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 …

Despite the encouraging clinical progress of chemotherapeutic agents in cancer treatment,
innovation and development of new effective anticancer candidates still represents a …

Molecular docking is a computational chemistry method which has become essential for the
rational drug design process. In this context, it has had great impact as a successful tool for …

Targeted therapy for acute myeloid leukemia (AML) is an effective strategy, but currently
there are very limited therapeutic targets for AML treatment. Histone lysine specific …

Recently, despite the great success achieved by the so‐called “magic bullets” in the
treatment of different diseases through a marked and specific interaction with the target of …

Due to the increasing costs and time consuming for new drug discovery, a large number of
pharmaceutical firms have chosen to modify the existing drug molecules for repositioning …

Abstract Lysine specific demethylase 1 (LSD1) and Histone deacetylases (HDACs) are
promising drug targets for cancers. Recent studies reveal an important functional interplay …

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 …

Since the first lysine-specific demethylase (KDM), lysine-specific demethylase 1 (LSD1), was
characterized in 2004, several families of KDMs have been identified. LSD1 can specifically …

The balance of methylation levels at histone H3 lysine 4 (H3K4) is regulated by KDM1A
(LSD1). KDM1A is overexpressed in several tumor types, thus representing an emerging …