Signal transducer and activator of transcription 3 (STAT3): a promising target for anticancer therapy

Ruxolitinib

(2015) C. Campas-Moya   DRUGS OF THE FUTURE

A Novel Small Molecule, LLL12, Inhibits STAT3 Phosphorylation and Activities and Exhibits Potent Growth-Suppressive Activity in Human Cancer Cells

(2015) Li Lin et al.   NEOPLASIA

The IGFR1 inhibitor NVP-AEW541 disrupts a pro-survival and pro-angiogenic IGF-STAT3-HIF1 pathway in human glioblastoma cells

(2010) Marzia B. Gariboldi et al.   BIOCHEMICAL PHARMACOLOGY

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

(2010) Xiaolei Zhang et al.   BIOCHEMICAL PHARMACOLOGY

Oleanane triterpenoid CDDO-Me induces apoptosis in multidrug resistant osteosarcoma cells through inhibition of Stat3 pathway

(2010) Keinosuke Ryu et al.   BMC CANCER

STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma

(2010) A Horiguchi et al.   BRITISH JOURNAL OF CANCER

Statins suppress interleukin-6-induced monocyte chemo-attractant protein-1 by inhibiting Janus kinase/signal transducers and activators of transcription pathways in human vascular endothelial cells

(2010) Michihisa Jougasaki et al.   BRITISH JOURNAL OF PHARMACOLOGY

Role of STAT3 decoy oligodeoxynucleotides on cell invasion and chemosensitivity in human epithelial ovarian cancer cells

(2010) Xiaolei Zhang et al.   CANCER GENETICS AND CYTOGENETICS

Novel STAT3 Phosphorylation Inhibitors Exhibit Potent Growth-Suppressive Activity in Pancreatic and Breast Cancer Cells

(2010) L. Lin et al.   CANCER RESEARCH

NCX-4016, a nitro-derivative of aspirin, inhibits EGFR and STAT3 signaling and mdulates Bcl-2 proteins in cisplatin-resistant human ovarian cancer cells and xenografts

(2010) Karuppaiyah Selvendiran et al.   CELL CYCLE

An unnatural amino acid that mimics phosphotyrosine

(2010) Jingyan Ge et al.   CHEMICAL COMMUNICATIONS

Epigenetic therapy of lymphoma using histone deacetylase inhibitors

(2010) Maribel Cotto et al.   Clinical & Translational Oncology

Activity of deacetylase inhibitor panobinostat (LBH589) in cutaneous T-cell lymphoma models: Defining molecular mechanisms of resistance

(2010) Wenlin Shao et al.   INTERNATIONAL JOURNAL OF CANCER

Fluacrypyrim, a novel STAT3 activation inhibitor, induces cell cycle arrest and apoptosis in cancer cells harboring constitutively-active STAT3

(2010) Zu-Yin Yu et al.   INTERNATIONAL JOURNAL OF CANCER

Inhibition of Epidermal Growth Factor Receptor Signaling bySaussurea involucrata, a Rare Traditional Chinese Medicinal Herb, in Human Hormone-Resistant Prostate Cancer PC-3 Cells

(2010) Tzong-Der Way et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

Meteorin promotes the formation of GFAP-positive glia via activation of the Jak-STAT3 pathway

(2010) H. S. Lee et al.   JOURNAL OF CELL SCIENCE

Discovery of 5-Chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a Novel Inhibitor of the Jak/Stat Pathway

(2010) Stephanos Ioannidis et al.   JOURNAL OF MEDICINAL CHEMISTRY

The gold compound auranofin induces apoptosis of human multiple myeloma cells through both down-regulation of STAT3 and inhibition of NF-κB activity

(2010) Aya Nakaya et al.   LEUKEMIA RESEARCH

The Intracellular Delivery of a Recombinant Peptide Derived from the Acidic Domain of PIAS3 Inhibits STAT3 Transactivation and Induces Tumor Cell Death

(2010) C. Borghouts et al.   MOLECULAR CANCER RESEARCH

5-Hydroxy-2-Methyl-1,4-Naphthoquinone, a Vitamin K3 Analogue, Suppresses STAT3 Activation Pathway through Induction of Protein Tyrosine Phosphatase, SHP-1: Potential Role in Chemosensitization

(2010) S. K. Sandur et al.   MOLECULAR CANCER RESEARCH

ZD6474, a Multitargeted Inhibitor for Receptor Tyrosine Kinases, Suppresses Growth of Gliomas Expressing an Epidermal Growth Factor Receptor Mutant, EGFRvIII, in the Brain

(2010) Jia-Jean Yiin et al.   MOLECULAR CANCER THERAPEUTICS

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

STAT3 Activation of miR-21 and miR-181b-1 via PTEN and CYLD Are Part of the Epigenetic Switch Linking Inflammation to Cancer

(2010) Dimitrios Iliopoulos et al.   MOLECULAR CELL

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

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

Naphtho[1,2-b]furan-4,5-dione disrupts Janus kinase-2 and induces apoptosis in breast cancer MDA-MB-231 cells

(2010) Kuei-Li Lin et al.   TOXICOLOGY IN VITRO

Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity

(2010) Dae-Seop Shin et al.   MedChemComm

Identification of Purine-Scaffold Small-Molecule Inhibitors of Stat3 Activation by QSAR Studies

(2010) Vijay M. Shahani et al.   ACS Medicinal Chemistry Letters

Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors

(2010) Jianyong Chen et al.   ACS Medicinal Chemistry Letters

Identification of a New Series of STAT3 Inhibitors by Virtual Screening

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

Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway

(2010) Xiaomei Ren et al.   ACS Medicinal Chemistry Letters

Cholinergic agonists regulate JAK2/STAT3 signaling to suppress endothelial cell activation

(2009) Prodyot K. Chatterjee et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

SCH66336, inhibitor of protein farnesylation, blocks signal transducer and activators of transcription 3 signaling in lung cancer and interacts with a small molecule inhibitor of epidermal growth factor receptor/human epidermal growth factor receptor 2

(2009) Afshin Dowlati et al.   ANTI-CANCER DRUGS

Novel high-throughput screening system for identifying STAT3–SH2 antagonists

(2009) Yutaka Uehara et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Inhibition of the JAK-STAT3 pathway by andrographolide enhances chemosensitivity of cancer cells to doxorubicin

(2009) Jing Zhou et al.   BIOCHEMICAL PHARMACOLOGY

Interaction of the chemopreventive agent resveratrol and its metabolite, piceatannol, with model membranes

(2009) Olga Wesołowska et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

A novel non-phosphorylated potential antitumoral peptide inhibits STAT3 biological activity☆

(2009) Jennifer Dourlat et al.   BIOCHIMIE

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

(2009) Christopher J. Burns et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors

(2009) Cindy Gomez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

LLL-3 inhibits STAT3 activity, suppresses glioblastoma cell growth and prolongs survival in a mouse glioblastoma model

(2009) B Fuh et al.   BRITISH JOURNAL OF CANCER

MS-1020 is a novel small molecule that selectively inhibits JAK3 activity

(2009) Byung-Hak Kim et al.   BRITISH JOURNAL OF HAEMATOLOGY

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

17-Hydroxy-jolkinolide B Inhibits Signal Transducers and Activators of Transcription 3 Signaling by Covalently Cross-Linking Janus Kinases and Induces Apoptosis of Human Cancer Cells

(2009) Y. Wang et al.   CANCER RESEARCH

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

Enalapril Alters Expression of Key Growth Factors in Experimental Diabetic Retinopathy

(2009) Hyun Woong Kim et al.   CURRENT EYE RESEARCH

Triptolide downregulates Rac1 and the JAK/STAT3 pathway and inhibits colitis-related colon cancer progression

(2009) Zhipeng Wang et al.   EXPERIMENTAL AND MOLECULAR MEDICINE

Satraplatin: leading the new generation of oral platinum agents

(2009) Ashish Bhargava et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Efficient killing of SW480 colon carcinoma cells by a signal transducer and activator of transcription (STAT) 3 hairpin decoy oligodeoxynucleotide - interference with interferon-γ-STAT1-mediated killing

(2009) Ali Tadlaoui Hbibi et al.   FEBS Journal

Manumycin inhibits STAT3, telomerase activity, and growth of glioma cells by elevating intracellular reactive oxygen species generation

(2009) Deobrat Dixit et al.   FREE RADICAL BIOLOGY AND MEDICINE

The novel HSP90 inhibitor STA-1474 exhibits biologic activity against osteosarcoma cell lines

(2009) Jennifer K. McCleese et al.   INTERNATIONAL JOURNAL OF CANCER

Rosmanol Potently Inhibits Lipopolysaccharide-Induced iNOS and COX-2 Expression through Downregulating MAPK, NF-κB, STAT3 and C/EBP Signaling Pathways

(2009) Ching-Shu Lai et al.   JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

12-O-Tetradecanoylphorbol-13-acetate Inhibits Melanoma Growth by Inactivation of STAT3 through Protein Kinase C-activated Tyrosine Phosphatase(s)

(2009) Masahiro Oka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure−Affinity Relationships of Glutamine Mimics Incorporated into Phosphopeptides Targeted to the SH2 Domain of Signal Transducer and Activator of Transcription 3

(2009) Pijus K. Mandal et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Deguelin suppresses cell proliferation via the inhibition of survivin expression and STAT3 phosphorylation in HTLV-1-transformed T cells

(2009) Shigeki Ito et al.   LEUKEMIA RESEARCH

A redox-silent analogue of tocotrienol acts as a potential cytotoxic agent against human mesothelioma cells

(2009) Korehito Kashiwagi et al.   LIFE SCIENCES

Bortezomib up-regulates activated signal transducer and activator of transcription-3 and synergizes with inhibitors of signal transducer and activator of transcription-3 to promote head and neck squamous cell carcinoma cell death

(2009) C. Li et al.   MOLECULAR CANCER THERAPEUTICS

Sorafenib, a dual Raf kinase/vascular endothelial growth factor receptor inhibitor has significant anti-myeloma activity and synergizes with common anti-myeloma drugs

(2009) V Ramakrishnan et al.   ONCOGENE

Synthesis of Phosphatase-Stable, Cell-Permeable Peptidomimetic Prodrugs That Target the SH2 Domain of Stat3

(2009) Pijus K. Mandal et al.   ORGANIC LETTERS

Anti-Cancer, Anti-Diabetic and Other Pharmacologic and Biological Activities of Penta-Galloyl-Glucose

(2009) Jinhui Zhang et al.   PHARMACEUTICAL RESEARCH

Chemical Probes that Competitively and Selectively Inhibit Stat3 Activation

(2009) Xuejun Xu et al.   PLoS One

Therapeutic potential of JAK2 inhibitors

(2009) S. Verstovsek   Hematology-American Society of Hematology Education Program

Discovery of the catechol structural moiety as a Stat3 SH2 domain inhibitor by virtual screening

(2008) Wenshan Hao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3

(2008) E. A. Nelson et al.   BLOOD

Cryptotanshinone Inhibits Constitutive Signal Transducer and Activator of Transcription 3 Function through Blocking the Dimerization in DU145 Prostate Cancer Cells

(2008) D.-S. Shin et al.   CANCER RESEARCH

STAT3 as a target for inducing apoptosis in solid and hematological tumors

(2008) Khandaker Al Zaid Siddiquee et al.   CELL RESEARCH

Targeting Protein-Protein Interactions: Suppression of Stat3 Dimerization with Rationally Designed Small-Molecule, Nonpeptidic SH2 Domain Binders

(2008) Patrick T. Gunning et al.   CHEMBIOCHEM

Molecular Approaches towards the Inhibition of the Signal Transducer and Activator of Transcription 3 (Stat3) Protein

(2008) Steven Fletcher et al.   ChemMedChem

STAT 3 as a Target for Cancer Drug Discovery

(2008) Luca Costantino et al.   CURRENT MEDICINAL CHEMISTRY

Targeting STAT3 in cancer: how successful are we?

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

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

TG101348, a JAK2-selective antagonist, inhibits primary hematopoietic cells derived from myeloproliferative disorder patients with JAK2V617F, MPLW515K or JAK2 exon 12 mutations as well as mutation negative patients

(2008) T L Lasho et al.   LEUKEMIA

Monomeric Recombinant Peptide Aptamers Are Required for Efficient Intracellular Uptake and Target Inhibition

(2008) C. Borghouts et al.   MOLECULAR CANCER RESEARCH

Penta-1,2,3,4,6-O-galloyl- -D-glucose induces p53 and inhibits STAT3 in prostate cancer cells in vitro and suppresses prostate xenograft tumor growth in vivo

(2008) H. Hu et al.   MOLECULAR CANCER THERAPEUTICS

A small-molecule compound identified through a cell-based screening inhibits JAK/STAT pathway signaling in human cancer cells

(2008) B. H. Kim et al.   MOLECULAR CANCER THERAPEUTICS

Design, synthesis, and studies of small molecule STAT3 inhibitors

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