Results 281 to 290 of about 197,157 (312)

Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors

open access: bronze, 2018
Andrea Milelli   +8 more
openalex   +2 more sources

Data from (R)-2-hydroxyglutarate inhibits KDM5 histone lysine demethylases to drive transformation in IDH-mutant cancers

open access: gold
Kathryn Gunn   +17 more
openalex   +1 more source
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Inhibitors of histone demethylases

Bioorganic & Medicinal Chemistry, 2011
Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared.
Lohse, Brian   +6 more
openaire   +3 more sources

In Vitro Histone Demethylase Assays

2022
Dynamic histone methylation regulates gene activation and repression. It is involved in proliferation, differentiation, lineage specification, and development. Histone demethylase assays are invaluable in studying histone demethylation substrate recognition, kinetics, regulation, and inhibition by small molecules, many of which are potential ...
openaire   +2 more sources

Recent Progress in Histone Demethylase Inhibitors

Journal of Medicinal Chemistry, 2016
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with small molecules both for the generation of probes for target exploration and for therapeutic purposes. Here we update on previous reviews on the inhibition of the lysine-specific demethylases (LSDs or KDM1s) and JmjC families of N-methyl-lysine demethylases (JmjC
McAllister   +6 more
openaire   +2 more sources

In Vitro Histone Demethylase Assays

2015
Histone methylation plays pivotal roles in modulating chromatin structure and dynamics and in turn regulates genomic processes that require access to the DNA template. The methylation status at different sites is dynamically regulated by histone methyltransferases and demethylases. During the past decade, two classes of proteins have been characterized
Kenji, Kokura, Lidong, Sun, Jia, Fang
openaire   +2 more sources

In Vitro Histone Demethylase Assays

2009
Histone methylation plays important roles in chromatin structure, transcription, and epigenetic state of the cell. Tremendous discoveries recently demonstrated that methylation mark is not static but is dynamically regulated by both histone methyltransferases and the histone demethylases.
Kenji, Kokura, Jia, Fang
openaire   +2 more sources

JMJD6 Is a Histone Arginine Demethylase

Science, 2007
Arginine methylation occurs on a number of proteins involved in a variety of cellular functions. Histone tails are known to be mono- and dimethylated on multiple arginine residues where they influence chromatin remodeling and gene expression. To date, no enzyme has been shown to reverse these regulatory modifications.
Bingsheng, Chang   +3 more
openaire   +2 more sources

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