(Q39147132)

9 September 2017

title

A chemical probe toolbox for dissecting the cancer epigenome. (English)

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9 September 2017

Ricky W Johnstone

3

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author name string

Jake Shortt

series ordinal

1

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9 September 2017

Christopher J Ott

series ordinal

2

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9 September 2017

James E Bradner

series ordinal

4

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9 September 2017

language of work or name

English

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publication date

1 February 2017

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9 September 2017

published in

Nature Reviews Cancer

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9 September 2017

volume

17

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9 September 2017

issue

3

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9 September 2017

page(s)

160-183

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Chromatin modifications and their function

9 September 2017

cites work

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Histone demethylation mediated by the nuclear amine oxidase homolog LSD1

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LSD1 demethylates repressive histone marks to promote androgen-receptor-dependent transcription

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The histone LSD1 demethylase in stemness and cancer transcription programs

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A novel nuclear protein, 5qNCA (LOC51780) is a candidate for the myeloid leukemia tumor suppressor gene on chromosome 5 band q31.

21 January 2018

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JHDM2A, a JmjC-containing H3K9 demethylase, facilitates transcription activation by androgen receptor

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Cooperative demethylation by JMJD2C and LSD1 promotes androgen receptor-dependent gene expression

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Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications

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

21 January 2018

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Structural basis for the inhibition of the LSD1 histone demethylase by the antidepressant trans-2-phenylcyclopropylamine

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

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Biochemical, structural, and biological evaluation of tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and LSD2

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

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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A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency

21 January 2018

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

21 January 2018

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Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia

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Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

21 January 2018

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Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates

21 January 2018

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A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases

21 January 2018

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A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

21 January 2018

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Contrasting roles of histone 3 lysine 27 demethylases in acute lymphoblastic leukaemia

21 January 2018

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Pharmacologic inhibition of histone demethylation as a therapy for pediatric brainstem glioma

21 January 2018

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Inhibition of demethylases by GSK-J1/J4.

21 January 2018

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How chromatin-binding modules interpret histone modifications: lessons from professional pocket pickers

21 January 2018

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Haematopoietic malignancies caused by dysregulation of a chromatin-binding PHD finger

21 January 2018

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Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain

21 January 2018

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Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3.

21 January 2018

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Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family

21 January 2018

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A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1

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 acetyltransferases

21 January 2018

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The Role of Histone Acetyltransferases in Normal and Malignant Hematopoiesis

21 January 2018

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Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor

21 January 2018

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Targeting p300 Addiction in CBP-Deficient Cancers Causes Synthetic Lethality by Apoptotic Cell Death due to Abrogation of MYC Expression

21 January 2018

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The leukemogenicity of AML1-ETO is dependent on site-specific lysine acetylation

21 January 2018

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Nitric Oxide-Mediated Histone Hyperacetylation in Oral Cancer: Target for a Water-Soluble HAT Inhibitor, CTK7A

21 January 2018

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Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents.

21 January 2018

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Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin

21 January 2018

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Probing p300/CBP associated factor (PCAF)-dependent pathways with a small molecule inhibitor

21 January 2018

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Salicylate, diflunisal and their metabolites inhibit CBP/p300 and exhibit anticancer activity

21 January 2018

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The structural basis of protein acetylation by the p300/CBP transcriptional coactivator

21 January 2018

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Structure of the p300 catalytic core and implications for chromatin targeting and HAT regulation

21 January 2018

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Anticancer activities of histone deacetylase inhibitors

21 January 2018

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Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors trichostatin and trapoxin

21 January 2018

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Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis.

21 January 2018

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Chemical phylogenetics of histone deacetylases

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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Structural Biasing Elements for In-Cell Histone Deacetylase Paralog Selectivity

21 January 2018

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Depudecin induces morphological reversion of transformed fibroblasts via the inhibition of histone deacetylase

21 January 2018

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KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo.

21 January 2018

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Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo

21 January 2018

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Trichostatin A increases SMN expression and survival in a mouse model of spinal muscular atrophy

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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Functional-genetic dissection of HDAC dependencies in mouse lymphoid and myeloid malignancies

21 January 2018

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Histone deacetylase 3 as a novel therapeutic target in multiple myeloma.

21 January 2018

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Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma

21 January 2018

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Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells

21 January 2018

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n-Butyrate causes histone modification in HeLa and Friend erythroleukaemia cells

21 January 2018

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Hydralazine and magnesium valproate as epigenetic treatment for myelodysplastic syndrome. Preliminary results of a phase-II trial

21 January 2018

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Results from a pivotal, open-label, phase II study of romidepsin in relapsed or refractory peripheral T-cell lymphoma after prior systemic therapy

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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A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors

21 January 2018

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Design and synthesis of 4-[(s-triazin-2-ylamino)methyl]-N-(2-aminophenyl)-benzamides and their analogues as a novel class of histone deacetylase inhibitors

21 January 2018

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Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases

21 January 2018

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Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).

21 January 2018

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Inhibition of the function of class IIa HDACs by blocking their interaction with MEF2

21 January 2018

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Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy

21 January 2018

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Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group

21 January 2018

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Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides

21 January 2018

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The multifaceted functions of sirtuins in cancer

21 January 2018

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Impaired DNA damage response, genome instability, and tumorigenesis in SIRT1 mutant mice

21 January 2018

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Sorting out functions of sirtuins in cancer

21 January 2018

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Sirtuin activators and inhibitors

21 January 2018

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Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan

21 January 2018

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Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes

21 January 2018

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Preclinical evaluation of a novel SIRT1 modulator SRT1720 in multiple myeloma cells

21 January 2018

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DOT1L inhibits SIRT1-mediated epigenetic silencing to maintain leukemic gene expression in MLL-rearranged leukemia.

21 January 2018

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Inhibition of silencing and accelerated aging by nicotinamide, a putative negative regulator of yeast sir2 and human SIRT1

21 January 2018

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Mechanism-based inhibition of Sir2 deacetylases by thioacetyl-lysine peptide

21 January 2018

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Design, synthesis, and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors

21 January 2018

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Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening

21 January 2018

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An in silico approach to discovering novel inhibitors of human sirtuin type 2.

21 January 2018

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Mechanisms and molecular probes of sirtuins.

21 January 2018

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Pleiotropic effects of the sirtuin inhibitor sirtinol involves concentration-dependent modulation of multiple nuclear receptor-mediated pathways in androgen-responsive prostate cancer cell LNCaP.

21 January 2018

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Identification of a small molecule inhibitor of Sir2p

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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Development of pyrazolone and isoxazol-5-one cambinol analogues as sirtuin inhibitors

21 January 2018

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Discovery, in vivo activity, and mechanism of action of a small-molecule p53 activator.

21 January 2018

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Activation of p53 by SIRT1 inhibition enhances elimination of CML leukemia stem cells in combination with imatinib

21 January 2018

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Tenovin-D3, a novel small-molecule inhibitor of sirtuin SirT2, increases p21 (CDKN1A) expression in a p53-independent manner.

21 January 2018

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The role of p21(waf1/cip1) and p27(Kip1) in HDACi-mediated tumor cell death and cell cycle arrest in the Eμ-myc model of B-cell lymphoma

21 January 2018

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Suramin: clinical uses and structure-activity relationships.

21 January 2018

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Inhibition of SIRT1 catalytic activity increases p53 acetylation but does not alter cell survival following DNA damage

21 January 2018

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Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease

21 January 2018

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Structure and ligand of a histone acetyltransferase bromodomain

21 January 2018

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Structure and function of a human TAFII250 double bromodomain module

21 January 2018

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The double bromodomain protein Brd4 binds to acetylated chromatin during interphase and mitosis

21 January 2018

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Brd4 marks select genes on mitotic chromatin and directs postmitotic transcription

21 January 2018

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Gene bookmarking accelerates the kinetics of post-mitotic transcriptional re-activation

21 January 2018

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Cooperative binding of two acetylation marks on a histone tail by a single bromodomain

21 January 2018

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BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

21 January 2018

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BRD-NUT oncoproteins: a family of closely related nuclear proteins that block epithelial differentiation and maintain the growth of carcinoma cells.

21 January 2018

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Selective inhibition of BET bromodomains

21 January 2018

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Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

21 January 2018

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Genome-wide localization of small molecules

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

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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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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The landscape of somatic copy-number alteration across human cancers

21 January 2018

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c-Myc regulates transcriptional pause release

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 MYC dependence in cancer by inhibiting BET bromodomains

21 January 2018

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BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

21 January 2018

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Selective inhibition of tumor oncogenes by disruption of super-enhancers

21 January 2018

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Extreme instability of myc mRNA in normal and transformed human cells.

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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Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA

21 January 2018

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

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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3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

21 January 2018

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The super elongation complex (SEC) and MLL in development and disease

21 January 2018

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The PAF complex synergizes with MLL fusion proteins at HOX loci to promote leukemogenesis

21 January 2018

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PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

21 January 2018

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Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

21 January 2018

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Safety, tolerability, and preliminary activity of CUDC-907, a first-in-class, oral, dual inhibitor of HDAC and PI3K, in patients with relapsed or refractory lymphoma or multiple myeloma: an open-label, dose-escalation, phase 1 trial

21 January 2018

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IDH mutations in cancer and progress toward development of targeted therapeutics

21 January 2018

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Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors

21 January 2018

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Toxicity of 5-aza-2'-deoxycytidine to mammalian cells is mediated primarily by covalent trapping of DNA methyltransferase rather than DNA demethylation

21 January 2018

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Mechanism of inhibition of DNA methyltransferases by cytidine analogs in cancer therapy

21 January 2018

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RNA-dependent inhibition of ribonucleotide reductase is a major pathway for 5-azacytidine activity in acute myeloid leukemia

21 January 2018

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Azacytidine inhibits RNA methylation at DNMT2 target sites in human cancer cell lines

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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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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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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TET2 mutations predict response to hypomethylating agents in myelodysplastic syndrome patients

21 January 2018

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Identifiers

DOI

10.1038/NRC.2016.148

1 reference

9 September 2017

1 reference