Yan Xiong, Holger Greschik, Catrine Johansson, Ludwig Seifert, Vicki Gamble, Kwang-Su Park, Vincent Fagan, Fengling Li, Irene Chau, Masoud Vedadi, Cheryl H Arrowsmith, Paul Brennan, Oleg Fedorov, Manfred Jung, Gillian Farnie, Jing Liu, Udo Oppermann, Roland Schüle, Jian Jin
The methyl-lysine reader protein SPIN1 plays important roles in various human diseases. However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly active SPIN1 inhibitors have been developed. We previously reported that our G9a/GLP inhibitor UNC0638 weakly inhibited SPIN1. Here, we present our comprehensive structure-activity relationship study that led to the discovery of compound 11 , a dual SPIN1 and G9a/GLP inhibitor, and compound 18 (MS8535), a SPIN1 selective inhibitor...
March 27, 2024: Journal of Medicinal Chemistry