To our delight, when the number of cyclo [DKP‐RGD] ligand moieties in the conjugates increases from 1 to 3, a clear trend of IC 50 decrease can be observed (entries 1–2→3→4), to reach an IC 50 lower than that of the free ligand 1 (entry 4 vs. entry 6).
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Multivalency Increases the Binding Strength of RGD Peptidomimetic-Paclitaxel Conjugates to Integrin α<sub>V</sub> β<sub>3</sub>.
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