Promises and challenges of anticancer drugs that target the epigenome (Q37962596)

26 August 2017

Promises and challenges of anticancer drugs that target the epigenome (English)

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26 August 2017

Ricky W Johnstone

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author name string

Inge Verbrugge

series ordinal

1

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PubMed ID

22126246

26 August 2017

Michael Bots

series ordinal

3

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26 August 2017

1 October 2011

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26 August 2017

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26 August 2017

3

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26 August 2017

547-565

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26 August 2017

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An operational definition of epigenetics

26 August 2017

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Cancer epigenetics reaches mainstream oncology

21 January 2018

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The epigenomics of cancer

21 January 2018

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21 January 2018

Epigenetics in cancer

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Crystal structure of the nucleosome core particle at 2.8 A resolution

21 January 2018

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Translating the Histone Code

21 January 2018

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DNA methylomes, histone codes and miRNAs: tying it all together

21 January 2018

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DNA methylation patterns and epigenetic memory

21 January 2018

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Baculovirus-mediated expression and characterization of the full-length murine DNA methyltransferase

21 January 2018

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DNA methyltransferases Dnmt3a and Dnmt3b are essential for de novo methylation and mammalian development

21 January 2018

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EUKARYOTIC CYTOSINE METHYLTRANSFERASES

21 January 2018

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Non-CpG methylation is prevalent in embryonic stem cells and may be mediated by DNA methyltransferase 3a.

21 January 2018

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Human DNA methylomes at base resolution show widespread epigenomic differences

21 January 2018

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21 January 2018

The mammalian epigenome

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Conversion of 5-methylcytosine to 5-hydroxymethylcytosine in mammalian DNA by MLL partner TET1

21 January 2018

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Role of Tet proteins in 5mC to 5hmC conversion, ES-cell self-renewal and inner cell mass specification

21 January 2018

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Tet1 and Tet2 regulate 5-hydroxymethylcytosine production and cell lineage specification in mouse embryonic stem cells

21 January 2018

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Tet proteins can convert 5-methylcytosine to 5-formylcytosine and 5-carboxylcytosine

21 January 2018

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TET1 is a DNA-binding protein that modulates DNA methylation and gene transcription via hydroxylation of 5-methylcytosine

21 January 2018

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Active DNA demethylation: many roads lead to Rome.

21 January 2018

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TET genes: new players in DNA demethylation and important determinants for stemness

21 January 2018

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Dynamic regulation of 5-hydroxymethylcytosine in mouse ES cells and during differentiation

21 January 2018

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Genome-wide mapping of 5-hydroxymethylcytosine in embryonic stem cells

21 January 2018

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TET1 and hydroxymethylcytosine in transcription and DNA methylation fidelity

21 January 2018

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

21 January 2018

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Reprogramming towards pluripotency requires AID-dependent DNA demethylation

21 January 2018

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Histone modifications: signalling receptors and potential elements of a heritable epigenetic code

21 January 2018

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Epigenetic modifications and human disease

21 January 2018

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Functions of site-specific histone acetylation and deacetylation

21 January 2018

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Histone acetylation in chromatin structure and transcription

21 January 2018

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Enhanced histone acetylation and transcription: a dynamic perspective

21 January 2018

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The role of chromatin during transcription

21 January 2018

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Histone acetyltransferase complexes: one size doesn't fit all

21 January 2018

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Lysine acetylation targets protein complexes and co-regulates major cellular functions

21 January 2018

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Acetylation and deacetylation of non-histone proteins

21 January 2018

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Inhibitors of NAD+ dependent histone deacetylases (sirtuins).

21 January 2018

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The Rpd3/Hda1 family of lysine deacetylases: from bacteria and yeast to mice and men

21 January 2018

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HDACi--targets beyond chromatin.

21 January 2018

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Histone demethylation mediated by the nuclear amine oxidase homolog LSD1

21 January 2018

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JmjC-domain-containing proteins and histone demethylation

21 January 2018

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Cancer treatment of the future: inhibitors of histone methyltransferases

21 January 2018

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Transcription regulation by histone methylation: interplay between different covalent modifications of the core histone tails

21 January 2018

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The key to development: interpreting the histone code?

21 January 2018

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Differentially expressed genes are marked by histone 3 lysine 9 trimethylation in human cancer cells

21 January 2018

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A bivalent chromatin structure marks key developmental genes in embryonic stem cells

21 January 2018

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Erasing the methyl mark: histone demethylases at the center of cellular differentiation and disease

21 January 2018

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Epigenetic silencing of the myelopoiesis regulator microRNA-223 by the AML1/ETO oncoprotein.

21 January 2018

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MicroRNAs and cancer: past, present, and potential future

21 January 2018

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The epigenetic progenitor origin of human cancer

21 January 2018

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Alterations in DNA methylation in human colon neoplasia

21 January 2018

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Genome-wide hypomethylation in human glioblastomas associated with specific copy number alteration, methylenetetrahydrofolate reductase allele status, and increased proliferation.

21 January 2018

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The history of cancer epigenetics

21 January 2018

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A cohort study of tumoral LINE-1 hypomethylation and prognosis in colon cancer

21 January 2018

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Cancer epigenetics comes of age

21 January 2018

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Molecular targets for epigenetic therapy of cancer

21 January 2018

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Aberrant methylation of p16(INK4a) is an early event in lung cancer and a potential biomarker for early diagnosis

21 January 2018

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DNA methylation and genomic imprinting: insights from cancer into epigenetic mechanisms

21 January 2018

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Elevated Dnmt3a activity promotes polyposis in Apc(Min) mice by relaxing extracellular restraints on Wnt signaling.

21 January 2018

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Dnmt3b promotes tumorigenesis in vivo by gene-specific de novo methylation and transcriptional silencing

21 January 2018

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Deficiency of Mbd2 suppresses intestinal tumorigenesis

21 January 2018

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Cancer cells express aberrant DNMT3B transcripts encoding truncated proteins

21 January 2018

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DNMT3B expression might contribute to CpG island methylator phenotype in colorectal cancer

21 January 2018

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A novel DNMT3B splice variant expressed in tumor and pluripotent cells modulates genomic DNA methylation patterns and displays altered DNA binding.

21 January 2018

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Recurrent DNMT3A mutations in patients with myelodysplastic syndromes

21 January 2018

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Exome sequencing identifies somatic mutations of DNA methyltransferase gene DNMT3A in acute monocytic leukemia

21 January 2018

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DNMT3A Mutations in Acute Myeloid Leukemia

21 January 2018

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Mutation of the DNA methyltransferase (DNMT) 1 gene in human colorectal cancers.

21 January 2018

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Acquired mutations in TET2 are common in myelodysplastic syndromes

21 January 2018

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Impaired hydroxylation of 5-methylcytosine in myeloid cancers with mutant TET2

21 January 2018

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Tet2 loss leads to increased hematopoietic stem cell self-renewal and myeloid transformation

21 January 2018

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TET2 inactivation results in pleiotropic hematopoietic abnormalities in mouse and is a recurrent event during human lymphomagenesis

21 January 2018

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Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation

21 January 2018

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Metabolism unhinged: IDH mutations in cancer.

21 January 2018

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Loss of acetylation at Lys16 and trimethylation at Lys20 of histone H4 is a common hallmark of human cancer

21 January 2018

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Rational combinations using HDAC inhibitors

21 January 2018

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Acetylation inactivates the transcriptional repressor BCL6.

21 January 2018

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CREBBP mutations in relapsed acute lymphoblastic leukaemia

21 January 2018

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Inactivating mutations of acetyltransferase genes in B-cell lymphoma

21 January 2018

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A truncating mutation of HDAC2 in human cancers confers resistance to histone deacetylase inhibition

21 January 2018

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hSIR2(SIRT1) functions as an NAD-dependent p53 deacetylase

21 January 2018

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The SIRT1 deacetylase suppresses intestinal tumorigenesis and colon cancer growth

21 January 2018

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SIRT1: recent lessons from mouse models.

21 January 2018

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Epigenetics in cancer: targeting chromatin modifications

21 January 2018

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The ability of E1A to rescue ras-induced premature senescence and confer transformation relies on inactivation of both p300/CBP and Rb family proteins

21 January 2018

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MOZ and MOZ-CBP cooperate with NF-kappaB to activate transcription from NF-kappaB-dependent promoters.

21 January 2018

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Fusion of the MORF and CBP genes in acute myeloid leukemia with the t(10;16)(q22;p13)

21 January 2018

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The diverse superfamily of lysine acetyltransferases and their roles in leukemia and other diseases

21 January 2018

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Therapeutic application of histone deacetylase inhibitors for central nervous system disorders

21 January 2018

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Role of histone H3 lysine 27 methylation in Polycomb-group silencing

21 January 2018

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EZH2 is a marker of aggressive breast cancer and promotes neoplastic transformation of breast epithelial cells

21 January 2018

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Gene silencing in cancer by histone H3 lysine 27 trimethylation independent of promoter DNA methylation

21 January 2018

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

21 January 2018

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

21 January 2018

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Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation

21 January 2018

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

21 January 2018

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Systematic sequencing of renal carcinoma reveals inactivation of histone modifying genes

21 January 2018

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Inactivating mutations of the histone methyltransferase gene EZH2 in myeloid disorders

21 January 2018

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The histone methyltransferase SETDB1 is recurrently amplified in melanoma and accelerates its onset

21 January 2018

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Differential CARM1 expression in prostate and colorectal cancers

21 January 2018

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Multiple recurrent genetic events converge on control of histone lysine methylation in medulloblastoma

21 January 2018

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Histone demethylase JMJD2B functions as a co-factor of estrogen receptor in breast cancer proliferation and mammary gland development

21 January 2018

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MLL: a histone methyltransferase disrupted in leukemia

21 January 2018

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The molecular biology of mixed lineage leukemia

21 January 2018

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DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis

21 January 2018

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5-Aza-deoxycytidine induces selective degradation of DNA methyltransferase 1 by a proteasomal pathway that requires the KEN box, bromo-adjacent homology domain, and nuclear localization signal

21 January 2018

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5-Azacytidine induced methyltransferase-DNA adducts block DNA replication in vivo.

21 January 2018

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Targeting DNA methylation

21 January 2018

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Safety and efficacy of azacitidine in myelodysplastic syndromes

21 January 2018

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The promises and pitfalls of epigenetic therapies in solid tumours

21 January 2018

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Phase I study of oral azacitidine in myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia

21 January 2018

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The novel DNA methylation inhibitor zebularine is effective against the development of murine T-cell lymphoma

21 January 2018

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Plasma pharmacokinetics, oral bioavailability, and interspecies scaling of the DNA methyltransferase inhibitor, zebularine

21 January 2018

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S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth

21 January 2018

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DNMT1 and DNMT3b cooperate to silence genes in human cancer cells

21 January 2018

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DNMT1 is required to maintain CpG methylation and aberrant gene silencing in human cancer cells

21 January 2018

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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.

21 January 2018

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A phase I biological study of MG98, an oligodeoxynucleotide antisense to DNA methyltransferase 1, in patients with high-risk myelodysplasia and acute myeloid leukemia

21 January 2018

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Histone deacetylase (HDAC) inhibitors in recent clinical trials for cancer therapy.

21 January 2018

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Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes

21 January 2018

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Phase IIb multicenter trial of vorinostat in patients with persistent, progressive, or treatment refractory cutaneous T-cell lymphoma

21 January 2018

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Phase 2 trial of oral vorinostat (suberoylanilide hydroxamic acid, SAHA) for refractory cutaneous T-cell lymphoma (CTCL)

21 January 2018

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Phase II multi-institutional trial of the histone deacetylase inhibitor romidepsin as monotherapy for patients with cutaneous T-cell lymphoma

21 January 2018

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Final results from a multicenter, international, pivotal study of romidepsin in refractory cutaneous T-cell lymphoma

21 January 2018

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Histone deacetylase inhibitor panobinostat induces clinical responses with associated alterations in gene expression profiles in cutaneous T-cell lymphoma

21 January 2018

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

21 January 2018

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Preliminary evidence of disease response to the pan deacetylase inhibitor panobinostat (LBH589) in refractory Hodgkin Lymphoma.

21 January 2018

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A phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumors

21 January 2018

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Vorinostat in solid and hematologic malignancies

21 January 2018

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Multicenter phase II trial of the histone deacetylase inhibitor pyridylmethyl-N-{4-[(2-aminophenyl)-carbamoyl]-benzyl}-carbamate in pretreated metastatic melanoma

21 January 2018

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Clinical and molecular responses in lung cancer patients receiving Romidepsin

21 January 2018

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Vorinostat in advanced prostate cancer patients progressing on prior chemotherapy (National Cancer Institute Trial 6862): trial results and interleukin-6 analysis: a study by the Department of Defense Prostate Cancer Clinical Trial Consortium [...]

21 January 2018

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Vorinostat (NSC# 701852) in patients with relapsed non-small cell lung cancer: a Wisconsin Oncology Network phase II study

21 January 2018

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Histone deacetylase inhibitors in cancer therapy

21 January 2018

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Protein methyltransferases as a target class for drug discovery

21 January 2018

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Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.

21 January 2018

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Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes

21 January 2018

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Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress

21 January 2018

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Reexpression of epigenetically silenced AML tumor suppressor genes by SUV39H1 inhibition

21 January 2018

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Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.

21 January 2018

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Histone deacetylases are critical targets of bortezomib-induced cytotoxicity in multiple myeloma

21 January 2018

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Combination therapy with vidaza and entinostat suppresses tumor growth and reprograms the epigenome in an orthotopic lung cancer model

21 January 2018

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A phase I dose-finding study of 5-azacytidine in combination with sodium phenylbutyrate in patients with refractory solid tumors

21 January 2018

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Revisiting the differentiation paradigm in acute promyelocytic leukemia

21 January 2018

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Anticancer activities of histone deacetylase inhibitors

21 January 2018

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Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors

21 January 2018

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Phase I study of decitabine with doxorubicin and cyclophosphamide in children with neuroblastoma and other solid tumors: a Children's Oncology Group study

21 January 2018

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Phase I study of vorinostat in combination with bortezomib for relapsed and refractory multiple myeloma

21 January 2018

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Vorinostat plus bortezomib for the treatment of relapsed/refractory multiple myeloma: a case series illustrating utility in clinical practice

21 January 2018

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

21 January 2018

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Constitutive activation of signal transducers and activators of transcription predicts vorinostat resistance in cutaneous T-cell lymphoma

21 January 2018

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Analysis of the apoptotic and therapeutic activities of histone deacetylase inhibitors by using a mouse model of B cell lymphoma

21 January 2018

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Activity of deacetylase inhibitor panobinostat (LBH589) in cutaneous T-cell lymphoma models: Defining molecular mechanisms of resistance

21 January 2018

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HR23B is a biomarker for tumor sensitivity to HDAC inhibitor-based therapy

21 January 2018

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Genome-wide loss-of-function screen reveals an important role for the proteasome in HDAC inhibitor-induced apoptosis

21 January 2018

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MLL-aberrant leukemia: complete cytogenetic remission following treatment with a histone deacetylase inhibitor (HDACi)

21 January 2018

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An oncogenomics-based in vivo RNAi screen identifies tumor suppressors in liver cancer

21 January 2018

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Combination therapy of established cancer using a histone deacetylase inhibitor and a TRAIL receptor agonist

21 January 2018

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Eradication of solid tumors using histone deacetylase inhibitors combined with immune-stimulating antibodies

21 January 2018

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Defining the target specificity of ABT-737 and synergistic antitumor activities in combination with histone deacetylase inhibitors

21 January 2018

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Mouse models of human AML accurately predict chemotherapy response

21 January 2018

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Histone Deacetylase Inhibitor Romidepsin Has Differential Activity in Core Binding Factor Acute Myeloid Leukemia

21 January 2018

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Efficacy of azacitidine compared with that of conventional care regimens in the treatment of higher-risk myelodysplastic syndromes: a randomised, open-label, phase III study

21 January 2018

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Further analysis of trials with azacitidine in patients with myelodysplastic syndrome: studies 8421, 8921, and 9221 by the Cancer and Leukemia Group B.

21 January 2018

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Decitabine improves patient outcomes in myelodysplastic syndromes: results of a phase III randomized study

21 January 2018

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Low-dose decitabine versus best supportive care in elderly patients with intermediate- or high-risk myelodysplastic syndrome (MDS) ineligible for intensive chemotherapy: final results of the randomized phase III study of the European Organisation fo

21 January 2018

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Activity of decitabine, a hypomethylating agent, in chronic myelomonocytic leukemia

21 January 2018

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Decitabine effect on tumor global DNA methylation and other parameters in a phase I trial in refractory solid tumors and lymphomas.

21 January 2018

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Phase II trial of DNA methyltransferase 1 inhibition with the antisense oligonucleotide MG98 in patients with metastatic renal carcinoma: a National Cancer Institute of Canada Clinical Trials Group investigational new drug study

21 January 2018

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Phase II trial of the histone deacetylase inhibitor pivaloyloxymethyl butyrate (Pivanex, AN-9) in advanced non-small cell lung cancer

21 January 2018

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Phase II study of belinostat (PXD101), a histone deacetylase inhibitor, for second line therapy of advanced malignant pleural mesothelioma

21 January 2018

1 reference

A phase I clinical trial of the histone deacetylase inhibitor belinostat in patients with advanced hematological neoplasia

21 January 2018

1 reference

Phase I and pharmacokinetic study of MS-275, a histone deacetylase inhibitor, in patients with advanced and refractory solid tumors or lymphoma

21 January 2018

1 reference

A phase I and pharmacokinetic study of the oral histone deacetylase inhibitor, MS-275, in patients with refractory solid tumors and lymphomas

21 January 2018

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A phase II multiple dose clinical trial of histone deacetylase inhibitor ITF2357 in patients with relapsed or progressive multiple myeloma

21 January 2018

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Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents

21 January 2018

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Phase 1 study of the oral isotype specific histone deacetylase inhibitor MGCD0103 in leukemia

21 January 2018

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A phase I study of intravenous LBH589, a novel cinnamic hydroxamic acid analogue histone deacetylase inhibitor, in patients with refractory hematologic malignancies

21 January 2018

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A phase 1 and pharmacodynamic study of depsipeptide (FK228) in chronic lymphocytic leukemia and acute myeloid leukemia.

21 January 2018

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Isoform-selective histone deacetylase inhibitors.

21 January 2018

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A phase I trial of depsipeptide (FR901228) in patients with advanced cancer.

21 January 2018

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Tolerability, pharmacodynamics, and pharmacokinetics studies of depsipeptide (romidepsin) in patients with acute myelogenous leukemia or advanced myelodysplastic syndromes

21 January 2018

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Clinical experience with intravenous and oral formulations of the novel histone deacetylase inhibitor suberoylanilide hydroxamic acid in patients with advanced hematologic malignancies

21 January 2018

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Vorinostat for treatment of cutaneous manifestations of advanced primary cutaneous T-cell lymphoma

21 January 2018

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Phase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group study

21 January 2018

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New clinical developments in histone deacetylase inhibitors for epigenetic therapy of cancer

21 January 2018

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Phase I and pharmacokinetic study of vorinostat, a histone deacetylase inhibitor, in combination with carboplatin and paclitaxel for advanced solid malignancies

21 January 2018

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Phase 1/2 study of the combination of 5-aza-2'-deoxycytidine with valproic acid in patients with leukemia

21 January 2018

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Phase I study of decitabine alone or in combination with valproic acid in acute myeloid leukemia

21 January 2018

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Concentrations of the DNA methyltransferase inhibitor 5-fluoro-2'-deoxycytidine (FdCyd) and its cytotoxic metabolites in plasma of patients treated with FdCyd and tetrahydrouridine (THU).

21 January 2018

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Stability of 5-fluoro-2'-deoxycytidine and tetrahydrouridine in combination

21 January 2018

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A phase II study of epigenetic therapy with hydralazine and magnesium valproate to overcome chemotherapy resistance in refractory solid tumors.

21 January 2018

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Mutations truncating the EP300 acetylase in human cancers

21 January 2018

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Tip60 is a haplo-insufficient tumour suppressor required for an oncogene-induced DNA damage response

21 January 2018

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Relaxation of insulin-like growth factor II gene imprinting implicated in Wilms' tumour

21 January 2018

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21 January 2018

Identifiers

DOI

10.2217/EPI.11.82

1 reference

26 August 2017

1 reference

PubMed ID

22126246