molecules of the month


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

Structure of selective small molecule inhibitor of LOX-1, BI-0115
1 min read

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.

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