Investigation of the binding characteristics between ligands and epidermal growth factor receptor by cell membrane chromatography.

摘要: The binding property between a ligand and its receptor is very important for numerous biological processes. In this study, we developed high epidermal growth factor (EGFR)-expression cell membrane chromatography (CMC) method to investigate the characteristics EGFR ligands gefitinib, erlotinib, canertinib, afatinib, vandetanib. Competitive analysis using gefitinib as marker was used interactions that occurred at specific sites on EGFR. ability of displacement measured from HEK293-EGFR/CMC column occupied by these ligands, which revealed following order: (KD, 8.49 ± 0.11 × 10-7  M) > erlotinib 1.07 ± 0.02 × 10-6  M) > canertinib 1.41 ± 0.07 × 10-6  M) > afatinib 1.80 ± 0.12 × 10-6  M) > vandetanib 1.99 ± 0.03 × 10-6  M). This order corresponded with values estimated frontal scores obtained molecular docking. Furthermore, thermodynamic indicated hydrogen bond or Van der Waals force main interaction in process all 5 ligands. Overall, results demonstrate CMC could be an effective tool receptors.