Rational Optimization of a Bispecific Ligand Trap Targeting EGF Receptor Family Ligands

Table 1 Affinity-optimized mutants are more potent than their parent forms in inhibition of growth factor–induced EGFR and HER3 phosphorylation

^aShown are the EC₅₀ values for HER/Fc-mediated inhibition of receptor phosphorylation. Serum-starved cells were treated with 3 nM EGF or TGF-α (N87 cells), or with NRG1-β (MCF7 cells), in the presence of increasing concentrations of the homodimer and heterodimer inhibitors. Cells were lysed 10 min later. Lysates were analyzed for the presence of phosphorylated EGFR or HER3 using a quantitative phosphotyrosine-ELISA assay. ^bNT: not tested.

ISSN: 1528-3658