Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Epigenetic regulation of chromatin plays a critical role in controlling stem cell function and
tumorigenesis. The histone lysine demethylase, KDM5B, which catalyzes the demethylation …

Methylation of lysine residues on histone tail is a dynamic epigenetic modification that plays
a key role in chromatin structure and gene regulation. Members of the KDM5 (also known as …

The KDM5/JARID1 family of Fe (II)-and α-ketoglutarate-dependent demethylases removes
methyl groups from methylated lysine 4 of histone H3. Accumulating evidence supports a …

The histone lysine demethylase 4 (KDM4) family plays an important role in regulating gene
transcription, DNA repair, and metabolism. The dysregulation of KDM4 functions is …

Acute myeloid leukemias (AMLs) with a rearrangement of the mixed-linage leukemia (MLL)
gene are aggressive hematopoietic malignancies. Here, we explored the feasibility of using …

Lysine-specific demethylase 4 A (KDM4A, also named JMJD2A, KIA0677, or JHDM3A) is a
demethylase that can remove methyl groups from histones H3K9me2/3, H3K36me2/3, and …

Jumonji-C domain-containing protein 5 (JMJD5) is a 2-oxoglutarate (2OG)-dependent
oxygenase that plays important roles in development, circadian rhythm, and cancer through …

The productive exploration of chemical space is an enduring challenge in chemical biology
and medicinal chemistry. Natural products are biologically relevant, and their frameworks …

Following the discovery of cell penetrant pyridine-4-carboxylate inhibitors of the KDM4
(JMJD2) and KDM5 (JARID1) families of histone lysine demethylases (eg, 1), further …