Predictive biomarkers and potential drug combinations of epi-drugs in cancer therapy

EZH2 Inhibition Sensitizes CARM1-High, Homologous Recombination Proficient Ovarian Cancers to PARP Inhibition

(2020) Sergey Karakashev et al.   CANCER CELL

5-Azacitidine Induces NOXA to Prime AML Cells for Venetoclax-mediated Apoptosis.

(2020) Sha Jin et al.   CLINICAL CANCER RESEARCH

Revealing the epigenetic effect of temozolomide on glioblastoma cell lines in therapeutic conditions

(2020) Agnieszka Belter et al.   PLoS One

Enasidenib in patients with mutant IDH2 myelodysplastic syndromes: a phase 1 subgroup analysis of the multicentre, AG221-C-001 trial

(2020) Eytan M Stein et al.   Lancet Haematology

Tazemetostat: First Approval

(2020) Sheridan M. Hoy   DRUGS

EZH2 deficient T-cell acute lymphoblastic leukemia is sensitized to CHK1 inhibition through enhanced replication stress

(2020) Theresa Elizabeth Leon et al.   Cancer Discovery

xCT Inhibition Increases Sensitivity to Vorinostat in a ROS-Dependent Manner

(2020) Keiko Miyamoto et al.   Cancers

Single-cell transcriptomics reveals regulators underlying immune cell diversity and immune subtypes associated with prognosis in nasopharyngeal carcinoma

(2020) Yu-Pei Chen et al.   CELL RESEARCH

Kinetics and mechanisms of mitotic inheritance of DNA methylation and their roles in aging-associated methylome deterioration

(2020) Xuan Ming et al.   CELL RESEARCH

EZH2: a novel target for cancer treatment

(2020) Ran Duan et al.   Journal of Hematology & Oncology

Imprecise DNMT1 activity coupled with neighbor-guided correction enables robust yet flexible epigenetic inheritance

(2020) Qiujun Wang et al.   NATURE GENETICS

RNA is essential for PRC2 chromatin occupancy and function in human pluripotent stem cells

(2020) Yicheng Long et al.   NATURE GENETICS

PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity

(2020) Hyungsoo Kim et al.   Science Translational Medicine

Immunotargeting of the xCT Cystine/Glutamate Antiporter Potentiates the Efficacy of HER2-Targeted Immunotherapies in Breast Cancer

(2020) Laura Conti et al.   Cancer Immunology Research

Decitabine/Cedazuridine: First Approval

(2020) Sohita Dhillon   DRUGS

Natural Products Extracted from Fungal Species as New Potential Anti-Cancer Drugs: A Structure-Based Drug Repurposing Approach Targeting HDAC7

(2020) Annalisa Maruca et al.   MOLECULES

Histone demethylase KDM6A directly senses oxygen to control chromatin and cell fate

(2019) Abhishek A. Chakraborty et al.   SCIENCE

LSD1 inhibition by tranylcypromine derivatives interferes with GFI1-mediated repression of PU.1 target genes and induces differentiation in AML

(2019) Jessica Barth et al.   LEUKEMIA

HDAC inhibitors tested in phase III trial

(2019) Diana Romero   Nature Reviews Clinical Oncology

Synergistic antitumor activity of artesunate and HDAC inhibitors through elevating heme synthesis via synergistic upregulation of ALAS1 expression

(2019) Cai-Ping Chen et al.   Acta Pharmaceutica Sinica B

M-TAP Dance: Targeting PRMT1 and PRMT5 Family Members to Push Cancer Cells Over the Edge

(2019) Nivine Srour et al.   CANCER CELL

HDAC Inhibition Enhances the In Vivo Efficacy of MEK Inhibitor Therapy in Uveal Melanoma

(2019) Fernanda Faião-Flores et al.   CLINICAL CANCER RESEARCH

Anti-tumor Activity and Epigenetic Impact of the Polyphenol Oleacein in Multiple Myeloma

(2019) Giada Juli et al.   Cancers

An Evolutionarily Conserved Function of Polycomb Silences the MHC Class I Antigen Presentation Pathway and Enables Immune Evasion in Cancer

(2019) Marian L. Burr et al.   CANCER CELL

Phase 1 study of the novel enhancer of zeste homolog 2 (EZH2) inhibitor GSK2816126 in patients with advanced hematological and solid tumors

(2019) Timothy A. Yap et al.   CLINICAL CANCER RESEARCH

Combining epigenetic drugs with other therapies for solid tumours — past lessons and future promise

(2019) Daphné Morel et al.   Nature Reviews Clinical Oncology

Regulation of PRMT5–MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

(2019) Shatha AbuHammad et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Re-programing Chromatin with a Bifunctional LSD1/HDAC Inhibitor Induces Therapeutic Differentiation in DIPG

(2019) Jamie N. Anastas et al.   CANCER CELL

Pre-clinical activity of combined LSD1 and mTORC1 inhibition in MLL-translocated acute myeloid leukaemia

(2019) Gauri Deb et al.   LEUKEMIA

EZH2 targeting reduces medulloblastoma growth through epigenetic reactivation of the BAI1/p53 tumor suppressor pathway

(2019) Hanwen Zhang et al.   ONCOGENE

Organic Cation Transporters in Health and Disease

(2019) Hermann Koepsell   PHARMACOLOGICAL REVIEWS

The timeline of epigenetic drug discovery: from reality to dreams

(2019) A. Ganesan et al.   Clinical Epigenetics

Epigenetic restriction of Hippo signaling by MORC2 underlies stemness of hepatocellular carcinoma cells

(2018) Tao Wang et al.   CELL DEATH AND DIFFERENTIATION

Enhancer of zeste homolog 2 (EZH2) inhibitors

(2018) Nitya Gulati et al.   LEUKEMIA & LYMPHOMA

DNA methyltransferase 3A isoform b contributes to repressing E-cadherin through cooperation of DNA methylation and H3K27/H3K9 methylation in EMT-related metastasis of gastric cancer

(2018) He Cui et al.   ONCOGENE

The past and presence of gene targeting: from chemicals and DNA via proteins to RNA

(2018) T. M. Geel et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing

(2018) Sarah V. Gerhart et al.   Scientific Reports

Modulation of EZH2 expression in T cells improves efficacy of anti–CTLA-4 therapy

(2018) Sangeeta Goswami et al.   JOURNAL OF CLINICAL INVESTIGATION

Rottlerin inhibits cell growth and invasion via down-regulation of EZH2 in prostate cancer

(2018) Nana Zheng et al.   CELL CYCLE

Integrative Proteomic Profiling Reveals PRC2-Dependent Epigenetic Crosstalk Maintains Ground-State Pluripotency

(2018) Guido van Mierlo et al.   Cell Stem Cell

Six Years (2012–2018) of Researches on Catalytic EZH2 Inhibitors: The Boom of the 2‐Pyridone Compounds

(2018) Rossella Fioravanti et al.   CHEMICAL RECORD

Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-trans retinoic acid in acute myeloid leukemia across subtypes

(2018) Kimberly N. Smitheman et al.   HAEMATOLOGICA

LncRNA and mRNA signatures associated with neoadjuvant chemoradiotherapy downstaging effects in rectal cancer

(2018) Ning Li et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Venetoclax with decitabine or azacitidine for AML

(2018) Manjulika Das   LANCET ONCOLOGY

Pre-emptive azacitidine for relapse prevention in acute myeloid leukaemia

(2018) Fernando Ramos   LANCET ONCOLOGY

Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors

(2017) Yue-Yang Ji et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of coexistence of BRAF V600E mutation and EZH2 gain specifically in melanoma as a promising target for combination therapy

(2017) Huan Yu et al.   Journal of Translational Medicine

Combination Targeted Therapy to Disrupt Aberrant Oncogenic Signaling and Reverse Epigenetic Dysfunction in IDH2 - and TET2 -Mutant Acute Myeloid Leukemia

(2017) Alan H. Shih et al.   Cancer Discovery

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

Epigenetic Homogeneity Within Colorectal Tumors Predicts Shorter Relapse-Free and Overall Survival Times for Patients With Locoregional Cancer

(2016) Anna Martínez-Cardús et al.   GASTROENTEROLOGY

OCT2 demethylation cracks open oxaliplatin resistance

(2016) Andrea Aguilar   Nature Reviews Nephrology

Anti-cancer effects of curcumin on lung cancer through the inhibition of EZH2 and NOTCH1

(2016) Guo-Qing Wu et al.   Oncotarget

Altering the Course of Small Cell Lung Cancer: Targeting Cancer Stem Cells via LSD1 Inhibition

(2015) C. Allison Stewart et al.   CANCER CELL

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

(2015) Helai P. Mohammad et al.   CANCER CELL

The Hedgehog pathway as targetable vulnerability with 5-azacytidine in myelodysplastic syndrome and acute myeloid leukemia

(2015) Raoul Tibes et al.   Journal of Hematology & Oncology

Vorinostat in patients with advanced malignant pleural mesothelioma who have progressed on previous chemotherapy (VANTAGE-014): a phase 3, double-blind, randomised, placebo-controlled trial

(2015) Lee M Krug et al.   LANCET ONCOLOGY

The Ezh2 polycomb group protein drives an aggressive phenotype in melanoma cancer stem cells and is a target of diet derived sulforaphane

(2015) Matthew L. Fisher et al.   MOLECULAR CARCINOGENESIS

Curcumin Reactivates Silenced Tumor Suppressor Gene RARβ by Reducing DNA Methylation

(2015) Apei Jiang et al.   PHYTOTHERAPY RESEARCH

A New Epigenetic Mechanism of Temozolomide Action in Glioma Cells

(2015) Anna-Maria Barciszewska et al.   PLoS One

Panobinostat Approved for Multiple Myeloma

(2015)   Cancer Discovery

Lysine Demethylase KDM4A Associates with Translation Machinery and Regulates Protein Synthesis

(2015) C. Van Rechem et al.   Cancer Discovery

Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors

(2014) Jimin Woo et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Abstract LB-212: Mcl-1 and FBW7 control a dominant survival pathway underlying HDAC and Bcl-2 inhibitor synergy in squamous cell carcinoma.

(2014) Lei He et al.   CANCER RESEARCH

Akt-Dependent Metabolic Reprogramming Regulates Tumor Cell Histone Acetylation

(2014) Joyce V. Lee et al.   Cell Metabolism

The Histone Deacetylase Inhibitor Abexinostat Induces Cancer Stem Cells Differentiation in Breast Cancer with Low Xist Expression

(2013) M. A. Salvador et al.   CLINICAL CANCER RESEARCH

Lysine-specific demethylase 1 is a therapeutic target for fetal hemoglobin induction

(2013) Lihong Shi et al.   NATURE MEDICINE

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

(2013) S. K. Knutson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The therapeutic effect of histone deacetylase inhibitor PCI-24781 on gallbladder carcinoma in BK5.erbB2 mice

(2012) Takuya Kitamura et al.   JOURNAL OF HEPATOLOGY

Epithelioid sarcoma is associated with a high percentage of SMARCB1 deletions

(2012) Lisa M Sullivan et al.   MODERN PATHOLOGY

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

(2012) Michael T. McCabe et al.   NATURE

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Improved Survival with MEK Inhibition in BRAF-Mutated Melanoma

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Epigenetic CpG Demethylation of the Promoter and Reactivation of the Expression of Neurog1 by Curcumin in Prostate LNCaP Cells

(2011) Limin Shu et al.   AAPS Journal

Aberrant Epigenetic Landscape in Cancer: How Cellular Identity Goes Awry

(2010) María Berdasco et al.   DEVELOPMENTAL CELL

Signaling Kinase AMPK Activates Stress-Promoted Transcription via Histone H2B Phosphorylation

(2010) D. Bungard et al.   SCIENCE

Loss of INI1 Expression is Characteristic of Both Conventional and Proximal-type Epithelioid Sarcoma

(2009) Jason L. Hornick et al.   AMERICAN JOURNAL OF SURGICAL PATHOLOGY

Combining PCI-24781, a Novel Histone Deacetylase Inhibitor, with Chemotherapy for the Treatment of Soft Tissue Sarcoma

(2009) G. Lopez et al.   CLINICAL CANCER RESEARCH

PCI-24781 Induces Caspase and Reactive Oxygen Species-Dependent Apoptosis Through NF- B Mechanisms and Is Synergistic with Bortezomib in Lymphoma Cells

(2009) S. Bhalla et al.   CLINICAL CANCER RESEARCH

Modulation of gene methylation by genistein or lycopene in breast cancer cells

(2008) Audrey King-Batoon et al.   ENVIRONMENTAL AND MOLECULAR MUTAGENESIS