Tranylcypromine

Tranylcypromine hydrochloride , also known as 2-PCPA, is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110), a histone demethylase, and non-hydrazine monoamine oxidases (MAO). Histones contain unstructured N-terminal residues that are the site of numerous post-translational modifications, involving acetylation, ubiquitination, methylation, and sumoylation to produce a specific gene regulatory outcome. Complementary enzymes catalyze the addition and removal of these modifications as needed. The amine oxidase domain-containing enzyme lysine-specific demethylase 1 (LSD1) is a part of one of two classes of histone demethylases capable of demethylating lysine residues. LSD1 shares similar catalytic sites with monoamine oxidases (MAO) A and B. Treatment of P19 embryonal carcinoma cells with tranylcypromine resulted in global increase in H3K4 methylation as well as transcriptional derepression of the pluripotent stem cell marker Oct43.