The timeline of epigenetic drug discovery: from reality to dreams

Development of new agents for peripheral T-cell lymphoma

(2019) Yuta Ito et al.   EXPERT OPINION ON BIOLOGICAL THERAPY

Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 (HDAC6) Inhibitors

(2019) Katharina Vögerl et al.   JOURNAL OF MEDICINAL CHEMISTRY

Epigenetic Enzyme Mutations: Role in Tumorigenesis and Molecular Inhibitors

(2019) Mei Han et al.   Frontiers in Oncology

Bromodomains: a new target class for drug development

(2019) Andrea G. Cochran et al.   NATURE REVIEWS DRUG DISCOVERY

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

(2018) Eytan M. Stein et al.   BLOOD

Optimal Management of Histone Deacetylase Inhibitor-Related Adverse Events in Patients With Multiple Myeloma: A Focus on Panobinostat

(2018) Jamie D. Cavenagh et al.   Clinical Lymphoma Myeloma & Leukemia

Epigenetic small molecule modulators of histone and DNA methylation

(2018) Alexander-Thomas Hauser et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Enhancer of zeste homolog 2 (EZH2) inhibitors

(2018) Nitya Gulati et al.   LEUKEMIA & LYMPHOMA

A Quinoline-Based DNA Methyltransferase Inhibitor as a Possible Adjuvant in Osteosarcoma Therapy

(2018) Maria Cristina Manara et al.   MOLECULAR CANCER THERAPEUTICS

Designer epigenome modifiers enable robust and sustained gene silencing in clinically relevant human cells

(2018) Tafadzwa Mlambo et al.   NUCLEIC ACIDS RESEARCH

Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity

(2018) Bertrand Lecointre et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Epigenetic drug discovery: a success story for cofactor interference

(2018) A. Ganesan   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Interplay between long non-coding RNAs and epigenetic machinery: emerging targets in cancer?

(2018) David J. Hanly et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

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

Targeting DNA Methyltranferases in Urological Tumors

(2018) Ângela Marques-Magalhães et al.   Frontiers in Pharmacology

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

(2018) Subhankar Biswas et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Genetics meets DNA methylation in rare diseases

(2018) Guillaume Velasco et al.   CLINICAL GENETICS

Identification of novel quinazoline derivatives as potent antiplasmodial agents

(2018) Anne Bouchut et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Clinical epigenetics: seizing opportunities for translation

(2018) María Berdasco et al.   NATURE REVIEWS GENETICS

Epigenetic drugs: More than meets the eye

(2017) Manel Esteller   Epigenetics

Rational Design of Bisubstrate-Type Analogues as Inhibitors of DNA Methyltransferases in Cancer Cells

(2017) Ludovic Halby et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives

(2017) Gebremedhin S. Hailu et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Epi proColon® 2.0 CE: A Blood-Based Screening Test for Colorectal Cancer

(2017) Yvette N. Lamb et al.   Molecular Diagnosis & Therapy

Uncovering BRD4 hyperphosphorylation associated with cellular transformation in NUT midline carcinoma

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

Highly selective inhibition of histone demethylases by de novo macrocyclic peptides

(2017) Akane Kawamura et al.   Nature Communications

Crystal structures of the mitochondrial deacylase Sirtuin 4 reveal isoform-specific acyl recognition and regulation features

(2017) Martin Pannek et al.   Nature Communications

Epi-drugs in combination with immunotherapy: a new avenue to improve anticancer efficacy

(2017) Roberta Mazzone et al.   Clinical Epigenetics

Epigenetic assays for chemical biology and drug discovery

(2017) Sheraz Gul   Clinical Epigenetics

Epigenetic strategies to reverse drug resistance in heterogeneous multiple myeloma

(2017) Mark E. Issa et al.   Clinical Epigenetics

Epigenetic mechanisms during ageing and neurogenesis as novel therapeutic avenues in human brain disorders

(2017) Raúl Delgado-Morales et al.   Clinical Epigenetics

RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease

(2016) Dean Gilham et al.   ATHEROSCLEROSIS

Histone demethylase LSD1 controls the phenotypic plasticity of cancer cells

(2016) Shinjiro Hino et al.   CANCER SCIENCE

Multitarget Drugs: an Epigenetic Epiphany

(2016) A. Ganesan   ChemMedChem

Combination Epigenetic Therapy in Advanced Breast Cancer with 5-Azacitidine and Entinostat: A Phase II National Cancer Institute/Stand Up to Cancer Study

(2016) Roisin M. Connolly et al.   CLINICAL CANCER RESEARCH

Romidepsin for the treatment of relapsed/refractory cutaneous T-cell lymphoma (mycosis fungoides/Sézary syndrome): Use in a community setting

(2016) Sunil A. Reddy   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

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

Writing of H3K4Me3 overcomes epigenetic silencing in a sustained but context-dependent manner

(2016) David Cano-Rodriguez et al.   Nature Communications

Polycomb repressive complex’s evolutionary conserved function: the role of EZH2 status and cellular background

(2016) Koraljka Gall Trošelj et al.   Clinical Epigenetics

Studying epigenetic complexes and their inhibitors with the proteomics toolbox

(2016) David Weigt et al.   Clinical Epigenetics

Genome-wide epigenomic profiling for biomarker discovery

(2016) René A. M. Dirks et al.   Clinical Epigenetics

Histone acetyltransferases: challenges in targeting bi-substrate enzymes

(2016) Hannah Wapenaar et al.   Clinical Epigenetics

A clinical-molecular update on azanucleoside-based therapy for the treatment of hematologic cancers

(2016) Jeannine Diesch et al.   Clinical Epigenetics

The emerging role of lysine methyltransferase SETD8 in human diseases

(2016) Ciro Milite et al.   Clinical Epigenetics

Epigenetic modulators as therapeutic targets in prostate cancer

(2016) Inês Graça et al.   Clinical Epigenetics

Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy

(2016) Ludovica Morera et al.   Clinical Epigenetics

Epigenetic polypharmacology: from combination therapy to multitargeted drugs

(2016) Angel R. de Lera et al.   Clinical Epigenetics

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

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

Discovery of Chemical Inhibitors of Human Bromodomains

(2015) Guangtao Zhang et al.   CHEMICAL REVIEWS

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

(2015) Jing Lu et al.   CHEMISTRY & BIOLOGY

Advances in the development of histone lysine demethylase inhibitors

(2015) Tamara Maes et al.   CURRENT OPINION IN PHARMACOLOGY

What Do You Mean, “Epigenetic”?

(2015) Carrie Deans et al.   GENETICS

Belinostat in Patients With Relapsed or Refractory Peripheral T-Cell Lymphoma: Results of the Pivotal Phase II BELIEF (CLN-19) Study

(2015) Owen A. O'Connor et al.   JOURNAL OF CLINICAL ONCOLOGY

Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents

(2015) Madhusoodanan Mottamal et al.   MOLECULES

A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

(2015) Elayne Chan-Penebre et al.   Nature Chemical Biology

Structural diversity of the epigenetics pocketome

(2015) Alexandre Cabaye et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Epigenetic therapy for solid tumors: from bench science to clinical trials

(2015) Yen-Yi Juo et al.   Epigenomics

Epigenetic control of HIV-1 post integration latency: implications for therapy

(2015) Amit Kumar et al.   Clinical Epigenetics

What Do You Mean, “Epigenetic”?

(2015) Carrie Deans et al.   GENETICS

Targeting epigenetic regulators for cancer therapy

(2014) Susan Wee et al.   Annals of the New York Academy of Sciences

Dysregulated Class I histone deacetylases are indicators of poor prognosis in multiple myeloma

(2014) Sridurga Mithraprabhu et al.   Epigenetics

Could valproic acid be an effective anticancer agent? The evidence so far

(2014) Seth A Brodie et al.   Expert Review of Anticancer Therapy

Harnessing the potential of epigenetic therapy to target solid tumors

(2014) Nita Ahuja et al.   JOURNAL OF CLINICAL INVESTIGATION

Prolonged Administration of Azacitidine With or Without Entinostat for Myelodysplastic Syndrome and Acute Myeloid Leukemia With Myelodysplasia-Related Changes: Results of the US Leukemia Intergroup Trial E1905

(2014) Thomas Prebet et al.   JOURNAL OF CLINICAL ONCOLOGY

Targeting DNA Methylation with Small Molecules: What’s Next?

(2014) Alexandre Erdmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Selective Inhibitors of Protein Methyltransferases

(2014) H. Ümit Kaniskan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Binding of the histone chaperone ASF1 to the CBP bromodomain promotes histone acetylation

(2014) C. Das et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

DNA Methyltransferase-1 Inhibitors as Epigenetic Therapy for Cancer

(2013) Varinder Singh et al.   CURRENT CANCER DRUG TARGETS

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

(2013) T. Clozel et al.   Cancer Discovery

Transient Low Doses of DNA-Demethylating Agents Exert Durable Antitumor Effects on Hematological and Epithelial Tumor Cells

(2012) Hsing-Chen Tsai et al.   CANCER CELL

Urinary phenylacetylglutamine as dosing biomarker for patients with urea cycle disorders

(2012) M. Mokhtarani et al.   MOLECULAR GENETICS AND METABOLISM

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

Phase 2 trial of romidepsin in patients with peripheral T-cell lymphoma

(2011) R. L. Piekarz et al.   BLOOD

Chromatin higher-order structures and gene regulation

(2011) Guohong Li et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains

(2011) Chun-wa Chung et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Mechanisms of Long Noncoding RNAs

(2011) Kevin C. Wang et al.   MOLECULAR CELL

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

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

Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes

(2010) Gorica Nikoloski et al.   NATURE GENETICS