Proteins are the main targets of most drugs; however, system-wide methods to monitor
protein activity and function are still underused in drug discovery. Novel biochemical …

The identification of heterozygous neomorphic isocitrate dehydrogenase (IDH) mutations
across multiple cancer types including both solid and hematologic malignancies has …

Since their discovery in the 1960s, the family of Fe (II)/2-oxoglutarate-dependent
oxygenases has undergone a tremendous expansion to include enzymes catalyzing a vast …

Gene mutations are strongly associated with tumor progression and are well known in
cancer development. However, recently discovered epigenetic alterations have shown the …

Gliomas and leukemias remain highly refractory to treatment, thus highlighting the need for
new and improved therapeutic strategies. Mutations in genes encoding enzymes involved in …

Decreased erythropoietin (EPO) production, shortened erythrocyte survival, and other
factors reducing the response to EPO contribute to anemia in patients who have a variety of …

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 …

The human 2-oxoglutarate (2OG)-and Fe (II)-dependent oxygenases factor inhibiting
hypoxia-inducible factor-α (FIH) and HIF-α prolyl residue hydroxylases 1–3 (PHD1–3) …

Alterations in mitochondrial metabolism influence cell differentiation and growth. This
process is regulated by the activity of 2-oxoglutarate (2OG)-dependent dioxygenases …

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 …