Fig. 1: Cell based high throughput screening assay on LOX-1. | Communications Chemistry

Fig. 1: Cell based high throughput screening assay on LOX-1.

From: A small-molecule inhibitor of lectin-like oxidized LDL receptor-1 acts by stabilizing an inactive receptor tetramer state

Fig. 1: Cell based high throughput screening assay on LOX-1.

a Representative fluorescence microscopic pictures (n = 16) of AF647 labeled human oxLDL uptake into a CHO-K1 cell line with doxycycline inducible expression of the human LOX-1 receptor (-/+ DOX). The length of the scale bar corresponds to 20 µM. blue: Hoechst 33342, red: AF647-oxLDL b The HTS assay principle is based on the cellular internalization of AF594-labeled human oxLDL. AF594-oxLDL uptake in CHO-TREx-hLOX-1 is blocked by 30 nM mAb-LOX-1 (P value < 0.0001). The assay shows a window of factor 10 between background (-Tet+Alexa oxLDL) and full induction (+Tet+Alexa oxLDL). The error bars indicate the standard deviation of the measurements. c Representative example of a concentration response curve of BI-0115 with an IC50 of 7.2 µM in the LOX-1 cellular uptake assay (n = 2 for each concentration, R2 = 0.98). The chemical structure of BI-0115 is indented.

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