National Center for
2I47: Crystal Structure Of Catalytic Domain Of Tace With Inhibitor
Bioorg. Med. Chem. Lett. (2007) 17 p.34-39
By focusing on the P1 portion of the piperidine beta-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.