33869-65-7

Upstream product

• 33869-64-6 α-N-Benzoyl-ε-N-carbobenzoxy-L-lysin-tert-butylester 
• 63628-63-7 Nε-benzyloxycarbonyl-L-lysine tert-butyl ester 
• 98-88-4 benzoyl chloride 
• 1946-80-1 Bz-Lys(Z)-OH 

Relevant academic research and scientific papers

Nonpeptidic propargylamines as inhibitors of lysine specific demethylase 1 (LSD1) with cellular activity

Lysine demethylases play an important role in epigenetic regulation and thus in the development of diseases like cancer or neurodegenerative disorders. As the lysine specific demethylase 1 (LSD1/KDM1) has been strongly connected to androgen and estrogen dependent gene expression, it serves as a promising target for the therapy of hormone dependent cancer. Here, we report on the discovery of new small molecule inhibitors of LSD1 containing a propargylamine warhead, starting out from lysine containing substrate analogues. On the basis of these substrate mimicking inhibitors, we were able to increase potency by a combination of similarity-based virtual screening and subsequent synthetic optimization resulting in more druglike LSD1 inhibitors that led to histone hypermethylation in breast cancer cells.