Octreotide Conjugates for Tumor Targeting and Imaging by Eduard Figueras, Ana Martins, Adina Borbély, Vadim Le Joncour, Paola Cordella, Raffaella Perego, Daniela Modena, Paolo Pagani, Simone Esposito, Giulio Auciello, Marcel Frese, Paola Gallinari, Pirjo Laakkonen, Christian Steinkühler, Norbert Sewald

“…In this study, we conjugated octreotide to cryptophycin, which is a highly cytotoxic depsipeptide, through the protease cleavable Val-Cit dipeptide linker using two different self-immolative moieties. The biological activity was investigated in vitro and the self-immolative part largely influenced the stability of the conjugates. …”
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Synthesis and Biological Evaluation of RGD–Cryptophycin Conjugates for Targeted Drug Delivery by Adina Borbély, Eduard Figueras, Ana Martins, Simone Esposito, Giulio Auciello, Edith Monteagudo, Annalise Di Marco, Vincenzo Summa, Paola Cordella, Raffaella Perego, Isabell Kemker, Marcel Frese, Paola Gallinari, Christian Steinkühler, Norbert Sewald

“…In this study, cryptophycin was conjugated to the cyclopeptide <i>c</i>(RGDfK), targeting integrin &#945;_v&#946;₃, across the protease-cleavable Val-Cit linker and two different self-immolative spacers. Plasma metabolic stability studies in vitro showed that our selected payload displays an improved stability compared to the parent compound, while the stability of the conjugates is strongly influenced by the self-immolative moiety. …”
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