Lysine-specific histone demethylases (KDM) Library

ChemDiv’s Library of Lysine (K)-Specific Demethylase (KDM) Inhibitors contains 3,856 compounds.

Lysine-specific histone demethylase (LSD) also known as lysine (K)-specific demethylase (KDM) plays a marked role in drug discovery due to its critical function in epigenetic regulation. These enzymes selectively remove methyl groups from lysine residues on histone proteins, influencing gene expression by altering chromatin structure. Dysregulation of KDM activity is linked to various diseases, including cancer, neurological disorders, and developmental abnormalities. Consequently, targeting KDMs offers a therapeutic strategy for modulating gene expression patterns that are aberrant in these diseases. The development of inhibitors or modulators of Ms is thus a significant area of focus in drug discovery, aiming to correct epigenetic imbalances associated with disease pathogenesis.

The current strategy for developing inhibitors or modulators of KDMs in drug discovery primarily involves targeting the enzymatic active sites to specifically disrupt their demethylase activity. This approach is based on our insights into the structure and function of these enzymes, gained through advanced techniques like crystallography and molecular modeling. In developing this library we have been focusing on creating diverse small molecule inhibitors that can bind to KDMs, thereby preventing them from removing methyl groups from histone proteins. This blockage can alter gene expression patterns that are dysregulated in various diseases, particularly cancers and neurological disorders. Further, in clinical therapy, KDMs inhibitors could be used to reprogram aberrant epigenetic landscapes, potentially reactivating tumor suppressor genes in cancer or modulating genes implicated in neurological diseases. As these therapies progress through clinical trials, they offer a promising avenue for treating diseases with an epigenetic basis, representing a novel class of targeted therapeutics.

Detailed information about our library of lysine (K)-specific demethylase (KDM) Inhibitors is provided in the slide deck above.