Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014). (Q38547122)

4 September 2017

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title

Inhibitors of emerging epigenetic targets for cancer therapy: a patent review (2010-2014). (English)

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4 September 2017

Minoru Tanaka

1

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4 September 2017

Justin M Roberts

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2

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4 September 2017

Jun Qi

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3

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4 September 2017

James E Bradner

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4

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4 September 2017

1 July 2015

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Pharmaceutical patent analyst

4 September 2017

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4 September 2017

4

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4 September 2017

4

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4 September 2017

261-284

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On the use of the word 'epigenetic'.

4 September 2017

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Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia

21 January 2018

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Patterns of somatic mutation in human cancer genomes

21 January 2018

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The genetic basis for cancer treatment decisions

21 January 2018

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21 January 2018

Cancer genome landscapes

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Mutations in regulators of the epigenome and their connections to global chromatin patterns in cancer

21 January 2018

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Epigenetic aberrations during oncogenesis.

21 January 2018

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Chromatin dynamics during cellular reprogramming

21 January 2018

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Exploiting epigenetic vulnerabilities for cancer therapeutics

21 January 2018

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Selective inhibition of BET bromodomains

21 January 2018

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

21 January 2018

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BET bromodomain inhibition as a therapeutic strategy to target c-Myc

21 January 2018

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Targeting MYCN in neuroblastoma by BET bromodomain inhibition

21 January 2018

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Efficacy of BET bromodomain inhibition in Kras-mutant non-small cell lung cancer

21 January 2018

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Chromatin modifications and their function

21 January 2018

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Protein methyltransferases as a target class for drug discovery

21 January 2018

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Histone acetyl transferases as emerging drug targets.

21 January 2018

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The Polycomb complex PRC2 and its mark in life

21 January 2018

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Methylation of H3-lysine 79 is mediated by a new family of HMTases without a SET domain

21 January 2018

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Structure of the catalytic domain of human DOT1L, a non-SET domain nucleosomal histone methyltransferase

21 January 2018

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MLL translocations, histone modifications and leukaemia stem-cell development

21 January 2018

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The pathogenesis of mixed-lineage leukemia

21 January 2018

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The diverse functions of Dot1 and H3K79 methylation.

21 January 2018

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H3K79 methylation profiles define murine and human MLL-AF4 leukemias

21 January 2018

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MLL-rearranged leukemia is dependent on aberrant H3K79 methylation by DOT1L.

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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A medicinal chemistry perspective for targeting histone H3 lysine-79 methyltransferase DOT1L.

21 January 2018

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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

21 January 2018

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Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors

21 January 2018

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Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L

21 January 2018

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EZH1 mediates methylation on histone H3 lysine 27 and complements EZH2 in maintaining stem cell identity and executing pluripotency

21 January 2018

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Ezh1 and Ezh2 maintain repressive chromatin through different mechanisms

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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Enhancer of zeste homolog 2 (EZH2) expression is an independent prognostic factor in renal cell carcinoma

21 January 2018

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The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states

21 January 2018

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Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

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

21 January 2018

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

21 January 2018

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Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

21 January 2018

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Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma

21 January 2018

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Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase

21 January 2018

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Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer

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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Histone demethylation mediated by the nuclear amine oxidase homolog LSD1

21 January 2018

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Distinct localization of histone H3 acetylation and H3-K4 methylation to the transcription start sites in the human genome.

21 January 2018

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Histone H3 lysine 4 methylation patterns in higher eukaryotic genes

21 January 2018

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Lysine-specific demethylase 1 is strongly expressed in poorly differentiated neuroblastoma: implications for therapy

21 January 2018

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Lysine-specific demethylase 1 (LSD1) is highly expressed in ER-negative breast cancers and a biomarker predicting aggressive biology

21 January 2018

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

21 January 2018

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Acute myelogenous leukemia stem cells: from Bench to Bedside.

21 January 2018

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The histone demethylase KDM1A sustains the oncogenic potential of MLL-AF9 leukemia stem cells

21 January 2018

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Lysine-specific demethylase 1 as a potential therapeutic target

21 January 2018

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Histone lysine demethylases as targets for anticancer therapy

21 January 2018

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trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1.

21 January 2018

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Identification of cell-active lysine specific demethylase 1-selective inhibitors

21 January 2018

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Structurally designed trans-2-phenylcyclopropylamine derivatives potently inhibit histone demethylase LSD1/KDM1

21 January 2018

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Readout of epigenetic modifications

21 January 2018

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Chemical phylogenetics of histone deacetylases

21 January 2018

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Interplay between different epigenetic modifications and mechanisms

21 January 2018

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Bromodomain: an acetyl-lysine binding domain

21 January 2018

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Targeting bromodomains: epigenetic readers of lysine acetylation

21 January 2018

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Recruitment of P-TEFb for stimulation of transcriptional elongation by the bromodomain protein Brd4

21 January 2018

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The mechanism of release of P-TEFb and HEXIM1 from the 7SK snRNP by viral and cellular activators includes a conformational change in 7SK

21 January 2018

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Phosphorylation and functions of the RNA polymerase II CTD

21 January 2018

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Brd4 recruits P-TEFb to chromosomes at late mitosis to promote G1 gene expression and cell cycle progression

21 January 2018

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Master transcription factors and mediator establish super-enhancers at key cell identity genes

21 January 2018

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Selective inhibition of tumor oncogenes by disruption of super-enhancers

21 January 2018

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Discovery and characterization of super-enhancer-associated dependencies in diffuse large B cell lymphoma.

21 January 2018

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Targeting MYC dependence in cancer by inhibiting BET bromodomains

21 January 2018

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NF-κB directs dynamic super enhancer formation in inflammation and atherogenesis

21 January 2018

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BRD4 bromodomain gene rearrangement in aggressive carcinoma with translocation t(15;19)

21 January 2018

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Midline carcinoma of children and young adults with NUT rearrangement.

21 January 2018

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Discovery and characterization of small molecule inhibitors of the BET family bromodomains

21 January 2018

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Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains

21 January 2018

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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

21 January 2018

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

21 January 2018

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From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

21 January 2018

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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A)

21 January 2018

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Brd4 coactivates transcriptional activation of NF-kappaB via specific binding to acetylated RelA

21 January 2018

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Two-pronged binding with bromodomain-containing protein 4 liberates positive transcription elongation factor b from inactive ribonucleoprotein complexes.

21 January 2018

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Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

21 January 2018

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Fragment-based discovery of bromodomain inhibitors part 1: inhibitor binding modes and implications for lead discovery

21 January 2018

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Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides

21 January 2018

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The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor

21 January 2018

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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

21 January 2018

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

21 January 2018

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Structure-Guided Design of Potent Diazobenzene Inhibitors for the BET Bromodomains

21 January 2018

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An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1

21 January 2018

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Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

21 January 2018

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Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

21 January 2018

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BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.

21 January 2018

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21 January 2018

Identifiers

DOI

10.4155/PPA.15.16

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4 September 2017

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