Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability

Inhibition of the angiotensin II type 2 receptor AT 2 R is a novel therapeutic strategy for glioblastoma

“…Studies of AT 2 R are challenging because of its generally low expression and knowledge of expression in human tumors is sparse. However, a limited number of selective AT 2 R ligands have been described, including the nonpeptide antagonist PD123319 (11) and derivatives such as EMA401 (2), the partial agonist CGP42112A (12), the nonpeptide agonist compound 21 (13), and more recently, our highly selective agonist [Y] 6 -AII (2,(14)(15)(16).…”