 Inhibitor, Induces Growth Arrest and Apoptosis in Adult T-Cell Leukemia Cells

(2010) J. Yang et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Inhibition of Constitutive Activation of STAT3 by Curcurbitacin-I (JSI-124) Sensitized Human B-Leukemia Cells to Apoptosis

(2010) G. Ishdorj et al.   MOLECULAR CANCER THERAPEUTICS

High frequency of concomitant mastocytosis in patients with acute myeloid leukemia exhibiting the transforming KIT mutation D816V

(2010) Robert Fritsche-Polanz et al.   Molecular Oncology

Reversible methylation of promoter-bound STAT3 by histone-modifying enzymes

(2010) J. Yang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of a New Series of STAT3 Inhibitors by Virtual Screening

(2010) Kenji Matsuno et al.   ACS Medicinal Chemistry Letters

Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML

(2009) J. Zhou et al.   BLOOD

KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation

(2009) Y. Shiotsu et al.   BLOOD

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

LLL-3, a STAT3 inhibitor, represses BCR-ABL-positive cell proliferation, activates apoptosis and improves the effects of Imatinib mesylate

(2009) Andre Luiz Mencalha et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Disruption of Transcriptionally Active Stat3 Dimers with Non-phosphorylated, Salicylic Acid-Based Small Molecules: Potent in vitro and Tumor Cell Activities

(2009) Steven Fletcher et al.   CHEMBIOCHEM

Loss of STAT5 causes liver fibrosis and cancer development through increased TGF-β and STAT3 activation

(2009) Atsushi Hosui et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Telomere Shortening and Oxidative Stress in Aged Macrophages Results in Impaired STAT5a Phosphorylation

(2009) C. Sebastian et al.   JOURNAL OF IMMUNOLOGY

A Rac GTPase-Activating Protein, MgcRacGAP, Is a Nuclear Localizing Signal-Containing Nuclear Chaperone in the Activation of STAT Transcription Factors

(2009) T. Kawashima et al.   MOLECULAR AND CELLULAR BIOLOGY

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

Chemical Probes that Competitively and Selectively Inhibit Stat3 Activation

(2009) Xuejun Xu et al.   PLoS One

Avicin D: A Protein Reactive Plant Isoprenoid Dephosphorylates Stat 3 by Regulating Both Kinase and Phosphatase Activities

(2009) Valsala Haridas et al.   PLoS One

Mitochondrial STAT3 Supports Ras-Dependent Oncogenic Transformation

(2009) D. J. Gough et al.   SCIENCE

KIT and Mastocytosis

(2008) Ken-Hong Lim et al.   ACTA HAEMATOLOGICA

IL-21 is expressed in Hodgkin lymphoma and activates STAT5: evidence that activated STAT5 is required for Hodgkin lymphomagenesis

(2008) F. A. Scheeren et al.   BLOOD

Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3

(2008) E. A. Nelson et al.   BLOOD

A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response

(2008) K. W. Pratz et al.   BLOOD

Oncogenic Kit controls neoplastic mast cell growth through a Stat5/PI3-kinase signaling cascade

(2008) N. Harir et al.   BLOOD

Internal tandem duplication of FLT3 (FLT3/ITD) induces increased ROS production, DNA damage, and misrepair: implications for poor prognosis in AML

(2008) A. Sallmyr et al.   BLOOD

Discovery of Chromone-Based Inhibitors of the Transcription Factor STAT5

(2008) Judith Müller et al.   CHEMBIOCHEM

WP1066, a Novel JAK2 Inhibitor, Suppresses Proliferation and Induces Apoptosis in Erythroid Human Cells Carrying the JAK2 V617F Mutation

(2008) S. Verstovsek et al.   CLINICAL CANCER RESEARCH

Role of Stat3 in suppressing anti-tumor immunity

(2008) Marcin Kortylewski et al.   CURRENT OPINION IN IMMUNOLOGY

Targeting STAT3 in cancer: how successful are we?

(2008) Peibin Yue et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Protein tyrosine phosphatases in the JAK/STAT pathway

(2008) Dan Xu   Frontiers in Bioscience-Landmark

Curcumin induces cell-arrest and apoptosis in association with the inhibition of constitutively active NF-κB and STAT3 pathways in Hodgkin's lymphoma cells

(2008) Gerardo G. Mackenzie et al.   INTERNATIONAL JOURNAL OF CANCER

Avicin D Selectively Induces Apoptosis and Downregulates p-STAT-3, bcl-2, and Survivin in Cutaneous T-Cell Lymphoma Cells

(2008) Chunlei Zhang et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Cucurbitacin I Inhibits Stat3 and Induces Apoptosis in Sézary Cells

(2008) Marloes S. van Kester et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Pathogenesis of myeloma bone disease

(2008) G D Roodman   LEUKEMIA

The kinase inhibitor LS104 induces apoptosis, enhances cytotoxic effects of chemotherapeutic drugs and is targeting the receptor tyrosine kinase FLT3 in acute myeloid leukemia

(2008) Stefan Kasper et al.   LEUKEMIA RESEARCH

Maximal STAT5-Induced Proliferation and Self-Renewal at Intermediate STAT5 Activity Levels

(2008) A. T. J. Wierenga et al.   MOLECULAR AND CELLULAR BIOLOGY

LS104, a non-ATP-competitive small-molecule inhibitor of JAK2, is potently inducing apoptosis in JAK2V617F-positive cells

(2008) D. B. Lipka et al.   MOLECULAR CANCER THERAPEUTICS

Stat3 contributes to resistance toward BCR-ABL inhibitors in a bone marrow microenvironment model of drug resistance

(2008) Nadine N. Bewry et al.   MOLECULAR CANCER THERAPEUTICS

Butein Suppresses Constitutive and Inducible Signal Transducer and Activator of Transcription (STAT) 3 Activation and STAT3-Regulated Gene Products through the Induction of a Protein Tyrosine Phosphatase SHP-1

(2008) M. K. Pandey et al.   MOLECULAR PHARMACOLOGY

The opposite effects of IL-15 and IL-21 on CLL B cells correlate with differential activation of the JAK/STAT and ERK1/2 pathways

(2007) D. de Totero 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