(Q37594007)

21 August 2017

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title

The emerging therapeutic potential of histone methyltransferase and demethylase inhibitors (English)

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21 August 2017

Manfred Jung

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Wolfgang Sippl

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Astrid Spannhoff

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21 August 2017

Alexander-Thomas Hauser

series ordinal

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21 August 2017

Ralf Heinke

series ordinal

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21 August 2017

publication date

1 October 2009

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21 August 2017

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21 August 2017

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21 August 2017

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21 August 2017

page(s)

1568-1582

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Chemical mechanisms of histone lysine and arginine modifications

21 August 2017

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Arginine methylation an emerging regulator of protein function

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Active genes are tri-methylated at K4 of histone H3

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Enzymatic demethylation of calf thymus histones

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The emerging functions of histone demethylases

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

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Structure and activity of enzymes that remove histone modifications

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Epigenetic control using natural products and synthetic molecules

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

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Set domain-containing protein, G9a, is a novel lysine-preferring mammalian histone methyltransferase with hyperactivity and specific selectivity to lysines 9 and 27 of histone H3

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G9a histone methyltransferase plays a dominant role in euchromatic histone H3 lysine 9 methylation and is essential for early embryogenesis

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7 January 2021

Protein lysine methyltransferase G9a acts on non-histone targets

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Arginine methylation at a glance

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Protein arginine methyltransferases: evolution and assessment of their pharmacological and therapeutic potential

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7 January 2021

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Methylation of histone H4 at arginine 3 occurs in vivo and is mediated by the nuclear receptor coactivator PRMT1

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7 January 2021

PRMT2, a member of the protein arginine methyltransferase family, is a coactivator of the androgen receptor

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7 January 2021

Protein arginine-methyltransferase-dependent oncogenesis

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7 January 2021

Arginine N-methyltransferase 1 is required for early postimplantation mouse development, but cells deficient in the enzyme are viable

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7 January 2021

Human SWI/SNF-associated PRMT5 methylates histone H3 arginine 8 and negatively regulates expression of ST7 and NM23 tumor suppressor genes

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7 January 2021

Expression of nitric oxide related enzymes in coronary heart disease

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7 January 2021

Mechanisms of Disease: biomarkers and molecular targets from microarray gene expression studies in prostate cancer

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7 January 2021

Hypoxic silencing of tumor suppressor RUNX3 by histone modification in gastric cancer cells

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7 January 2021

Association of the SUV39H1 histone methyltransferase with the DNA methyltransferase 1 at mRNA expression level in primary colorectal cancer.

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7 January 2021

Downregulation of histone H3 lysine 9 methyltransferase G9a induces centrosome disruption and chromosome instability in cancer cells.

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7 January 2021

The MMSET protein is a histone methyltransferase with characteristics of a transcriptional corepressor

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7 January 2021

hDOT1L links histone methylation to leukemogenesis

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Histone demethylation mediated by the nuclear amine oxidase homolog LSD1

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

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

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7 January 2021

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

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

p53 is regulated by the lysine demethylase LSD1

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7 January 2021

Structure and mechanism of lysine-specific demethylase enzymes

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7 January 2021

Crystal structure and mechanism of human lysine-specific demethylase-1.

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7 January 2021

Crystal structure of human histone lysine-specific demethylase 1 (LSD1).

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7 January 2021

Functional interplay between histone demethylase and deacetylase enzymes

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7 January 2021

Human histone demethylase LSD1 reads the histone code

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7 January 2021

Jmjd2b antagonizes H3K9 trimethylation at pericentric heterochromatin in mammalian cells

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7 January 2021

Recognition of unmethylated histone H3 lysine 4 links BHC80 to LSD1-mediated gene repression

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7 January 2021

Regulation of LSD1 histone demethylase activity by its associated factors

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7 January 2021

Histone lysine demethylases: emerging roles in development, physiology and disease

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7 January 2021

JmjC-domain-containing proteins and histone demethylation

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7 January 2021

Histone demethylation by a family of JmjC domain-containing proteins

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7 January 2021

Reversal of histone lysine trimethylation by the JMJD2 family of histone demethylases

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7 January 2021

Methylation: lost in hydroxylation?

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7 January 2021

Histone demethylation by hydroxylation: chemistry in action

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7 January 2021

Structural basis of the recognition of a methylated histone tail by JMJD2A

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7 January 2021

Diversity within the JMJD2 histone demethylase family

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Functional dynamics of H3K9 methylation during meiotic prophase progression

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

JMJD3 is a histone H3K27 demethylase.

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

It takes a PHD to read the histone code

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Structural basis for the methylation state-specific recognition of histone H4-K20 by 53BP1 and Crb2 in DNA repair

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Di-methyl H4 lysine 20 targets the checkpoint protein Crb2 to sites of DNA damage

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Demethylation of trimethylated histone H3 Lys4 in vivo by JARID1 JmjC proteins.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

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

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

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

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

The hairless gene mutated in congenital hair loss disorders encodes a novel nuclear receptor corepressor

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

JMJD6 is a histone arginine demethylase

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Human PAD4 regulates histone arginine methylation levels via demethylimination

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Androgen receptor coactivators lysine-specific histone demethylase 1 and four and a half LIM domain protein 2 predict risk of prostate cancer recurrence

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

The lysine-specific demethylase 1 is required for cell proliferation in both p53-dependent and -independent manners

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Carcinogen-induced histone alteration in normal human mammary epithelial cells

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

PLU-1 nuclear protein, which is upregulated in breast cancer, shows restricted expression in normal human adult tissues: a new cancer/testis antigen?

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

PLU-1 is an H3K4 demethylase involved in transcriptional repression and breast cancer cell proliferation

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7 January 2021

The putative oncogene GASC1 demethylates tri- and dimethylated lysine 9 on histone H3

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7 January 2021

JARID1B is a histone H3 lysine 4 demethylase up-regulated in prostate cancer

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Mutations in PHF8 are associated with X linked mental retardation and cleft lip/cleft palate

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

The histone H3K4 demethylase SMCX links REST target genes to X-linked mental retardation.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Small molecule regulators of protein arginine methyltransferases

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7 January 2021

Target-based approach to inhibitors of histone arginine methyltransferases

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7 January 2021

Assays for the identification and evaluation of histone acetyltransferase inhibitors

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

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

1 reference

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7 January 2021

A novel arginine methyltransferase inhibitor with cellular activity

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Avidin plate assay system for enzymatic characterization of a histone lysine methyltransferase

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7 January 2021

A coupled fluorescent assay for histone methyltransferases

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7 January 2021

A general fluorescence-based coupled assay for S-adenosylmethionine-dependent methyltransferases

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

An enzyme-coupled continuous spectrophotometric assay for S-adenosylmethionine-dependent methyltransferases.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

An enzyme-coupled colorimetric assay for S-adenosylmethionine-dependent methyltransferases

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Inhibitory study of protein arginine methyltransferase 1 using a fluorescent approach.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

A Spectrophotometric Method for Determining the Oxidative Deamination of Methylamine by the Amine Oxidases

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Specificity and mechanism of JMJD2A, a trimethyllysine-specific histone demethylase

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Histone demethylation catalysed by LSD1 is a flavin-dependent oxidative process

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Properties of purified recombinant human polyamine oxidase, PAOh1/SMO

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7 January 2021

Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes

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7 January 2021

Clinical development of histone deacetylase inhibitors as anticancer agents

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7 January 2021

Anticancer activities of histone deacetylase inhibitors

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7 January 2021

Sinefungin, a potent inhibitor of S-adenosylmethionine: Protein O-methyltransferase

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7 January 2021

Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Structural basis for the product specificity of histone lysine methyltransferases

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors.

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7 January 2021

Virtual screening and biological characterization of novel histone arginine methyltransferase PRMT1 inhibitors

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7 January 2021

Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1).

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7 January 2021

Depression and monoamine oxidase

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7 January 2021

Structural insights into the mechanism of amine oxidation by monoamine oxidases A and B

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7 January 2021

Short review on monoamine oxidase and its inhibitors

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7 January 2021

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

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Crystal structure of histone demethylase LSD1 and tranylcypromine at 2.25 A

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

A mechanism-based inactivator for histone demethylase LSD1.

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

Regulation of coactivator complex assembly and function by protein arginine methylation and demethylimination

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https://api.crossref.org/works/10.1002%2FCMDC.200900301

7 January 2021

MBD2/NuRD and MBD3/NuRD, two distinct complexes with different biochemical and functional properties.

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7 January 2021

Identifiers

DOI

10.1002/CMDC.200900301

1 reference

21 August 2017

1 reference