Epigenetic drugs against cancer: an evolving landscape

The journey of resveratrol from yeast to human

(2016) Silvie Timmers et al.   Aging-US

The Class I Hdac Inhibitor Mgcd0103 Induces Cell Cycle Arrest and Apoptosis in Colon Cancer Initiating Cells by Upregulating Dickkopf-1 and Non-Canonical Wnt Signaling

(2015)   Oncotarget

Resveratrol-sulfates provide an intracellular reservoir for generation of parent resveratrol, which induces autophagy in cancer cells

(2014) Catherine Andreadi et al.   Autophagy

Inhibition of lysine-specific demethylase 1 by the acyclic diterpenoid geranylgeranoic acid and its derivatives

(2014) Chiharu Sakane et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

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

shRNA screening identifies JMJD1C as being required for leukemia maintenance

(2014) P. Sroczynska et al.   BLOOD

Anti-Tumoral Effect of the Non-Nucleoside DNMT Inhibitor RG108 in Human Prostate Cancer Cells

(2014) Ines Graca et al.   CURRENT PHARMACEUTICAL DESIGN

Cytostatic and Apoptotic Effects of DNMT and HDAC Inhibitors in Endometrial Cancer Cells

(2014) Shaohua Xu et al.   CURRENT PHARMACEUTICAL DESIGN

Epigenetics and Oncology

(2014) Padmaja Mummaneni et al.   PHARMACOTHERAPY

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

(2014) Ramzi F. Sweis et al.   ACS Medicinal Chemistry Letters

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

(2013) S. R. Daigle et al.   BLOOD

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

Differential effects of garcinol and curcumin on histone and p53 modifications in tumour cells

(2013) Hilary M Collins et al.   BMC CANCER

Anticancer efficacy of cisplatin and trichostatin A or 5-aza-2′-deoxycytidine on ovarian cancer

(2013) F Meng et al.   BRITISH JOURNAL OF CANCER

The promise and failures of epigenetic therapies for cancer treatment

(2013) Pasano Bojang et al.   CANCER TREATMENT REVIEWS

Phase I Study of Panobinostat plus Everolimus in Patients with Relapsed or Refractory Lymphoma

(2013) Y. Oki et al.   CLINICAL CANCER RESEARCH

Phase I Trial of a New Schedule of Romidepsin in Patients with Advanced Cancers

(2013) L. Amiri-Kordestani et al.   CLINICAL CANCER RESEARCH

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP

(2013) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia

(2013) M A Dawson et al.   LEUKEMIA

Chromatin proteins and modifications as drug targets

(2013) Kristian Helin et al.   NATURE

Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases

(2013) Fanny L Cherblanc et al.   Nature Chemical Biology

Histone lysine demethylases as targets for anticancer therapy

(2013) Jonas W. Højfeldt et al.   NATURE REVIEWS DRUG DISCOVERY

DNA Methyltransferase Inhibitor Zebularine Inhibits Human Hepatic Carcinoma Cells Proliferation and Induces Apoptosis

(2013) Kazuaki Nakamura et al.   PLoS One

Resveratrol Inhibits the Growth of Gastric Cancer by Inducing G1 Phase Arrest and Senescence in a Sirt1-Dependent Manner

(2013) Qing Yang 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

5-hydroxymethylcytosine and its potential roles in development and cancer

(2013) Gerd P Pfeifer et al.   Epigenetics & Chromatin

Histone deacetylase inhibition in the treatment of acute myeloid leukemia: the effects of valproic acid on leukemic cells, and the clinical and experimental evidence for combining valproic acid with other antileukemic agents

(2013) Hanne Fredly et al.   Clinical Epigenetics

The class I-specific HDAC inhibitor MS-275 modulates the differentiation potential of mouse embryonic stem cells

(2013) G. Franci et al.   Biology Open

Myelodysplastic syndromes: 2012 update on diagnosis, risk-stratification, and management

(2012) Guillermo Garcia-Manero   AMERICAN JOURNAL OF HEMATOLOGY

Sirtuin activators and inhibitors

(2012) José M. Villalba et al.   BIOFACTORS

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

(2012) William J. Harris 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

DNA methyltransferase inhibitor RG108 and histone deacetylase inhibitors cooperate to enhance NB4 cell differentiation and E-cadherin re-expression by chromatin remodelling

(2012) Jurate Savickiene et al.   CELL BIOLOGY INTERNATIONAL

Highly Ligand Efficient and SelectiveN-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product Psammaplin A

(2012) Matthias G. J. Baud et al.   ChemMedChem

Design, Synthesis, and Biological Evaluation of 2-Aminobenzanilide Derivatives as Potent and Selective HDAC Inhibitors

(2012) Diana A. Stolfa et al.   ChemMedChem

Molecular Pathways: The Complexity of the Epigenome in Cancer and Recent Clinical Advances

(2012) M. Conte et al.   CLINICAL CANCER RESEARCH

Rejuvenating Sirtuins: The Rise of a New Family of Cancer Drug Targets

(2012) Santina Bruzzone et al.   CURRENT PHARMACEUTICAL DESIGN

Decitabine for acute myeloid leukemia

(2012) Peter W Marks   Expert Review of Anticancer Therapy

Garcinol, a Histone Acetyltransferase Inhibitor, Radiosensitizes Cancer Cells by Inhibiting Non-Homologous End Joining

(2012) Takahiro Oike et al.   INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS

Histone Deacetylase Inhibitors: Structure-Based Modeling and Isoform-Selectivity Prediction

(2012) Laura Silvestri et al.   Journal of Chemical Information and Modeling

Trials with ‘epigenetic’ drugs: An update

(2012) Angela Nebbioso et al.   Molecular Oncology

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

(2012) Laurens Kruidenier et al.   NATURE

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

(2012) Michael T. McCabe et al.   NATURE

Targeting Epigenetic Readers in Cancer

(2012) Mark A. Dawson et al.   NEW ENGLAND JOURNAL OF MEDICINE

Characterisation of a Tip60 Specific Inhibitor, NU9056, in Prostate Cancer

(2012) Kelly Coffey et al.   PLoS One

Vorinostat, an HDAC inhibitor attenuates epidermoid squamous cell carcinoma growth by dampening mTOR signaling pathway in a human xenograft murine model

(2012) Deepali Kurundkar et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Chemosensitization of tumors by resveratrol

(2011) Subash C. Gupta et al.   Annals of the New York Academy of Sciences

Resveratrol and cellular mechanisms of cancer prevention

(2011) Yogeshwer Shukla et al.   Annals of the New York Academy of Sciences

Sensitization of tumor cells by targeting histone deacetylases

(2011) Paola Perego et al.   BIOCHEMICAL PHARMACOLOGY

Phase I study of the histone deacetylase inhibitor entinostat in combination with 13-cis retinoic acid in patients with solid tumours

(2011) R Pili et al.   BRITISH JOURNAL OF CANCER

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

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

Combination Therapy with Vidaza and Entinostat Suppresses Tumor Growth and Reprograms the Epigenome in an Orthotopic Lung Cancer Model

(2011) Steven A. Belinsky et al.   CANCER RESEARCH

Nicotinamide Blocks Proliferation and Induces Apoptosis of Chronic Lymphocytic Leukemia Cells through Activation of the p53/miR-34a/SIRT1 Tumor Suppressor Network

(2011) V. Audrito et al.   CANCER RESEARCH

5-Hydroxymethylcytosine Is Strongly Depleted in Human Cancers but Its Levels Do Not Correlate with IDH1 Mutations

(2011) S.-G. Jin et al.   CANCER RESEARCH

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

Epigenetic aberrations during oncogenesis

(2011) Maria Hatziapostolou et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Discovery of curcumin, a component of golden spice, and its miraculous biological activities

(2011) Subash C Gupta et al.   CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY

Resveratrol in cardiovascular disease: what is known from current research?

(2011) Hong Wang et al.   HEART FAILURE REVIEWS

HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

(2011) Omar Khan et al.   IMMUNOLOGY AND CELL BIOLOGY

Recurrent DNMT3A mutations in patients with myelodysplastic syndromes

(2011) M J Walter et al.   LEUKEMIA

LBH-589 (panobinostat) potentiates fludarabine anti-leukemic activity through a JNK- and XIAP-dependent mechanism

(2011) Roberto Rosato et al.   LEUKEMIA RESEARCH

DNA Methyltransferase Inhibitor, Zebularine, Delays Tumor Growth and Induces Apoptosis in a Genetically Engineered Mouse Model of Breast Cancer

(2011) M. Chen et al.   MOLECULAR CANCER THERAPEUTICS

Death Receptor Pathway Activation and Increase of ROS Production by the Triple Epigenetic Inhibitor UVI5008

(2011) A. Nebbioso et al.   MOLECULAR CANCER THERAPEUTICS

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Mutations in DNMT1 cause hereditary sensory neuropathy with dementia and hearing loss

(2011) Christopher J Klein et al.   NATURE GENETICS

Dnmt3a is essential for hematopoietic stem cell differentiation

(2011) Grant A Challen et al.   NATURE GENETICS

Cancer epigenetics reaches mainstream oncology

(2011) Manuel Rodríguez-Paredes et al.   NATURE MEDICINE

Synergistic Interactions between HDAC and Sirtuin Inhibitors in Human Leukemia Cells

(2011) Michele Cea et al.   PLoS One

Role of checkpoint kinase 1 (Chk1) in the mechanisms of resistance to histone deacetylase inhibitors

(2011) J.-H. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Tet Proteins Can Convert 5-Methylcytosine to 5-Formylcytosine and 5-Carboxylcytosine

(2011) S. Ito et al.   SCIENCE

Failure of Hypomethylating Agent–Based Therapy in Myelodysplastic Syndromes

(2011) Tapan M. Kadia et al.   SEMINARS IN ONCOLOGY

Potential beneficial effects of butyrate in intestinal and extraintestinal diseases

(2011) Roberto Berni Canani   WORLD JOURNAL OF GASTROENTEROLOGY

Virtual Ligand Screening of the p300/CBP Histone Acetyltransferase: Identification of a Selective Small Molecule Inhibitor

(2010) Erin M. Bowers et al.   CHEMISTRY & BIOLOGY

Structural studies on human 2-oxoglutarate dependent oxygenases

(2010) Michael A McDonough et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

RNA methylation by Dnmt2 protects transfer RNAs against stress-induced cleavage

(2010) M. Schaefer et al.   GENES & DEVELOPMENT

SRT1720, SRT2183, SRT1460, and Resveratrol Are Not Direct Activators of SIRT1

(2010) Michelle Pacholec et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Protein Lysine Methyltransferase G9a Inhibitors: Design, Synthesis, and Structure Activity Relationships of 2,4-Diamino-7-aminoalkoxy-quinazolines.

(2010) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biological rationale for the use of DNA methyltransferase inhibitors as new strategy for modulation of tumor response to chemotherapy and radiation

(2010) Giovanni L Gravina et al.   Molecular Cancer

The Histone Deacetylase Inhibitor MGCD0103 Has Both Deacetylase and Microtubule Inhibitory Activity

(2010) K. Chia et al.   MOLECULAR PHARMACOLOGY

Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

(2010) Gillian L. Dalgliesh et al.   NATURE

Selective inhibition of BET bromodomains

(2010) Panagis Filippakopoulos et al.   NATURE

DNMT3AMutations in Acute Myeloid Leukemia

(2010) Timothy J. Ley et al.   NEW ENGLAND JOURNAL OF MEDICINE

Histone deacetylase inhibitor induces DNA damage, which normal but not transformed cells can repair

(2010) J.- H. Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sirtuins inhibitors: The approach to affinity and selectivity

(2009) Yana Cen   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors

(2009) Astrid Spannhoff et al.   ChemMedChem

Solving the Dnmt2 enigma

(2009) Matthias Schaefer et al.   CHROMOSOMA

SIRT1 controls circadian clock circuitry and promotes cell survival: a connection with age-related neoplasms

(2009) Brittney Jung-Hynes et al.   FASEB JOURNAL

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

(2009) Feng Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Cell-Active Lysine Specific Demethylase 1-Selective Inhibitors

(2009) Rie Ueda et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Recent progress in the biology and physiology of sirtuins

(2009) Toren Finkel et al.   NATURE

Somatic mutations of the histone H3K27 demethylase gene UTX in human cancer

(2009) Gijs van Haaften et al.   NATURE GENETICS

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

(2009) Yanqi Chang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Curcumin, resveratrol and flavonoids as anti-inflammatory, cyto- and DNA-protective dietary compounds

(2009) Kavita Bisht et al.   TOXICOLOGY

Long-term effects of resveratrol supplementation on suppression of atherogenic lesion formation and cholesterol synthesis in apo E-deficient mice

(2008) Gyeong-Min Do et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Chemical mechanisms of histone lysine and arginine modifications

(2008) Brian C. Smith et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

A Phase I Biological Study of MG98, an Oligodeoxynucleotide Antisense to DNA Methyltransferase 1, in Patients with High-Risk Myelodysplasia and Acute Myeloid Leukemia

(2008) R. B. Klisovic et al.   CLINICAL CANCER RESEARCH

Histone Deacetylase Inhibitor Panobinostat Induces Clinical Responses with Associated Alterations in Gene Expression Profiles in Cutaneous T-Cell Lymphoma

(2008) L. Ellis et al.   CLINICAL CANCER RESEARCH

Resveratrol: A Natural Compound with Pharmacological Potential in Neurodegenerative Diseases

(2008) Héctor I. Rocha-González et al.   CNS Neuroscience & Therapeutics

The potential role of histone deacetylase inhibitors in the treatment of non-small-cell lung cancer

(2008) Cesare Gridelli et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Epi-drugs to fight cancer: From chemistry to cancer treatment, the road ahead

(2008) Antonello Mai et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Suramin: Clinical Uses and Structure-Activity Relationships

(2008) Ross McGeary et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

A new path to the cancer epigenome

(2008) Victoria M Richon   NATURE BIOTECHNOLOGY

Epigenetics in Cancer

(2008) Manel Esteller   NEW ENGLAND JOURNAL OF MEDICINE