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Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

Nature medicine, 2019-03, Vol.25 (3), p.403-418

2019

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Genomic landscape of lung adenocarcinoma in East Asians

Nature genetics, 2020-02, Vol.52 (2), p.177-186

2020

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EZH2 as a potential target in cancer therapy

Epigenomics, 2014-06, Vol.6 (3), p.341-351

2014

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Untangling the role of mutant histone H3 in diffuse intrinsic pontine glioma

Nature medicine, 2017-04, Vol.23 (4), p.413-414

Creasy, Caretha L

2017

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The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors

Nature communications, 2015-01, Vol.6 (1), p.6051-6051, Article 6051

2015

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EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2―activating mutations

Nature (London), 2012-12, Vol.492 (7427), p.108-112

2012

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Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors

Clinical cancer research, 2019-12, Vol.25 (24), p.7331-7339

2019

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Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Proceedings of the National Academy of Sciences - PNAS, 2012-02, Vol.109 (8), p.2989-2994

2012

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Efficacy and safety of trametinib in Japanese patients with advanced biliary tract cancers refractory to gemcitabine

Cancer science, 2018-01, Vol.109 (1), p.215-224

2018

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Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer

Oncotarget, 2013-12, Vol.4 (12), p.2419-2429

2013

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The Tumor Suppressor Mst1 Promotes Changes in the Cellular Redox State by Phosphorylation and Inactivation of Peroxiredoxin-1 Protein

The Journal of biological chemistry, 2013-03, Vol.288 (12), p.8762-8771

2013

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Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

ACS medicinal chemistry letters, 2012-12, Vol.3 (12), p.1091-1096

2012

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Identification of hnRNP-A1 as a pharmacodynamic biomarker of type I PRMT inhibition in blood and tumor tissues

Scientific reports, 2020-12, Vol.10 (1), p.22155-22155, Article 22155

2020

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Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML

Cancer discovery, 2019-07, Vol.9 (7), p.872-889

2019

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Neuroprotective Role of the Reaper-Related Serine Protease HtrA2/Omi Revealed by Targeted Deletion in Mice

Molecular and Cellular Biology, 2004-11, Vol.24 (22), p.9848-9862

2004

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A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation

Molecular cancer therapeutics, 2014-12, Vol.13 (12), p.3062-3073

2014

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Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

ACS chemical biology, 2014-03, Vol.9 (3), p.622-629

2014

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The Serine Protease Omi/HtrA2 Regulates Apoptosis by Binding XIAP through a Reaper-like Motif

The Journal of biological chemistry, 2002-01, Vol.277 (1), p.439-444

2002

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Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

ACS medicinal chemistry letters, 2020-02, Vol.11 (2), p.133-140

2020

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ALDH1A1 is a novel EZH2 target gene in epithelial ovarian cancer identified by genome-wide approaches

Cancer prevention research (Philadelphia, Pa.), 2012-03, Vol.5 (3), p.484-491

2012

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A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1

SLAS discovery, 2018-01, Vol.23 (1), p.34-46

2018

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Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens

Journal of biomolecular screening, 2012-12, Vol.17 (10), p.1279-1292

2012

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DYRK3 Dual-specificity Kinase Attenuates Erythropoiesis during Anemia

The Journal of biological chemistry, 2008-12, Vol.283 (52), p.36665-36675

2008

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Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

Genomic landscape of lung adenocarcinoma in East Asians

EZH2 as a potential target in cancer therapy

Untangling the role of mutant histone H3 in diffuse intrinsic pontine glioma

The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2―activating mutations

Phase I Study of the Novel Enhancer of Zeste Homolog 2 (EZH2) Inhibitor GSK2816126 in Patients with Advanced Hematologic and Solid Tumors

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Efficacy and safety of trametinib in Japanese patients with advanced biliary tract cancers refractory to gemcitabine

Loss of tumor suppressor KDM6A amplifies PRC2-regulated transcriptional repression in bladder cancer and can be targeted through inhibition of EZH2

Inhibition of BET bromodomain proteins as a therapeutic approach in prostate cancer

EZH2 Is Required for Germinal Center Formation and Somatic EZH2 Mutations Promote Lymphoid Transformation

The Tumor Suppressor Mst1 Promotes Changes in the Cellular Redox State by Phosphorylation and Inactivation of Peroxiredoxin-1 Protein

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

Identification of hnRNP-A1 as a pharmacodynamic biomarker of type I PRMT inhibition in blood and tumor tissues

Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML

Neuroprotective Role of the Reaper-Related Serine Protease HtrA2/Omi Revealed by Targeted Deletion in Mice

A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation

Long Residence Time Inhibition of EZH2 in Activated Polycomb Repressive Complex 2

The Serine Protease Omi/HtrA2 Regulates Apoptosis by Binding XIAP through a Reaper-like Motif

Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors

ALDH1A1 is a novel EZH2 target gene in epithelial ovarian cancer identified by genome-wide approaches

A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1

Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens

DYRK3 Dual-specificity Kinase Attenuates Erythropoiesis during Anemia

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