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Multivalent binding is often used to increase the strength of ligand–receptor interactions. In oncology, the development of multimeric conjugates aims at promoting a more efficient recognition of target antigens, possibly leading to better therapeutic performance. The affinity for integrin αVβ3 of multimeric conjugates (cyclo[DKP‐RGD])n‐Val‐Ala‐PTX (n=1–4) increases with the number of cyclo[DKP‐RGD]...
This work reports the synthesis of three multimeric RGD peptidomimetic‐paclitaxel conjugates featuring a number of αVβ3 integrin ligands ranging from 2 to 4. These constructs were assembled by conjugation of the integrin αVβ3 ligand cyclo[DKP‐RGD]‐CH2NH2 with paclitaxel via a 2′‐carbamate with a self‐immolative spacer, the lysosomally cleavable Val‐Ala dipeptide linker, a multimeric scaffold, a triazole...
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