Figure 1.
Design and characterization of FAP-activated prodrugs and analog controls. (A) Design of FAP-activated prodrugs and their non-FAP cleavable analog controls. (B) FAP-mediated activation of prodrugs ex vivo. The active form of the drugs (A- or S-12ADT, respectively) were produced from both FAP-cleavable prodrugs (ASGPAGP-A12ADT and ERGETGP-S12ADT), but not from the non-FAP cleavable prodrug analogs. (p) represents the D-isomer of proline and (µ) represents morpholino-cap on the NH2-terminus of the prodrug peptide sequence.