Histone N ε-methyl lysine demethylases KDM2/7 have been identified as potential targets for
cancer therapies. On the basis of the crystal structure of KDM7B, we designed and prepared …

We report the stereoselective synthesis and biological activity of a novel series of
tranylcypromine (TCPA) derivatives (14a–k, 15, 16), potent inhibitors of KDM1A. The new …

Histone lysine demethylases (KDMs) play a key role in epigenetic regulation and KDM5A
and KDM5B have been identified as potential anti-cancer drug targets. Using structural …

Abstract Lysine demethylase 5B (KDM5B) is a histone demethylase identified in 2007, which
is responsible for erasing H3K4me2/3 activation marker. It participates in multiple repressive …

Histone lysine demethylases (KDMs) have drawn much attention as targets of therapeutic
agents. KDM5 proteins, which are Fe (II)/α-ketoglutarate-dependent demethylases, are …

Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related
processes. Herein, we describe our discovery of a series of potent KDM4 inhibitors that are …

This communication describes the identification and optimization of a series of pan-KDM5
inhibitors derived from compound 1, a hit initially identified against KDM4C. Compound 1 …

Lysine-specific histone demethylase 3 (KDM3) subfamily proteins are H3K9me2/me1
histone demethylases that promote gene expression. The KDM3 subfamily primarily consists …

Histone demethylation is a vital process in epigenetic regulation of gene expression. A
number of histone demethylases are present to control the methylated states of histone …

Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of
gene expression, yet there are few selective, cell‐permeable inhibitors or suitable tool …