ETS transcription factors as emerging drug targets in cancer

Benzothiophenone Derivatives Targeting Mutant Forms of Estrogen Receptor-α in Hormone-Resistant Breast Cancers

(2018) Kriti Singh et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Ewing sarcoma

(2018) Thomas G. P. Grünewald et al.   Nature Reviews Disease Primers

Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer

(2018) Lavinia A. Carabet et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Toxic Colors: The Use of Deep Learning for Predicting Toxicity of Compounds Merely from Their Graphic Images

(2018) Michael Fernandez et al.   Journal of Chemical Information and Modeling

Best Practices of Computer-Aided Drug Discovery: Lessons Learned from the Development of a Preclinical Candidate for Prostate Cancer with a New Mechanism of Action

(2017) Fuqiang Ban et al.   Journal of Chemical Information and Modeling

Pharmacological inhibition of the transcription factor PU.1 in leukemia

(2017) Iléana Antony-Debré et al.   JOURNAL OF CLINICAL INVESTIGATION

ETV4 Facilitates Cell-Cycle Progression in Pancreatic Cells through Transcriptional Regulation of Cyclin D1

(2017) Nikhil Tyagi et al.   MOLECULAR CANCER RESEARCH

ERF mutations reveal a balance of ETS factors controlling prostate oncogenesis

(2017) Rohit Bose et al.   NATURE

Critical assessment of methods of protein structure prediction (CASP)-Round XII

(2017) John Moult et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

ETV6 in hematopoiesis and leukemia predisposition

(2017) Hanno Hock et al.   SEMINARS IN HEMATOLOGY

Prostate-derived Ets factor, an oncogenic driver in breast cancer

(2017) Ashwani K Sood et al.   TUMOR BIOLOGY

Acute lymphoblastic leukemia: a comprehensive review and 2017 update

(2017) T Terwilliger et al.   Blood Cancer Journal

Discovery and characterization of small molecules targeting the DNA-binding ETS domain of ERG in prostate cancer

(2017) Miriam S. Butler et al.   Oncotarget

ESE3 Inhibits Pancreatic Cancer Metastasis by Upregulating E-Cadherin

(2016) Tiansuo Zhao et al.   CANCER RESEARCH

Urine TMPRSS2:ERG Plus PCA3 for Individualized Prostate Cancer Risk Assessment

(2016) Scott A. Tomlins et al.   EUROPEAN UROLOGY

Englerin A Inhibits EWS-FLI1 DNA Binding in Ewing Sarcoma Cells

(2016) Vittorio Caropreso et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Global, regional, and national life expectancy, all-cause mortality, and cause-specific mortality for 249 causes of death, 1980–2015: a systematic analysis for the Global Burden of Disease Study 2015

(2016) Haidong Wang et al.   LANCET

A comprehensive map of molecular drug targets

(2016) Rita Santos et al.   NATURE REVIEWS DRUG DISCOVERY

ELK3 promotes the migration and invasion of liver cancer stem cells by targeting HIF-1α

(2016) Joon Ho Lee et al.   ONCOLOGY REPORTS

Signatures of prostate-derived Ets factor (PDEF) in cancer

(2016) Nitin Mahajan   TUMOR BIOLOGY

‘Acute myeloid leukemia: a comprehensive review and 2016 update’

(2016) I De Kouchkovsky et al.   Blood Cancer Journal

MZF-1/Elk-1 interaction domain as therapeutic target for protein kinase Cα-based triple-negative breast cancer cells

(2016) Chia-Jen Lee et al.   Oncotarget

The ELK3-GATA3 axis orchestrates invasion and metastasis of breast cancer cells in vitro and in vivo

(2016) Sun-Young Kong et al.   Oncotarget

Statins affect ETS1-overexpressing triple-negative breast cancer cells by restoring DUSP4 deficiency

(2016) Hae Hyun Jung et al.   Scientific Reports

Integrative Clinical Genomics of Advanced Prostate Cancer

(2015) Dan Robinson et al.   CELL

The Molecular Taxonomy of Primary Prostate Cancer

(2015) Adam Abeshouse et al.   CELL

ZINC 15 – Ligand Discovery for Everyone

(2015) Teague Sterling et al.   Journal of Chemical Information and Modeling

Knockdown of EHF inhibited the proliferation, invasion and tumorigenesis of ovarian cancer cells

(2015) Zhongping Cheng et al.   MOLECULAR CARCINOGENESIS

The oncogene ERG: a key factor in prostate cancer

(2015) P Adamo et al.   ONCOGENE

The transcription factor GABP selectively binds and activates the mutant TERT promoter in cancer

(2015) R. J. A. Bell et al.   SCIENCE

Tissue-based map of the human proteome

(2015) M. Uhlen et al.   SCIENCE

The role of the transcription factor Ets1 in carcinoma

(2015) Jürgen Dittmer   SEMINARS IN CANCER BIOLOGY

Ecteinascidin 743 Interferes with the Activity of EWS-FLI1 in Ewing Sarcoma Cells

(2015) Patrick J. Grohar et al.   NEOPLASIA

Molecular Pathways: Targeting ETS Gene Fusions in Cancer

(2014) F. Y. Feng et al.   CLINICAL CANCER RESEARCH

Selectively Targeting the DNA-binding Domain of the Androgen Receptor as a Prospective Therapy for Prostate Cancer

(2014) Kush Dalal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Small Molecule That Binds and Inhibits the ETV1 Transcription Factor Oncoprotein

(2014) M. S. Pop et al.   MOLECULAR CANCER THERAPEUTICS

High-risk prostate cancer—classification and therapy

(2014) Albert J. Chang et al.   Nature Reviews Clinical Oncology

ETS1 is a genome-wide effector of RAS/ERK signaling in epithelial cells

(2014) Joshua P. Plotnik et al.   NUCLEIC ACIDS RESEARCH

The ets transcription factor Fli-1 in development, cancer and disease

(2014) Y Li et al.   ONCOGENE

A Small Molecule Inhibitor of ETV1, YK-4-279, Prevents Prostate Cancer Growth and Metastasis in a Mouse Xenograft Model

(2014) Said Rahim et al.   PLoS One

Ablation of the oncogenic transcription factor ERG by deubiquitinase inhibition in prostate cancer

(2014) S. Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Overexpression of ETV4 is associated with poor prognosis in prostate cancer: involvement of uPA/uPAR and MMPs

(2014) Mei Qi et al.   TUMOR BIOLOGY

Elf3 drives β-catenin transactivation and associates with poor prognosis in colorectal cancer

(2014) J-L Wang et al.   Cell Death & Disease

ERG induces taxane resistance in castration-resistant prostate cancer

(2014) Giuseppe Galletti et al.   Nature Communications

Activity of a heptad of transcription factors is associated with stem cell programs and clinical outcome in acute myeloid leukemia

(2013) E. Diffner et al.   BLOOD

Frequent copy number gains at 1q21 and 1q32 are associated with overexpression of the ETS transcription factors ETV3 and ELF3 in breast cancer irrespective of molecular subtypes

(2013) Bárbara Mesquita et al.   BREAST CANCER RESEARCH AND TREATMENT

ETS Transcription Factor ESE1/ELF3 Orchestrates a Positive Feedback Loop That Constitutively Activates NF- B and Drives Prostate Cancer Progression

(2013) N. Longoni et al.   CANCER RESEARCH

ETV1 directs androgen metabolism and confers aggressive prostate cancer in targeted mice and patients

(2013) E. Baena et al.   GENES & DEVELOPMENT

ETV4 promotes metastasis in response to activation of PI3-kinase and Ras signaling in a mouse model of advanced prostate cancer

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

Targeted Therapy for Breast Cancer Prevention

(2013) Petra den Hollander et al.   Frontiers in Oncology

ETV1, 4 and 5: An oncogenic subfamily of ETS transcription factors

(2012) Sangphil Oh et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

ESE3/EHF Controls Epithelial Cell Differentiation and Its Loss Leads to Prostate Tumors with Mesenchymal and Stem-like Features

(2012) D. Albino et al.   CANCER RESEARCH

Integrin-linked kinase as a target for ERG-mediated invasive properties in prostate cancer models

(2012) D. D. Becker-Santos et al.   CARCINOGENESIS

Highly Specific Targeting of the TMPRSS2/ERG Fusion Gene Using Liposomal Nanovectors

(2012) L. Shao et al.   CLINICAL CANCER RESEARCH

Small-molecule screen identifies modulators of EWS/FLI1 target gene expression and cell survival in Ewing's sarcoma

(2012) Aleksandar Boro et al.   INTERNATIONAL JOURNAL OF CANCER

Targeting the DNA-binding activity of the human ERG transcription factor using new heterocyclic dithiophene diamidines

(2012) Raja Nhili et al.   NUCLEIC ACIDS RESEARCH

Drug-mediated inhibition of Fli-1 for the treatment of leukemia

(2012) Y-J Li et al.   Blood Cancer Journal

Expression of Elf-1 and survivin in non-small cell lung cancer and their relationship to intratumoral microvessel density

(2012) Dong-Xia Yang et al.   Chinese Journal of Cancer

Overexpression of ETV4 is oncogenic in prostate cells through promotion of both cell proliferation and epithelial to mesenchymal transition

(2012) A Pellecchia et al.   Oncogenesis

Genomic and Biochemical Insights into the Specificity of ETS Transcription Factors

(2011) Peter C. Hollenhorst et al.   Annual Review of Biochemistry

Promotion and maintenance of leukemia by ERG

(2011) S. Tsuzuki et al.   BLOOD

Mechanistic Rationale for Inhibition of Poly(ADP-Ribose) Polymerase in ETS Gene Fusion-Positive Prostate Cancer

(2011) J. Chad Brenner et al.   CANCER CELL

TMPRSS2-ERG-Mediated Feed-Forward Regulation of Wild-Type ERG in Human Prostate Cancers

(2011) R.-S. Mani et al.   CANCER RESEARCH

ERG dependence distinguishes developmental control of hematopoietic stem cell maintenance from hematopoietic specification

(2011) S. Taoudi et al.   GENES & DEVELOPMENT

Acute myeloid leukemia: A central role for the ETS factor ERG

(2011) Joost H.A. Martens   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Identification of an Inhibitor of the EWS-FLI1 Oncogenic Transcription Factor by High-Throughput Screening

(2011) Patrick J. Grohar et al.   JNCI-Journal of the National Cancer Institute

Multiple roles of the epithelium-specific ETS transcription factor, ESE-1, in development and disease

(2011) Jordan R Oliver et al.   LABORATORY INVESTIGATION

Breast and cervical cancer in 187 countries between 1980 and 2010: a systematic analysis

(2011) Mohammad H Forouzanfar et al.   LANCET

YK-4-279 Inhibits ERG and ETV1 Mediated Prostate Cancer Cell Invasion

(2011) Said Rahim et al.   PLoS One

The relationship between early embryo development and tumourigenesis

(2010) Yanlei Ma et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

The role of PU.1 and GATA-1 transcription factors during normal and leukemogenic hematopoiesis

(2010) P Burda et al.   LEUKEMIA

ERG Is a Megakaryocytic Oncogene

(2009) S. Salek-Ardakani et al.   CANCER RESEARCH

Advances in Ewing's Sarcoma Research: Where Are We Now and What Lies Ahead?

(2009) J. L. Ordonez et al.   CANCER RESEARCH

Ets2 transcription factor, telomerase activity and breast cancer

(2009) Julie M Dwyer et al.   CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY

A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma

(2009) Hayriye V Erkizan et al.   NATURE MEDICINE

E74-like factor 2 transactivates valosin-containing protein gene, a gene involved in cancer growth

(2008) Ying Qiu et al.   EXPERIMENTAL AND MOLECULAR PATHOLOGY

Reduced tumorigenesis in mouse mammary cancer cells following inhibition of Pea3- or Erm-dependent transcription

(2008) V. Firlej et al.   JOURNAL OF CELL SCIENCE

Identification of ETS-like transcription factor 4 as a novel androgen receptor target in prostate cancer cells

(2008) H Makkonen et al.   ONCOGENE