DESCRIPTION BI-0115 is a small molecule inhibitor of LOX-1 (lectin-like oxidized LDL receptor-1). BI-0115 displays a good selectivity profile and a relatively clean Eurofins Safety Panel 44™ profile with an acceptable in vitro profile that showed clear inhibition of oxLDL internalization.1 LOX-1 is a scavenger receptor that mediates the uptake of oxLDL by vascular cells that has been shown to lead to plaque formation in arteries.2 A first co-crystal structure of LOX-1 and BI-0115 provided insights into a new mechanism of LOX-1 inhibition with two small molecule inhibitors placed at a head-to-head interface of two LOX-1 dimers. The inhibitory mechanism is mediated by the stabilization of a protein-protein interaction.1 We think that BI-0115 is a valuable chemical probe to study LOX-1 mediated signal transduction pathways and cellular effects in different pathogenic pathways. Furthermore, the mechanism of LOX-1 inhibition describes a new way of targeting C-type lectin like receptors and might strongly influence drug discovery on this protein family. (opnMe Portal)