Chemical and biochemical perspectives of protein lysine methylation
M Luo - Chemical reviews, 2018 - ACS Publications
Protein lysine methylation is a distinct posttranslational modification that causes minimal
changes in the size and electrostatic status of lysine residues. Lysine methylation plays …
changes in the size and electrostatic status of lysine residues. Lysine methylation plays …
Fluorescence polarization assays in small molecule screening
WA Lea, A Simeonov - Expert opinion on drug discovery, 2011 - Taylor & Francis
Importance of the field: Fluorescence polarization (FP) is a homogeneous method that
allows rapid and quantitative analysis of diverse molecular interactions and enzyme …
allows rapid and quantitative analysis of diverse molecular interactions and enzyme …
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells
Protein lysine methyltransferases G9a and GLP modulate the transcriptional repression of a
variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as …
variety of genes via dimethylation of Lys9 on histone H3 (H3K9me2) as well as …
Structural biology of human H3K9 methyltransferases
H Wu, J Min, VV Lunin, T Antoshenko, L Dombrovski… - PloS one, 2010 - journals.plos.org
SET domain methyltransferases deposit methyl marks on specific histone tail lysine residues
and play a major role in epigenetic regulation of gene transcription. We solved the structures …
and play a major role in epigenetic regulation of gene transcription. We solved the structures …
Small molecule inhibitors of protein arginine methyltransferases
Introduction: Arginine methylation is an abundant posttranslational modification occurring in
mammalian cells and catalyzed by protein arginine methyltransferases (PRMTs) …
mammalian cells and catalyzed by protein arginine methyltransferases (PRMTs) …
Discovery of a 2, 4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a
F Liu, X Chen, A Allali-Hassani, AM Quinn… - Journal of medicinal …, 2009 - ACS Publications
SAR exploration of the 2, 4-diamino-6, 7-dimethoxyquinazoline template led to the discovery
of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal …
of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal …
Discovery of the first-in-class G9a/GLP covalent inhibitors
The highly homologous protein lysine methyltransferases G9a and GLP, which catalyze
mono-and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various …
mono-and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various …
Structural and functional analysis of SET8, a histone H4 Lys-20 methyltransferase
JF Couture, E Collazo, JS Brunzelle… - Genes & …, 2005 - genesdev.cshlp.org
SET8 (also known as PR-SET7) is a histone H4-Lys-20-specific methyltransferase that is
implicated in cell-cycle-dependent transcriptional silencing and mitotic regulation in …
implicated in cell-cycle-dependent transcriptional silencing and mitotic regulation in …
Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2, 4-diamino-7-aminoalkoxy-quinazolines.
F Liu, X Chen, A Allali-Hassani, AM Quinn… - Journal of medicinal …, 2010 - ACS Publications
Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3
(H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic …
(H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic …
[HTML][HTML] Division of labor between the chromodomains of HP1 and Suv39 methylase enables coordination of heterochromatin spread
In Schizosaccharomyces pombe, heterochromatin spread, which is marked by histone 3
lysine 9 methylation (H3K9me), requires the chromodomains (CDs) of the H3K9 methylase …
lysine 9 methylation (H3K9me), requires the chromodomains (CDs) of the H3K9 methylase …