Epigenetic cancer therapy: rationales, targets and drugs

Genome-wide promoter DNA methylation dynamics of human hematopoietic progenitor cells during differentiation and aging

(2011) M. T. Bocker et al.   BLOOD

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

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

MLL-Rearranged Leukemia Is Dependent on Aberrant H3K79 Methylation by DOT1L

(2011) Kathrin M. Bernt et al.   CANCER CELL

HDACs link the DNA damage response, processing of double-strand breaks and autophagy

(2011) Thomas Robert et al.   NATURE

TET1 and hydroxymethylcytosine in transcription and DNA methylation fidelity

(2011) Kristine Williams et al.   NATURE

Dual functions of Tet1 in transcriptional regulation in mouse embryonic stem cells

(2011) Hao Wu et al.   NATURE

Increased methylation variation in epigenetic domains across cancer types

(2011) Kasper Daniel Hansen et al.   NATURE GENETICS

Variability in transport and biotransformation of cytarabine is associated with its toxicity in peripheral blood mononuclear cells

(2011) Sumit Parmar et al.   PHARMACOGENOMICS

Azacytidine and Decitabine Induce Gene-Specific and Non-Random DNA Demethylation in Human Cancer Cell Lines

(2011) Sabine Hagemann et al.   PLoS One

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

(2011) S. Ito et al.   SCIENCE

Wilms Tumor Chromatin Profiles Highlight Stem Cell Properties and a Renal Developmental Network

(2010) Aviva Presser Aiden et al.   Cell Stem Cell

Vectorial Transport of Nucleoside Analogs from the Apical to the Basolateral Membrane in Double-Transfected Cells Expressing the Human Concentrative Nucleoside Transporter hCNT3 and the Export Pump ABCC4

(2010) M. Rius et al.   DRUG METABOLISM AND DISPOSITION

Pharmacokinetics of gemcitabine in non-small-cell lung cancer patients: impact of the 79A>C cytidine deaminase polymorphism

(2010) Jan Gerard Maring et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Delivery of 5-Azacytidine to Human Cancer Cells by Elaidic Acid Esterification Increases Therapeutic Drug Efficacy

(2010) B. Brueckner et al.   MOLECULAR CANCER THERAPEUTICS

S110, a 5-Aza-2'-Deoxycytidine-Containing Dinucleotide, Is an Effective DNA Methylation Inhibitor In vivo and Can Reduce Tumor Growth

(2010) J. C. Chuang et al.   MOLECULAR CANCER THERAPEUTICS

Natural products as DNA methyltransferase inhibitors: a computer-aided discovery approach

(2010) Jose L. Medina-Franco et al.   MOLECULAR DIVERSITY

Comprehensive methylome map of lineage commitment from haematopoietic progenitors

(2010) Hong Ji et al.   NATURE

Somatic mutations of the histone methyltransferase gene EZH2 in myelodysplastic syndromes

(2010) Gorica Nikoloski et al.   NATURE GENETICS

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

Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

(2010) Thomas Ernst et al.   NATURE GENETICS

As we bring demethylating drugs to the clinic, we better know the DICE being cast

(2010) P M Lizardi   ONCOGENE

Demethylation of a LINE-1 antisense promoter in the cMet locus impairs Met signalling through induction of illegitimate transcription

(2010) B Weber et al.   ONCOGENE

A Comparison of Azacitidine and Decitabine Activities in Acute Myeloid Leukemia Cell Lines

(2010) Paul W. Hollenbach et al.   PLoS One

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

Hypomethylation of a LINE-1 Promoter Activates an Alternate Transcript of the MET Oncogene in Bladders with Cancer

(2010) Erika M. Wolff et al.   PLoS Genetics

Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation

(2009) Dirk Kuck et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Early epigenetic changes and DNA damage do not predict clinical response in an overlapping schedule of 5-azacytidine and entinostat in patients with myeloid malignancies

(2009) T. E. Fandy et al.   BLOOD

Genome-wide Loss-of-Function Screen Reveals an Important Role for the Proteasome in HDAC Inhibitor-Induced Apoptosis

(2009) Susan Fotheringham et al.   CANCER CELL

Targeting DNA Methylation

(2009) J.-P. J. Issa et al.   CLINICAL CANCER RESEARCH

Transport of Nucleoside Analogs Across the Plasma Membrane: A Clue to Understanding Drug-Induced Cytotoxicity

(2009) I. Huber-Ruano et al.   CURRENT DRUG METABOLISM

Phase II Multi-Institutional Trial of the Histone Deacetylase Inhibitor Romidepsin As Monotherapy for Patients With Cutaneous T-Cell Lymphoma

(2009) Richard L. Piekarz et al.   JOURNAL OF CLINICAL ONCOLOGY

Human concentrative nucleoside transporter 1-mediated uptake of 5-azacytidine enhances DNA demethylation

(2009) M. Rius et al.   MOLECULAR CANCER THERAPEUTICS

DNA methylation protects hematopoietic stem cell multipotency from myeloerythroid restriction

(2009) Ann-Marie Bröske et al.   NATURE GENETICS

Human Nucleoside Transporters: Biomarkers for Response to Nucleoside Drugs

(2009) Vijaya L. Damaraju et al.   NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS

Lysine Acetylation Targets Protein Complexes and Co-Regulates Major Cellular Functions

(2009) C. Choudhary et al.   SCIENCE

Genetics and epigenetics: stability and plasticity during cellular differentiation

(2009) Fabio Mohn et al.   TRENDS IN GENETICS

Mechanisms of resistance to 5-aza-2'-deoxycytidine in human cancer cell lines

(2008) T. Qin et al.   BLOOD

Cytidine deaminase genotype and toxicity of cytosine arabinoside therapy in children with acute myeloid leukemia

(2008) Deepika Bhatla et al.   BRITISH JOURNAL OF HAEMATOLOGY

Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine

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

EZH1 Mediates Methylation on Histone H3 Lysine 27 and Complements EZH2 in Maintaining Stem Cell Identity and Executing Pluripotency

(2008) Xiaohua Shen et al.   MOLECULAR CELL

Roles of the EZH2 histone methyltransferase in cancer epigenetics

(2008) Jeffrey A. Simon et al.   MUTATION RESEARCH-FUNDAMENTAL AND MOLECULAR MECHANISMS OF MUTAGENESIS

Is there a code embedded in proteins that is based on post-translational modifications?

(2008) Robert J. Sims et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY