Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a - Test2 - elhamkhani - TriplyDB

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

http://www.wikidata.org/entity/Q27684229

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Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives Open access chemical probes for epigenetic targets Synthesis of lysine methyltransferase inhibitors Epigenetic modulators as therapeutic targets in prostate cancer Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 G9a inhibition potentiates the anti-tumour activity of DNA double-strand break inducing agents by impairing DNA repair independent of p53 status Epigenetic drugs against cancer: an evolving landscape.Structure-activity relationship studies of SETD8 inhibitors.Selective inhibitors of protein methyltransferases The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.Identification and Structure-Activity Relationship Studies of Small-Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1.Developing Spindlin1 small-molecule inhibitors by using protein microarrays.Chromatin deregulation in disease.Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.S-adenosyl methionine is necessary for inhibition of the methyltransferase G9a by the lysine 9 to methionine mutation on histone H3.The H3K9 dimethyltransferases EHMT1/2 protect against pathological cardiac hypertrophy The Lysine Methyltransferase G9a in Immune Cell Differentiation and Function.Regulation of CD4 T-cell differentiation and inflammation by repressive histone methylation.Inhibitors of Protein Methyltransferases and Demethylases.Marked for death: targeting epigenetic changes in cancer.Selective targeting of epigenetic reader domains.Nonhistone Lysine Methylation in the Regulation of Cancer Pathways.Recently discovered EZH2 and EHMT2 (G9a) inhibitors.Inhibitors of enzymes catalyzing modifications to histone lysine residues: structure, function and activity.A chemical probe toolbox for dissecting the cancer epigenome.Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors†Electronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.Structure based design, synthesis and activity studies of small hybrid molecules as HDAC and G9a dual inhibitors.Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity† †The authors declare no competing interests. ‡ ‡Electronic supplementary information (ESI) available: Supple Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8.Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity.Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice.Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.Targeting Epigenetic Aberrations in Pancreatic Cancer, a New Path to Improve Patient Outcomes?Identification of a peptide inhibitor for the histone methyltransferase WHSC1.Histone methylation changes are required for life cycle progression in the human parasite Schistosoma mansoni.

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Discovery and Development of Potent and Selective Inhibitors of Histone Methyltransferase G9a

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2014 nî lūn-bûn

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2014 թուականի Փետրուարին հրատարակուած գիտական յօդուած

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2014 թվականի փետրվարին հրատարակված գիտական հոդված

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2014年の論文

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2014年学术文章

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2014年學術文章

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ACS Medicinal Chemistry Letters

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Discovery and Development of P ...... Histone Methyltransferase G9a

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Andrew M Petros

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Chris Tse

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David Maag

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Fengling Li

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

Jun Guo

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Marina Pliushchev

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Masoud Vedadi

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Michael R Michaelides

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Nirupama B Soni

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Ramzi F Sweis

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P2860

G9a and Glp methylate lysine 373 in the tumor suppressor p53

Covalent histone modifications--miswritten, misinterpreted and mis-erased in human cancers

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells

The epigenomics of cancer

Histone methyltransferases G9a and GLP form heteromeric complexes and are both crucial for methylation of euchromatin at H3-K9

The diverse functions of histone lysine methylation

Epigenetic modifications and human disease

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

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

Unsafe SETs: histone lysine methyltransferases and cancer.

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205-209

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10.1021/ML400496H

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2

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Aagianik kimischri

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