Fig. 1.

Generation of MMP-14 inhibitory Fab 1F8 by CDR-H3 grafting. (A) Scheme of library design. MMP-14 inhibitory motif is inserted into CDR-H3 for library construction. Motif flanking residuals and other five CDRs are diversified. (B) CDR amino acid sequences of isolated Fab 1F8. (C) Dose–response binding affinity curves (EC₅₀) of purified Fab 1F8 and Fab DX-2400, a potent MMP-14 inhibitor (Devy et al., 2009). (D) Inhibition function of purified Fabs 1F8 and DX-2400. An 1 μM quenched-fluorescent substrate peptide and 1 nM cdMMP-14 were used in förster resonance energy transfer (FRET) inhibition assays. K_I values were calculated based on the models described in Cer et al. (2009).