Figure 1.

Structure of legumain and αvβ3 integrin inhibitors, the antibody programming agents, and chemically programmed antibodies. Compounds 3–5 reacted with Ab 38C2 at 37 °C for 2–24 h affording anti-legumain, anti-integrin cpAbs (38C2-3, 38C2-4) and cp-bsAb (38C2-5). Compound [4a] is an intermediate produced by an in situ retro aldol reaction of compound 4 before the latter reacts with the Ab. Key: legumain and integrin inhibitors are portrayed in green and blue, respectively.