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Overview
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BI-0115 is a highly selective inhibitor for the lectin-like oxidised low-density lipoproteins (LDL) receptor 1 (LOX-1). In vitro, BI-0115 inhibits internalisation of oxidised LDL (oxLDL) with IC50 of 5.4 µM. The crystal studies revealed that BI-0115 glues two LOX-1 dimers together, resulting in blocked access of oxLDL. LOX-1 is a Ctype lectin-like receptor expressed on endothelial cells, macrophages and vascular smooth muscle. It is responsible for the regulation, internalisation and degradation of oxidised low-density lipoproteins (oxLDL). BI-0115 is a novel inhibitor to LOX-1 and is a valuable tool to study LOX-1 biology, and their role in diseases, such as, cancer and atheroschelerosis.
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Overview