Genetic Interactions of STAT3 and Anticancer Drug Development

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

Diverse Mechanisms of Somatic Structural Variations in Human Cancer Genomes

(2013) Lixing Yang et al.   CELL

Specific fate decisions in adult hepatic progenitor cells driven by MET and EGFR signaling

(2013) M. Kitade et al.   GENES & DEVELOPMENT

Intermittent Preventive Therapy for Malaria During Pregnancy Using 2 vs 3 or More Doses of Sulfadoxine-Pyrimethamine and Risk of Low Birth Weight in Africa

(2013) Kassoum Kayentao et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Tofacitinib (CP-690,550) in combination with methotrexate in patients with active rheumatoid arthritis with an inadequate response to tumour necrosis factor inhibitors: a randomised phase 3 trial

(2013) Gerd R Burmester et al.   LANCET

Expression of AFP and STAT3 Is Involved in Arsenic Trioxide-Induced Apoptosis and Inhibition of Proliferation in AFP-Producing Gastric Cancer Cells

(2013) Yanfei Jia et al.   PLoS One

Antitumor activity of a novel STAT3 inhibitor and redox modulator in non-small cell lung cancer cells

(2012) Xiaoying Liu et al.   BIOCHEMICAL PHARMACOLOGY

EGFR pathway biomarkers in erlotinib-treated patients with advanced pancreatic cancer: translational results from the randomised, crossover phase 3 trial AIO-PK0104

(2012) S Boeck et al.   BRITISH JOURNAL OF CANCER

JAK2-related pathway induces acquired erlotinib resistance in lung cancer cells harboring an epidermal growth factor receptor-activating mutation

(2012) Daijiro Harada et al.   CANCER SCIENCE

U.S. Food and Drug Administration Approval: Ruxolitinib for the Treatment of Patients with Intermediate and High-Risk Myelofibrosis

(2012) A. Deisseroth et al.   CLINICAL CANCER RESEARCH

Ruxolitinib: The First FDA Approved Therapy for the Treatment of Myelofibrosis

(2012) J. Mascarenhas et al.   CLINICAL CANCER RESEARCH

Targeting Stat3 Abrogates EGFR Inhibitor Resistance in Cancer

(2012) M. Sen et al.   CLINICAL CANCER RESEARCH

Let-7 Expression Is a Significant Determinant of Response to Chemotherapy through the Regulation of IL-6/STAT3 Pathway in Esophageal Squamous Cell Carcinoma

(2012) K. Sugimura et al.   CLINICAL CANCER RESEARCH

Platelet-derived growth factor receptors differentially inform intertumoral and intratumoral heterogeneity

(2012) Y. Kim et al.   GENES & DEVELOPMENT

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

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

Small Molecule Inhibitors of Signal Transducer and Activator of Transcription 3 (Stat3) Protein

(2012) Bikash Debnath et al.   JOURNAL OF MEDICINAL CHEMISTRY

Gold(I) Carbene Complexes Causing Thioredoxin 1 and Thioredoxin 2 Oxidation as Potential Anticancer Agents

(2012) Esther Schuh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of IL-6R/JAK1/STAT3 Signaling Induces De Novo Resistance to Irreversible EGFR Inhibitors in Non-Small Cell Lung Cancer with T790M Resistance Mutation

(2012) S. M. Kim et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Tofacitinib, an Oral Janus Kinase Inhibitor, in Active Ulcerative Colitis

(2012) William J. Sandborn et al.   NEW ENGLAND JOURNAL OF MEDICINE

Interleukin-11 Links Oxidative Stress and Compensatory Proliferation

(2012) T. Nishina et al.   Science Signaling

Suppression of Stat3 activity sensitizes gefitinib-resistant non small cell lung cancer cells

(2011) Huan-Chih Chiu et al.   BIOCHEMICAL PHARMACOLOGY

Nonreceptor Tyrosine Kinase BMX Maintains Self-Renewal and Tumorigenic Potential of Glioblastoma Stem Cells by Activating STAT3

(2011) Olga A. Guryanova et al.   CANCER CELL

Stat3/Socs3 Activation by IL-6 Transsignaling Promotes Progression of Pancreatic Intraepithelial Neoplasia and Development of Pancreatic Cancer

(2011) Marina Lesina et al.   CANCER CELL

STAT3 Mediates Resistance to MEK Inhibitor through MicroRNA miR-17

(2011) B. Dai et al.   CANCER RESEARCH

STAT3 Plays a Critical Role in KRAS-Induced Pancreatic Tumorigenesis

(2011) R. B. Corcoran et al.   CANCER RESEARCH

Combined Blockade of Src Kinase and Epidermal Growth Factor Receptor with Gemcitabine Overcomes STAT3-Mediated Resistance of Inhibition of Pancreatic Tumor Growth

(2011) N. S. Nagaraj et al.   CLINICAL CANCER RESEARCH

STAT3 Expression, Molecular Features, Inflammation Patterns, and Prognosis in a Database of 724 Colorectal Cancers

(2011) Teppei Morikawa et al.   CLINICAL CANCER RESEARCH

An adolescent with marked hyperimmuno-globulinemia E showing minimal change nephrotic syndrome and a STAT3 gene mutation

(2011) K. Miyazaki et al.   CLINICAL NEPHROLOGY

The R(h)oads to Stat3: Stat3 activation by the Rho GTPases

(2011) Leda Raptis et al.   EXPERIMENTAL CELL RESEARCH

Pyrimethamine inhibits adult polycystic kidney disease by modulating STAT signaling pathways

(2011) Ayumi Takakura et al.   HUMAN MOLECULAR GENETICS

NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations

(2011) EUNJU PARK et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Mitochondrial-targeted Signal Transducer and Activator of Transcription 3 (STAT3) Protects against Ischemia-induced Changes in the Electron Transport Chain and the Generation of Reactive Oxygen Species

(2011) Karol Szczepanek et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The JAK2/STAT3 signaling pathway is required for growth of CD44+CD24– stem cell–like breast cancer cells in human tumors

(2011) Lauren L.C. Marotta et al.   JOURNAL OF CLINICAL INVESTIGATION

Somatic mutations activating STAT3 in human inflammatory hepatocellular adenomas

(2011) Camilla Pilati et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Phase II failures: 2008–2010

(2011) John Arrowsmith   NATURE REVIEWS DRUG DISCOVERY

Phase III and submission failures: 2007–2010

(2011) John Arrowsmith   NATURE REVIEWS DRUG DISCOVERY

Tyrosine Kinase ETK/BMX Is Up-Regulated in Bladder Cancer and Predicts Poor Prognosis in Patients with Cystectomy

(2011) Shengjie Guo et al.   PLoS One

Antitumor Activity of a Novel Oncrasin Analogue Is Mediated by JNK Activation and STAT3 Inhibition

(2011) Wei Guo et al.   PLoS One

Maintenance of tumor initiating cells of defined genetic composition by nucleostemin

(2011) N. Okamoto et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Clinical value of signal transducers and activators of transcription 3 (STAT3) gene expression in human osteosarcoma

(2010) Yu-Cai Wang et al.   ACTA HISTOCHEMICA

A novel small-molecule disrupts Stat3 SH2 domain–phosphotyrosine interactions and Stat3-dependent tumor processes

(2010) Xiaolei Zhang et al.   BIOCHEMICAL PHARMACOLOGY

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

(2010) I. Hazan-Halevy et al.   BLOOD

Constitutively Active Stat3 Enhances Neu-Mediated Migration and Metastasis in Mammary Tumors via Upregulation of Cten

(2010) I. Barbieri et al.   CANCER RESEARCH

Destructive pulmonary staphylococcal infection in a boy with hyper-IgE syndrome: a novel mutation in the signal transducer and activator of transcription 3 (STAT3) gene (p.Y657S)

(2010) Jin-yan Liu et al.   EUROPEAN JOURNAL OF PEDIATRICS

Antagonistic effect of flavonoids on NSC-741909-mediated antitumor activity via scavenging of reactive oxygen species

(2010) Wei Guo et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A Cell-permeable Stat3 SH2 Domain Mimetic Inhibits Stat3 Activation and Induces Antitumor Cell Effectsin Vitro

(2010) Wei Zhao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Diffuse Large B Cell Lymphoma in Hyper-IgE Syndrome Due To STAT3 Mutation

(2010) Attila Kumánovics et al.   JOURNAL OF CLINICAL IMMUNOLOGY

WT1: a weak spot in KRAS-induced transformation

(2010) Silvia Licciulli et al.   JOURNAL OF CLINICAL INVESTIGATION

Thioredoxin-like 2 regulates human cancer cell growth and metastasis via redox homeostasis and NF-κB signaling

(2010) Ying Qu et al.   JOURNAL OF CLINICAL INVESTIGATION

Oxidative stress in NSC-741909-induced apoptosis of cancer cells

(2010) Xiaoli Wei et al.   Journal of Translational Medicine

Sorafenib Induces Growth Arrest and Apoptosis of Human Glioblastoma Cells through the Dephosphorylation of Signal Transducers and Activators of Transcription 3

(2010) Fan Yang et al.   MOLECULAR CANCER THERAPEUTICS

Oncogenically active MYD88 mutations in human lymphoma

(2010) Vu N. Ngo et al.   NATURE

Diverse somatic mutation patterns and pathway alterations in human cancers

(2010) Zhengyan Kan et al.   NATURE

Epidermal growth factor receptor variant III mediates head and neck cancer cell invasion via STAT3 activation

(2010) S E Wheeler et al.   ONCOGENE

Disruption of Astrocyte STAT3 Signaling Decreases Mitochondrial Function and Increases Oxidative Stress In Vitro

(2010) Theodore A. Sarafian et al.   PLoS One

STAT3 is a substrate of SYK tyrosine kinase in B-lineage leukemia/lymphoma cells exposed to oxidative stress

(2010) F. M. Uckun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synthetic Lethal Screen of an EGFR-Centered Network to Improve Targeted Therapies

(2010) I. Astsaturov et al.   Science Signaling

Expression of activated signal transducer and activator of transcription-3 predicts poor prognosis in cervical squamous-cell carcinoma

(2009) S Takemoto et al.   BRITISH JOURNAL OF CANCER

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

(2009) Michael Hedvat et al.   CANCER CELL

Sustained Src Inhibition Results in Signal Transducer and Activator of Transcription 3 (STAT3) Activation and Cancer Cell Survival via Altered Janus-Activated Kinase-STAT3 Binding

(2009) B. Sen et al.   CANCER RESEARCH

Ferritin Heavy Chain–Mediated Iron Homeostasis and Subsequent Increased Reactive Oxygen Species Production Are Essential for Epithelial-Mesenchymal Transition

(2009) Ke-Hua Zhang et al.   CANCER RESEARCH

Identification of a Stat3-Dependent Transcription Regulatory Network Involved in Metastatic Progression

(2009) J. J. Ranger et al.   CANCER RESEARCH

An Epigenetic Switch Involving NF-κB, Lin28, Let-7 MicroRNA, and IL6 Links Inflammation to Cell Transformation

(2009) Dimitrios Iliopoulos et al.   CELL

Synthetic Lethal Interaction between Oncogenic KRAS Dependency and STK33 Suppression in Human Cancer Cells

(2009) Claudia Scholl et al.   CELL

A Genome-wide RNAi Screen Identifies Multiple Synthetic Lethal Interactions with the Ras Oncogene

(2009) Ji Luo et al.   CELL

Reciprocal Regulation of c-Src and STAT3 in Non-Small Cell Lung Cancer

(2009) L. A. Byers et al.   CLINICAL CANCER RESEARCH

Dangerous liaisons: STAT3 and NF-κB collaboration and crosstalk in cancer

(2009) Sergei I. Grivennikov et al.   CYTOKINE & GROWTH FACTOR REVIEWS

Activated Rac1 requires gp130 for Stat3 activation, cell proliferation and migration

(2009) Rozanne Arulanandam et al.   EXPERIMENTAL CELL RESEARCH

Sorafenib inhibits signal transducer and activator of transcription-3 signaling in cholangiocarcinoma cells by activating the phosphatase shatterproof 2

(2009) Boris R. A. Blechacz et al.   HEPATOLOGY

Stat3 promotes directional cell migration by regulating Rac1 activity via its activator  PIX

(2009) T. S. Teng et al.   JOURNAL OF CELL SCIENCE

Analysis of PTEN, BRAF, and EGFR Status in Determining Benefit From Cetuximab Therapy in Wild-Type KRAS Metastatic Colon Cancer

(2009) Pierre Laurent-Puig et al.   JOURNAL OF CLINICAL ONCOLOGY

Efficacy and safety of intermittent preventive treatment with sulfadoxine-pyrimethamine for malaria in African infants: a pooled analysis of six randomised, placebo-controlled trials

(2009) John J Aponte et al.   LANCET

pY-STAT3 and p53 expression predict outcome for poor prognosis diffuse large B-cell lymphoma treated with high dose chemotherapy and autologous stem cell transplantation

(2009) Douglas A. Stewart et al.   LEUKEMIA & LYMPHOMA

Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1)

(2009) W. Guo et al.   MOLECULAR CANCER THERAPEUTICS

Association of reactive oxygen species levels and radioresistance in cancer stem cells

(2009) Maximilian Diehn et al.   NATURE

Systematic RNA interference reveals that oncogenic KRAS-driven cancers require TBK1

(2009) David A. Barbie et al.   NATURE

A comprehensive catalogue of somatic mutations from a human cancer genome

(2009) Erin D. Pleasance et al.   NATURE

STAT3 inhibition of gluconeogenesis is downregulated by SirT1

(2009) Yongzhan Nie et al.   NATURE CELL BIOLOGY

Screening for Epidermal Growth Factor Receptor Mutations in Lung Cancer

(2009) Rafael Rosell et al.   NEW ENGLAND JOURNAL OF MEDICINE

The STAT3 inhibitor NSC 74859 is effective in hepatocellular cancers with disrupted TGF-β signaling

(2009) L Lin et al.   ONCOGENE

Mitochondrial STAT3 Supports Ras-Dependent Oncogenic Transformation

(2009) D. J. Gough et al.   SCIENCE

Stat3 Promotes Metastatic Progression of Prostate Cancer

(2008) Junaid Abdulghani et al.   AMERICAN JOURNAL OF PATHOLOGY

Is the focus moving toward a combination of targeted drugs?

(2008) Steven Grant   BEST PRACTICE & RESEARCH CLINICAL HAEMATOLOGY

Identification of a Small Molecule with Synthetic Lethality for K-Ras and Protein Kinase C Iota

(2008) W. Guo et al.   CANCER RESEARCH

Activation of Signal Transducer and Activator of Transcription 3 through a Phosphomimetic Serine 727 Promotes Prostate Tumorigenesis Independent of Tyrosine 705 Phosphorylation

(2008) H. R. Qin et al.   CANCER RESEARCH

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

Constitutively Activated STAT3 Frequently Coexpresses with Epidermal Growth Factor Receptor in High-Grade Gliomas and Targeting STAT3 Sensitizes Them to Iressa and Alkylators

(2008) H.-W. Lo et al.   CLINICAL CANCER RESEARCH

The Incidence, Correlation with Tumor-Infiltrating Inflammation, and Prognosis of Phosphorylated STAT3 Expression in Human Gliomas

(2008) M. Abou-Ghazal et al.   CLINICAL CANCER RESEARCH

Inverse Association between Raf Kinase Inhibitory Protein and Signal Transducers and Activators of Transcription 3 Expression in Gastric Adenocarcinoma Patients: Implications for Clinical Outcome

(2008) D. Chatterjee et al.   CLINICAL CANCER RESEARCH

The State of Innovation in Drug Development

(2008) I Kola   CLINICAL PHARMACOLOGY & THERAPEUTICS

S-Glutathionylation Impairs Signal Transducer and Activator of Transcription 3 Activation and Signaling

(2008) Yi Xie et al.   ENDOCRINOLOGY

Targeting STAT3 in cancer: how successful are we?

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

Novel signal transducer and activator of transcription 3 (STAT3) mutations, reduced TH17 cell numbers, and variably defective STAT3 phosphorylation in hyper-IgE syndrome

(2008) Ellen D. Renner et al.   JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY

Twist Is Transcriptionally Induced by Activation of STAT3 and Mediates STAT3 Oncogenic Function

(2008) George Z. Cheng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Deficiency of Th17 cells in hyper IgE syndrome due to mutations inSTAT3

(2008) Cindy S. Ma et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Mutations inSTAT3andIL12RB1impair the development of human IL-17–producing T cells

(2008) Ludovic de Beaucoudrey et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Novel and recurrent STAT3 mutations in hyper-IgE syndrome patients from different ethnic groups

(2008) Hong Jiao et al.   MOLECULAR IMMUNOLOGY

Somatic mutations affect key pathways in lung adenocarcinoma

(2008) Li Ding et al.   NATURE

Impaired TH17 cell differentiation in subjects with autosomal dominant hyper-IgE syndrome

(2008) Joshua D. Milner et al.   NATURE

Requirement of histone deacetylase1 (HDAC1) in signal transducer and activator of transcription 3 (STAT3) nucleocytoplasmic distribution

(2008) S. Ray et al.   NUCLEIC ACIDS RESEARCH

Suppression of non-small cell lung tumor development by the let-7 microRNA family

(2008) M. S. Kumar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

ROS-Generating Mitochondrial DNA Mutations Can Regulate Tumor Cell Metastasis

(2008) K. Ishikawa et al.   SCIENCE

Modeling synthetic lethality

(2008) Nolwenn Le Meur et al.   GENOME BIOLOGY

Design, synthesis, and studies of small molecule STAT3 inhibitors

(2007) Deepak Bhasin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS