SEN177

SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases[1][2][3].

[1]Cecilia Pozzi, et al. The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders. J Biol Inorg Chem. 2018 Dec;23(8):1219-1226.|[2]Maria Jimenez-Sanchez, et al. siRNA screen identifies QPCT as a druggable target for Huntington's disease. Nat Chem Biol. 2015 May;11(5):347-354.|[3]Baumann N, et al. Enhancement of epidermal growth factor receptor antibody tumor immunotherapy by glutaminyl cyclase inhibition to interfere with CD47/signal regulatory protein alpha interactions. Cancer Sci. 2021 Aug;112(8):3029-3040.