Fig. 4
From: Ab locks for improving the selectivity and safety of antibody drugs
Endogenous LAP peptide is a widely applied Ab lock for enhancing the selectivity of Ab drugs to the disease site. Chen et al. used latency-associated peptide (LAP) derived from transforming growth factor-β (TGF-β) as a widely applied Ab lock and connected it to the N-terminal of the heavy chain of Ab drugs (e.g., the anti-EGFR Ab, Cetuximab, or the anti-TNF-α Ab, Infliximab) by a substrate peptide for MMP-2 (i.e., GPLGVR). The LAP domain reduced the antigen binding activity of Ab drugs and was selectively activated by MMP-2 for specific antigen targeting at the disease site. Ab, antibody; EGFR, epidermal growth factor receptor; TNF-α, tumor necrosis factor α; MMP, matrix metalloproteinase