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Molecular structures of the αvβ3 integrin‐targeted conjugate cyclo(DKP‐RGD)‐NPV‐PTX (5), of its diastereoisomer cyclo(DKP‐RGD)‐NPv‐PTX (6), whose linker bears d‐valine (v), and of the uncleavable conjugate cyclo(DKP‐RGD)‐unc‐PTX (7). Mechanism of PTX release upon linker cleavage is depicted, consisting in the fast 1,6‐elimination of the p‐aminobenzyl carbamate 8, followed by amine cyclization in compound 10, which results in the formation of cyclic urea 11 and free Paclitaxel (12).
