Development and Utilization of Novel Transglutaminase 2 Inhibitors for Potential Treatment of Autoimmune Disease and Gastrointestinal Disorder.

Transglutaminases, classified explicitly as "protein-glutamine: amine γ-glutamyl transferases", catalyze the formation of isopeptide bonds between the γ-amino group of lysine and the γ-glutamyl group of glutamine, leading to the release of ammonia. These enzymes play pivotal roles in diverse medical conditions such as cardiovascular, autoimmune, neurodegenerative, and dermatological diseases, as well as in wound healing and inflammatory diseases. This Patent Highlight presents novel inhibitors of transglutaminases, specifically transglutaminase 2 (TG2), and their synthetic processes. In addition, these inhibitors are effective treatments for diseases linked to TG2, such as celiac disease and fibrotic disorders. Therefore, these inhibitors can be active agents in pharmaceutical treatments.