selective LOX-1 lectin inhibitor/tetramerizer
in vitro activity and co-crystallized in tetramer
from 1M cmpd cellular HTS
Commun. Chem., Jun. 10, 2020
Boehringer Ingelheim, Biberach, DE
BI-0115 inhibits the C-type lectin family member lectin-like oxidized LDL-receptor-1 (LOX-1) by stabilizing an inactive tetrameric form of the protein. Interestingly, co-crystollography demonstrates that inter-ligand interactions between two BI-0115 molecules contribute to the dimerization of LOX-1 homodimers.