Clinical advances in targeting epigenetics for cancer therapy

A Phase 2a Study of the LSD1 Inhibitor Img-7289 (bomedemstat) for the Treatment of Myelofibrosis

(2020) Kristen Pettit et al.   BLOOD

Phase 2 Multicenter Study of Tazemetostat, an EZH2 Inhibitor, in Patients with Relapsed or Refractory Follicular Lymphoma

(2020) Franck Morschhauser et al.   BLOOD

A LYSA Phase Ib Study of tazemetostat (EPZ-6438) plus R-CHOP in newly diagnosed Diffuse Large B Cell Lymphoma (DLBCL) patients with poor prognosis features

(2020) Clémentine Sarkozy et al.   CLINICAL CANCER RESEARCH

Make your best BET: The emerging role of BET inhibitor treatment in malignant tumors

(2020) Oliver Bechter et al.   PHARMACOLOGY & THERAPEUTICS

In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor

(2020) Aidan G. Gilmartin et al.   HAEMATOLOGICA

The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer

(2020) Raffaella Soldi et al.   PLoS One

Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer

(2020) R. Vatapalli et al.   Nature Communications

BRD4 Inhibition Enhances Azacitidine Efficacy in Acute Myeloid Leukemia and Myelodysplastic Syndromes

(2019) Fernando Vieira Pericole et al.   Frontiers in Oncology

Targeting NOTCH activation in small cell lung cancer through LSD1 inhibition

(2019) Arnaud Augert et al.   Science Signaling

HDAC inhibitors tested in phase III trial

(2019) Diana Romero   Nature Reviews Clinical Oncology

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

Guadecitabine (SGI-110): an investigational drug for the treatment of myelodysplastic syndrome and acute myeloid leukemia

(2019) Georgina S. Daher-Reyes et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

The emerging role of epigenetic therapeutics in immuno-oncology

(2019) Michael J. Topper et al.   Nature Reviews Clinical Oncology

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

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

1383PDPhase I study of CC-90011 in patients with advanced solid tumours (STs) and relapsed/refractory non-hodgkin lymphoma (R/R NHL)

(2019) A Hollebecque et al.   ANNALS OF ONCOLOGY

Results from a Global Randomized Phase 3 Study of Guadecitabine (G) Vs Treatment Choice (TC) in 815 Patients with Treatment Naïve (TN) AML Unfit for Intensive Chemotherapy (IC) ASTRAL-1 Study: Analysis By Number of Cycles

(2019) Gail J. Roboz et al.   BLOOD

Reduction of Global H3K27me3 Enhances HER2/ErbB2 Targeted Therapy

(2019) Alison Hirukawa et al.   Cell Reports

EZH2 negatively regulates PD-L1 expression in hepatocellular carcinoma

(2019) Gang Xiao et al.   Journal for ImmunoTherapy of Cancer

41OA phase I study of CPI-0610, a bromodomain and extra terminal protein (BET) inhibitor in patients with relapsed or refractory lymphoma

(2018) K A Blum et al.   ANNALS OF ONCOLOGY

Epigenetic Mechanisms Regulating Adaptive Responses to Targeted Kinase Inhibitors in Cancer

(2018) Steven P. Angus et al.   Annual Review of Pharmacology and Toxicology

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

(2018) Eytan M. Stein et al.   BLOOD

LSD1 Ablation Stimulates Anti-tumor Immunity and Enables Checkpoint Blockade

(2018) Wanqiang Sheng et al.   CELL

Low-dose decitabine enhances the effect of PD-1 blockade in colorectal cancer with microsatellite stability by re-modulating the tumor microenvironment

(2018) Ganjun Yu et al.   Cellular & Molecular Immunology

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

(2018) Chong Qin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study

(2018) Antoine Italiano et al.   LANCET ONCOLOGY

Tumor innate immunity primed by specific interferon-stimulated endogenous retroviruses

(2018) Israel Cañadas et al.   NATURE MEDICINE

Nucleosidic DNA demethylating epigenetic drugs – A comprehensive review from discovery to clinic

(2018) Khushboo Agrawal et al.   PHARMACOLOGY & THERAPEUTICS

DNA methyltransferase inhibition upregulates MHC-I to potentiate cytotoxic T lymphocyte responses in breast cancer

(2018) Na Luo et al.   Nature Communications

Abstract 1379: INCB059872, a novel FAD-directed LSD1 Inhibitor, is active in prostate cancer models and impacts prostate cancer stem-like cells

(2018) Gianluca Civenni et al.   CANCER RESEARCH

Uveal melanoma patients (pts) treated with abbv-075 (mivebresib), a pan-inhibitor of bromodomain and extraterminal (BET) proteins: Results from a phase 1 study.

(2018) Sapna Pradyuman Patel et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase ib/2a study of PLX51107, a small molecule BET inhibitor, in subjects with advanced hematological malignancies and solid tumors.

(2018) Amita Patnaik et al.   JOURNAL OF CLINICAL ONCOLOGY

Results of the first-in-human study of ABBV-075 (mivebresib), a pan-inhibitor of bromodomain (BD) and extra terminal (BET) proteins, in patients (pts) with relapsed/refractory (R/R) solid tumors.

(2018) Sarina Anne Piha-Paul et al.   JOURNAL OF CLINICAL ONCOLOGY

First-in-human study of ABBV-075 (mivebresib), a pan-inhibitor of bromodomain and extra terminal (BET) proteins, in patients (pts) with relapsed/refractory (RR) acute myeloid leukemia (AML): Preliminary data.

(2018) Gautam Borthakur et al.   JOURNAL OF CLINICAL ONCOLOGY

Venetoclax combined with decitabine or azacitidine in treatment-naive, elderly patients with acute myeloid leukemia

(2018) Courtney D. DiNardo et al.   BLOOD

Enhanced anti-tumor efficacy of checkpoint inhibitors in combination with the histone deacetylase inhibitor Belinostat in a murine hepatocellular carcinoma model

(2018) Diana Llopiz et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

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

BRD4 and Cancer: going beyond transcriptional regulation

(2018) Benedetta Donati et al.   Molecular Cancer

Efficacy, Safety, and Biomarkers of Response to Azacitidine and Nivolumab in Relapsed/Refractory Acute Myeloid Leukemia: A Non-randomized, Open-label, Phase 2 Study

(2018) Naval Daver et al.   Cancer Discovery

Tranylcypromine in mind (Part I): Review of pharmacology

(2017) Sven Ulrich et al.   EUROPEAN NEUROPSYCHOPHARMACOLOGY

Epigenetic Combination Therapy for Children With Secondary Myelodysplastic Syndrome (MDS)/Acute Myeloid Leukemia (AML) and Concurrent Solid Tumor Relapse

(2017) Chana L. Glasser et al.   JOURNAL OF PEDIATRIC HEMATOLOGY ONCOLOGY

Guadecitabine (SGI-110) in treatment-naive patients with acute myeloid leukaemia: phase 2 results from a multicentre, randomised, phase 1/2 trial

(2017) Hagop M Kantarjian et al.   LANCET ONCOLOGY

Pathways and mechanisms of venetoclax resistance

(2017) Prithviraj Bose et al.   LEUKEMIA & LYMPHOMA

DNMT and HDAC inhibitors induce cryptic transcription start sites encoded in long terminal repeats

(2017) David Brocks et al.   NATURE GENETICS

Histone demethylase LSD1 regulates hematopoietic stem cells homeostasis and protects from death by endotoxic shock

(2017) Jianxun Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lysine-Specific Demethylase 1 (LSD1) Inhibitors as Potential Treatment for Different Types of Cancers

(2017) Ahmed F. Abdel-Magid   ACS Medicinal Chemistry Letters

RVX-297- a novel BD2 selective inhibitor of BET bromodomains

(2016) Olesya A. Kharenko et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment

(2016) Yi C. Zheng et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

(2016) Rishi G. Vaswani et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting EZH2 in cancer

(2016) Kimberly H Kim et al.   NATURE MEDICINE

Targeting the cancer epigenome for therapy

(2016) Peter A. Jones et al.   NATURE REVIEWS GENETICS

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

(2016) Kanak Raina et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

TCPs: privileged scaffolds for identifying potent LSD1 inhibitors for cancer therapy

(2016) Yi-Chao Zheng et al.   Epigenomics

Targeting Chromatin Regulators Inhibits Leukemogenic Gene Expression in NPM1 Mutant Leukemia

(2016) M. W. M. Ku hn et al.   Cancer Discovery

Efficacy and Biological Correlates of Response in a Phase II Study of Venetoclax Monotherapy in Patients with Acute Myelogenous Leukemia

(2016) M. Konopleva et al.   Cancer Discovery

Clinical Response of Carcinomas Harboring the BRD4-NUT Oncoprotein to the Targeted Bromodomain Inhibitor OTX015/MK-8628

(2016) A. Stathis et al.   Cancer Discovery

Histone Lysine Demethylase Inhibitors

(2016) Ashwini Jambhekar et al.   Cold Spring Harbor Perspectives in Medicine

HDACs and HDAC Inhibitors in Cancer Development and Therapy

(2016) Yixuan Li et al.   Cold Spring Harbor Perspectives in Medicine

Combinatorial epigenetic therapy in diffuse large B cell lymphoma pre-clinical models and patients

(2016) Benet Pera et al.   Clinical Epigenetics

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

(2016) Céline Berthon et al.   Lancet Haematology

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

International phase 3 study of azacitidine vs conventional care regimens in older patients with newly diagnosed AML with >30% blasts

(2015) H. Dombret et al.   BLOOD

Ricolinostat (ACY-1215) induced inhibition of aggresome formation accelerates carfilzomib-induced multiple myeloma cell death

(2015) Yuko Mishima et al.   BRITISH JOURNAL OF HAEMATOLOGY

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

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

DNA-Demethylating Agents Target Colorectal Cancer Cells by Inducing Viral Mimicry by Endogenous Transcripts

(2015) David Roulois et al.   CELL

Inhibiting DNA Methylation Causes an Interferon Response in Cancer via dsRNA Including Endogenous Retroviruses

(2015) Katherine B. Chiappinelli et al.   CELL

The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

(2015) M. Boi et al.   CLINICAL CANCER RESEARCH

DNA hypomethylation-mediated activation ofCancer/Testis Antigen 45(CT45) genes is associated with disease progression and reduced survival in epithelial ovarian cancer

(2015) Wa Zhang et al.   Epigenetics

The oncogenic BRD4-NUT chromatin regulator drives aberrant transcription within large topological domains

(2015) Artyom A. Alekseyenko et al.   GENES & DEVELOPMENT

Phase I study of the mTOR inhibitor ridaforolimus and the HDAC inhibitor vorinostat in advanced renal cell carcinoma and other solid tumors

(2015) Matthew Zibelman et al.   INVESTIGATIONAL NEW DRUGS

Vorinostat, a histone deacetylase (HDAC) inhibitor, promotes cell cycle arrest and re-sensitizes rituximab- and chemo-resistant lymphoma cells to chemotherapy agents

(2015) Kai Xue et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Safety and tolerability of guadecitabine (SGI-110) in patients with myelodysplastic syndrome and acute myeloid leukaemia: a multicentre, randomised, dose-escalation phase 1 study

(2015) Jean-Pierre J Issa et al.   LANCET ONCOLOGY

Panobinostat reduces hypoxia-induced cisplatin resistance of non-small cell lung carcinoma cells via HIF-1α destabilization

(2015) Carina Fischer et al.   Molecular Cancer

Loss of BAP1 function leads to EZH2-dependent transformation

(2015) Lindsay M LaFave et al.   NATURE MEDICINE

DNA methylation in small cell lung cancer defines distinct disease subtypes and correlates with high expression of EZH2

(2015) J T Poirier et al.   ONCOGENE

Apicidin inhibits cell growth by downregulating IGF-1R in salivary mucoepidermoid carcinoma cells

(2015) MEE-YOUNG AHN et al.   ONCOLOGY REPORTS

Histone deacetylase 6 promotes growth of glioblastoma through inhibition of SMAD2 signaling

(2015) Shun Li et al.   TUMOR BIOLOGY

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

(2015) Daniel Zingg et al.   Nature Communications

DOT1L: a new therapeutic target for aggressive breast cancer

(2015) Jeong-Yeon Lee et al.   Oncotarget

BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells

(2015) Marie-Magdelaine Coudé et al.   Oncotarget

Decitabine Enhances Lymphocyte Migration and Function and Synergizes with CTLA-4 Blockade in a Murine Ovarian Cancer Model

(2015) L. Wang et al.   Cancer Immunology Research

HDAC Inhibition Upregulates PD-1 Ligands in Melanoma and Augments Immunotherapy with PD-1 Blockade

(2015) D. M. Woods et al.   Cancer Immunology Research

HDAC8, A Potential Therapeutic Target for the Treatment of Malignant Peripheral Nerve Sheath Tumors (MPNST)

(2015) Gonzalo Lopez et al.   PLoS One

Pharmacologic down-regulation of EZH2 suppresses bladder cancer in vitro and in vivo

(2015) Shou-Hung Tang et al.   Oncotarget

mTOR kinase inhibitors synergize with histone deacetylase inhibitors to kill B-cell acute lymphoblastic leukemia cells

(2015) Brandon R. Beagle et al.   Oncotarget

Romidepsin induces cell cycle arrest, apoptosis, histone hyperacetylation and reduces matrix metalloproteinases 2 and 9 expression in bortezomib sensitized non-small cell lung cancer cells

(2014) Selvaraju Karthik et al.   BIOMEDICINE & PHARMACOTHERAPY

Molecular Pathways: Resistance to Kinase Inhibitors and Implications for Therapeutic Strategies

(2014) C. M. Lovly et al.   CLINICAL CANCER RESEARCH

The combination of irreversible EGFR TKIs and SAHA induces apoptosis and autophagy-mediated cell death to overcome acquired resistance in EGFRT790M-mutated lung cancer

(2014) Tae-Gul Lee et al.   INTERNATIONAL JOURNAL OF CANCER

Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening

(2014) Shijie Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma

(2014) S. K. Knutson et al.   MOLECULAR CANCER THERAPEUTICS

Enhancer Malfunction in Cancer

(2014) Hans-Martin Herz et al.   MOLECULAR CELL

Epigenomic alterations define lethal CIMP-positive ependymomas of infancy

(2014) S. C. Mack et al.   NATURE

RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist

(2014) Kevin G. McLure et al.   PLoS One

Erasers of Histone Acetylation: The Histone Deacetylase Enzymes

(2014) E. Seto et al.   Cold Spring Harbor Perspectives in Biology

Mutations in SETD2 and genes affecting histone H3K36 methylation target hemispheric high-grade gliomas

(2013) Adam M. Fontebasso et al.   ACTA NEUROPATHOLOGICA

Romidepsin for the treatment of T-cell lymphomas

(2013) A. L. McGraw   AMERICAN JOURNAL OF HEALTH-SYSTEM PHARMACY

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

EZH2 mutations are frequent and represent an early event in follicular lymphoma

(2013) C. Bodor et al.   BLOOD

p53-dependent and p53-independent anticancer effects of different histone deacetylase inhibitors

(2013) J Sonnemann et al.   BRITISH JOURNAL OF CANCER

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Interplay between the Cancer Genome and Epigenome

(2013) Hui Shen et al.   CELL

Selective HDAC1/HDAC2 Inhibitors Induce Neuroblastoma Differentiation

(2013) Stacey M. Frumm et al.   CHEMISTRY & BIOLOGY

Histone deacetylase inhibitor potentiated the ability of MTOR inhibitor to induce autophagic cell death in Burkitt leukemia/lymphoma

(2013) Li Dong et al.   Journal of Hematology & Oncology

Histone deacetylase 3 as a novel therapeutic target in multiple myeloma

(2013) J Minami et al.   LEUKEMIA

Expression of PD-L1, PD-L2, PD-1 and CTLA4 in myelodysplastic syndromes is enhanced by treatment with hypomethylating agents

(2013) H Yang et al.   LEUKEMIA

Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group

(2013) Mercedes Lobera et al.   Nature Chemical Biology

The Cancer Genome Atlas Pan-Cancer analysis project

(2013) John N Weinstein et al.   NATURE GENETICS

Inhibition of Histone Deacetylase 3 Causes Replication Stress in Cutaneous T Cell Lymphoma

(2013) Christina E. Wells et al.   PLoS One

Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly

(2013) Takayoshi Suzuki et al.   PLoS One

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

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

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

The HDAC inhibitor, MPT0E028, enhances erlotinib-induced cell death in EGFR-TKI-resistant NSCLC cells

(2013) M-C Chen et al.   Cell Death & Disease

Mechanism-Based Epigenetic Chemosensitization Therapy of Diffuse Large B-Cell Lymphoma

(2013) T. Clozel et al.   Cancer Discovery

Aberrant patterns of H3K4 and H3K27 histone lysine methylation occur across subgroups in medulloblastoma

(2012) Adrian M. Dubuc et al.   ACTA NEUROPATHOLOGICA

Concomitant inhibition of DNA methyltransferase and BCL-2 protein function synergistically induce mitochondrial apoptosis in acute myelogenous leukemia cells

(2012) Twee Tsao et al.   ANNALS OF HEMATOLOGY

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

(2012) L. Santo et al.   BLOOD

The Histone Demethylase KDM1A Sustains the Oncogenic Potential of MLL-AF9 Leukemia Stem Cells

(2012) William J. Harris et al.   CANCER CELL

Cancer Genetics and Epigenetics: Two Sides of the Same Coin?

(2012) Jueng Soo You et al.   CANCER CELL

MG98, a Second-Generation DNMT1 Inhibitor, in the Treatment of Advanced Renal Cell Carcinoma

(2012) Robert J. Amato et al.   CANCER INVESTIGATION

A Phase I Pharmacokinetic and Pharmacodynamic Study of CHR-3996, an Oral Class I Selective Histone Deacetylase Inhibitor in Refractory Solid Tumors

(2012) U. Banerji et al.   CLINICAL CANCER RESEARCH

Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

(2012) Guangtao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Multicenter, Randomized, Open-Label, Phase III Trial of Decitabine Versus Patient Choice, With Physician Advice, of Either Supportive Care or Low-Dose Cytarabine for the Treatment of Older Patients With Newly Diagnosed Acute Myeloid Leukemia

(2012) Hagop M. Kantarjian et al.   JOURNAL OF CLINICAL ONCOLOGY

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

(2012) Michael T. McCabe et al.   NATURE

Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

(2012) Tino Schenk et al.   NATURE MEDICINE

Histone deacetylase inhibitors sensitize glioblastoma cells to TRAIL-induced apoptosis by c-myc-mediated downregulation of cFLIP

(2012) A Bangert et al.   ONCOGENE

Class I Histone Deacetylase Inhibitor Entinostat Suppresses Regulatory T Cells and Enhances Immunotherapies in Renal and Prostate Cancer Models

(2012) Li Shen et al.   PLoS One

Discovery and prioritization of somatic mutations in diffuse large B-cell lymphoma (DLBCL) by whole-exome sequencing

(2012) J. G. Lohr et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

(2011) Scott R. Daigle et al.   CANCER CELL

Entinostat for treatment of solid tumors and hematologic malignancies

(2011) Jeffrey Knipstein et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Deep sequencing reveals distinct patterns of DNA methylation in prostate cancer

(2011) J. H. Kim et al.   GENOME RESEARCH

Lysine-specific demethylase 1 is highly expressed in solitary fibrous tumors, synovial sarcomas, rhabdomyosarcomas, desmoplastic small round cell tumors, and malignant peripheral nerve sheath tumors

(2011) Hans-Ulrich Schildhaus et al.   HUMAN PATHOLOGY

Role of androgen receptor and associated lysine-demethylase coregulators, LSD1 and JMJD2A, in localized and advanced human bladder cancer

(2011) Eric C. Kauffman et al.   MOLECULAR CARCINOGENESIS

LSD1 regulates the balance between self-renewal and differentiation in human embryonic stem cells

(2011) Antonio Adamo et al.   NATURE CELL BIOLOGY

Combination Epigenetic Therapy Has Efficacy in Patients with Refractory Advanced Non-Small Cell Lung Cancer

(2011) R. A. Juergens et al.   Cancer Discovery

Leukemic IDH1 and IDH2 Mutations Result in a Hypermethylation Phenotype, Disrupt TET2 Function, and Impair Hematopoietic Differentiation

(2010) Maria E. Figueroa et al.   CANCER CELL

Epigenetic Antagonism between Polycomb and SWI/SNF Complexes during Oncogenic Transformation

(2010) Boris G. Wilson et al.   CANCER CELL

Overexpression of LSD1 contributes to human carcinogenesis through chromatin regulation in various cancers

(2010) Shinya Hayami et al.   INTERNATIONAL JOURNAL OF CANCER

Discovery of 2-(6-{[(6-Fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a Class I Selective Orally Active Histone Deacetylase Inhibitor

(2010) David Moffat et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biochemical, Structural, and Biological Evaluation of Tranylcypromine Derivatives as Inhibitors of Histone Demethylases LSD1 and LSD2

(2010) Claudia Binda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Enhancer of Zeste Homolog 2 Promotes the Proliferation and Invasion of Epithelial Ovarian Cancer Cells

(2010) H. Li et al.   MOLECULAR CANCER RESEARCH

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

Somatic mutations altering EZH2 (Tyr641) in follicular and diffuse large B-cell lymphomas of germinal-center origin

(2010) Ryan D Morin et al.   NATURE GENETICS

Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas

(2010) C. J. Sneeringer et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lysine-Specific Demethylase 1 Is Strongly Expressed in Poorly Differentiated Neuroblastoma: Implications for Therapy

(2009) J. H. Schulte et al.   CANCER RESEARCH

Phase I Study of MG98, an Oligonucleotide Antisense Inhibitor of Human DNA Methyltransferase 1, Given as a 7-Day Infusion in Patients with Advanced Solid Tumors

(2009) R. Plummer et al.   CLINICAL CANCER RESEARCH

Histone Deacetylase 8 in Neuroblastoma Tumorigenesis

(2008) I. Oehme et al.   CLINICAL CANCER RESEARCH

Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine

(2008) Carlo Stresemann et al.   INTERNATIONAL JOURNAL OF CANCER

A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas

(2008) S Balasubramanian et al.   LEUKEMIA

SWI/SNF Mediates Polycomb Eviction and Epigenetic Reprogramming of the INK4b-ARF-INK4a Locus

(2008) S. K. Kia et al.   MOLECULAR AND CELLULAR BIOLOGY