(Q37590090)

21 August 2017

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title

Protein methyltransferases as a target class for drug discovery (English)

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21 August 2017

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Robert A Copeland

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21 August 2017

Michael E Solomon

series ordinal

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21 August 2017

Victoria M Richon

series ordinal

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21 August 2017

publication date

1 September 2009

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Nature Reviews Drug Discovery

21 August 2017

published in

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21 August 2017

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21 August 2017

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21 August 2017

page(s)

724-732

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The language of covalent histone modifications

21 August 2017

cites work

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Chromatin modifications and their function

31 March 2020

1 reference

Chemical mechanisms of histone lysine and arginine modifications

31 March 2020

1 reference

Chemical probes for histone-modifying enzymes

31 March 2020

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Chromatin-modifying enzymes as therapeutic targets--Part 1

31 March 2020

1 reference

At the flick of a switch: epigenetic drugs

31 March 2020

1 reference

The epigenomics of cancer

31 March 2020

1 reference

Epigenetic control of T-helper-cell differentiation

31 March 2020

1 reference

Epigenetic regulation in psychiatric disorders

31 March 2020

1 reference

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

31 March 2020

1 reference

H3K79 methylation profiles define murine and human MLL-AF4 leukemias

31 March 2020

1 reference

Arginine methylation regulates the p53 response

31 March 2020

1 reference

Aberrant expression of CARM1, a transcriptional coactivator of androgen receptor, in the development of prostate carcinoma and androgen-independent status

31 March 2020

1 reference

Unsafe SETs: histone lysine methyltransferases and cancer

31 March 2020

1 reference

Roles of the EZH2 histone methyltransferase in cancer epigenetics

31 March 2020

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The SET-domain protein superfamily: protein lysine methyltransferases

31 March 2020

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ESET/SETDB1 gene expression and histone H3 (K9) trimethylation in Huntington's disease

31 March 2020

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The arginine methyltransferase CARM1 regulates the coupling of transcription and mRNA processing.

31 March 2020

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Role of the histone H3 lysine 4 methyltransferase, SET7/9, in the regulation of NF-kappaB-dependent inflammatory genes. Relevance to diabetes and inflammation

31 March 2020

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Arginine methyltransferase CARM1 is a promoter-specific regulator of NF-kappaB-dependent gene expression

31 March 2020

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Protein arginine methyltransferase 1 coactivates NF-kappaB-dependent gene expression synergistically with CARM1 and PARP1.

31 March 2020

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Trimethylation of histone H3 lysine 4 by Set1 in the lytic infection of human herpes simplex virus 1.

31 March 2020

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Coactivator-associated arginine methyltransferase 1 enhances transcriptional activity of the human T-cell lymphotropic virus type 1 long terminal repeat through direct interaction with Tax.

31 March 2020

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Structural and sequence motifs of protein (histone) methylation enzymes

31 March 2020

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High-throughput kinase profiling as a platform for drug discovery

31 March 2020

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Small molecule regulators of protein arginine methyltransferases

31 March 2020

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New nomenclature for chromatin-modifying enzymes

31 March 2020

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Enzymatic mechanism and product specificity of SET-domain protein lysine methyltransferases

31 March 2020

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A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

31 March 2020

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A quantitative analysis of kinase inhibitor selectivity

31 March 2020

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

31 March 2020

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Structure of the conserved core of the yeast Dot1p, a nucleosomal histone H3 lysine 79 methyltransferase

31 March 2020

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In vitro and in vivo analyses of a Phe/Tyr switch controlling product specificity of histone lysine methyltransferases

31 March 2020

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Mechanism of multiple lysine methylation by the SET domain enzyme Rubisco LSMT

31 March 2020

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Structural basis for the product specificity of histone lysine methyltransferases

31 March 2020

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Nonprocessive methylation by Dot1 leads to functional redundancy of histone H3K79 methylation states

31 March 2020

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Biological effects of inhibitors of S-adenosylhomocysteine hydrolase

31 March 2020

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DNA methylation as a target for drug design

31 March 2020

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Panobinostat treatment depletes EZH2 and DNMT1 levels and enhances decitabine mediated de-repression of JunB and loss of survival of human acute leukemia cells

31 March 2020

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

31 March 2020

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N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

31 March 2020

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

31 March 2020

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Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).

31 March 2020

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Functional insights from structures of coactivator-associated arginine methyltransferase 1 domains

31 March 2020

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Structural and functional analysis of SET8, a histone H4 Lys-20 methyltransferase

31 March 2020

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Novel agents on the horizon for cancer therapy

31 March 2020

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Chromatin, cancer and drug therapies

31 March 2020

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

31 March 2020

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Deregulation of histone lysine methyltransferases contributes to oncogenic transformation of human bronchoepithelial cells

31 March 2020

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

31 March 2020

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Involvement of a homolog of Drosophila trithorax by 11q23 chromosomal translocations in acute leukemias

31 March 2020

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The t(4;11) chromosome translocation of human acute leukemias fuses the ALL-1 gene, related to Drosophila trithorax, to the AF-4 gene

31 March 2020

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Therapeutic targeting of MLL.

31 March 2020

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NUP98-NSD1 links H3K36 methylation to Hox-A gene activation and leukaemogenesis.

31 March 2020

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

31 March 2020

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Multiple-myeloma-related WHSC1/MMSET isoform RE-IIBP is a histone methyltransferase with transcriptional repression activity

31 March 2020

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The multiple myeloma associated MMSET gene contributes to cellular adhesion, clonogenic growth, and tumorigenicity.

31 March 2020

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NSD3, a new SET domain-containing gene, maps to 8p12 and is amplified in human breast cancer cell lines

31 March 2020

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NUP98 is fused to the NSD3 gene in acute myeloid leukemia associated with t(8;11)(p11.2;p15).

31 March 2020

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High-resolution genomic profiles of human lung cancer

31 March 2020

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hDOT1L links histone methylation to leukemogenesis

31 March 2020

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The mixed-lineage leukemia fusion partner AF4 stimulates RNA polymerase II transcriptional elongation and mediates coordinated chromatin remodeling

31 March 2020

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SMYD3 encodes a histone methyltransferase involved in the proliferation of cancer cells

31 March 2020

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Enhanced SMYD3 expression is essential for the growth of breast cancer cells

31 March 2020

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EZH2 is downstream of the pRB-E2F pathway, essential for proliferation and amplified in cancer

31 March 2020

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The polycomb group protein EZH2 is involved in progression of prostate cancer

31 March 2020

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Regulation of Estrogen Receptor α by the SET7 Lysine Methyltransferase

31 March 2020

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Gene amplification and overexpression of PRDM14 in breast cancers.

31 March 2020

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Involvement of arginine methyltransferase CARM1 in androgen receptor function and prostate cancer cell viability

31 March 2020

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CARM1 regulates estrogen-stimulated breast cancer growth through up-regulation of E2F1.

31 March 2020

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PRMT5-mediated methylation of histone H4R3 recruits DNMT3A, coupling histone and DNA methylation in gene silencing.

31 March 2020

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Substrate specificity and kinetic mechanism of mammalian G9a histone H3 methyltransferase

31 March 2020

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Catalytic properties and kinetic mechanism of human recombinant Lys-9 histone H3 methyltransferase SUV39H1: participation of the chromodomain in enzymatic catalysis.

31 March 2020

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

31 March 2020

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

31 March 2020

1 reference

Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists

31 March 2020

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/19721445

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Catalytic roles for carbon-oxygen hydrogen bonding in SET domain lysine methyltransferases

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/19721445

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1038/NRD2974

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21 August 2017

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