Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. - Wikidata - awgldk - TriplyDB

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.

http://www.wikidata.org/entity/Q34059822

about

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells Synthesis of lysine methyltransferase inhibitors Epigenomics of leukemia: from mechanisms to therapeutic applications Chemical probes of histone lysine methyltransferases Current chemical biology approaches to interrogate protein methyltransferases Small-Molecule Ligands of Methyl-Lysine Binding Proteins Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a The emerging role of lysine methyltransferase SETD8 in human diseases Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 DNA methylation-independent reversion of gemcitabine resistance by hydralazine in cervical cancer cells Functional Characterization of D9, a Novel Deazaneplanocin A (DZNep) Analog, in Targeting Acute Myeloid Leukemia (AML)AlphaScreen-Based Assays: Ultra-High-Throughput Screening for Small-Molecule Inhibitors of Challenging Enzymes and Protein-Protein Interactions Assay development for histone methyltransferases.Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.Methods for Activity Analysis of the Proteins that Regulate Histone Methylation Chromatin proteins and modifications as drug targets.TR-FRET cellular assays for interrogating posttranslational modifications of histone H3.Fluorescence-based methods for screening writers and readers of histone methyl marks.Efficient hit-finding approaches for histone methyltransferases: the key parameters.Inhibition of H3K9 methyltransferase G9a repressed cell proliferation and induced autophagy in neuroblastoma cells.Perspectives on the discovery of small-molecule modulators for epigenetic processes.Current limitations and future opportunities for epigenetic therapies.Development of diaminoquinazoline histone lysine methyltransferase inhibitors as potent blood-stage antimalarial compounds Microscale thermophoresis quantifies biomolecular interactions under previously challenging conditions Small-molecule inhibitors of the protein methyltransferase SET7/9 identified in a high-throughput screen.An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1 Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum Epigenetic drugs against cancer: an evolving landscape.Writing and rewriting the epigenetic code of cancer cells: from engineered proteins to small molecules Use of epigenetic drugs in disease: an overview.Small-molecular modulators of cancer-associated epigenetic mechanisms.Managing missing measurements in small-molecule screens.Structure-activity relationship studies of SETD8 inhibitors.Recent progress in the discovery of small-molecule inhibitors of the HMT EZH2 for the treatment of cancer.Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans Selective inhibitors of protein methyltransferases Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines Promoting illiteracy in epigenetics: an emerging therapeutic strategy.

P2860

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P2860

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.

http://www.wikidata.org/entity/Q34059822

description

2010 nî lūn-bûn

@nan

2010 թուականի Օգոստոսին հրատարակուած գիտական յօդուած

@hyw

2010 թվականի օգոստոսին հրատարակված գիտական հոդված

@hy

2010年の論文

@ja

2010年論文

@yue

2010年論文

@zh-hant

2010年論文

@zh-hk

2010年論文

@zh-mo

2010年論文

@zh-tw

2010年论文

@wuu

name

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@ast

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@en

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

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type

label

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

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Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

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Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@nl

prefLabel

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@ast

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@en

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@nl

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P1433

Journal of Medicinal Chemistry

P1476

Protein lysine methyltransfera ...... no-7-aminoalkoxy-quinazolines.

@en

P2093

Abdellah Allali-Hassani

http://www.w3.org/2001/XMLSchema#string

Aiping Dong

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Alena Siarheyeva

http://www.w3.org/2001/XMLSchema#string

Amy M Quinn

http://www.w3.org/2001/XMLSchema#string

Dmitri B Kireev

http://www.w3.org/2001/XMLSchema#string

Feng Liu

http://www.w3.org/2001/XMLSchema#string

Guillermo Senisterra

http://www.w3.org/2001/XMLSchema#string

Irene Chau

http://www.w3.org/2001/XMLSchema#string

J Martin Herold

http://www.w3.org/2001/XMLSchema#string

Jacqueline L Norris

http://www.w3.org/2001/XMLSchema#string

P2860

Translating the Histone Code

Regulation of chromatin structure by site-specific histone H3 methyltransferases

G9a and Glp methylate lysine 373 in the tumor suppressor p53

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

L3MBTL1 recognition of mono- and dimethylated histones

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

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

The language of covalent histone modifications

Chromatin modifications and their function

The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability

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5844-5857

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scholarly article

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10.1021/JM100478Y

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P407

P433

15

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P478

53

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P50

Cheryl Arrowsmith

Gregory A Wasney

P577

2010-08-01T00:00:00Z

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45112489

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20614940

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P921

protein structure

P932

2920043

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