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Design and synthesis of novel dual-cyclic RGD peptides for α v β 3 integrin targeting.
Bioorganic & Medicinal Chemistry Letters 2019 Februrary 2
The specific binding of RGD cyclic peptide with integrin αv β3 attracts great research interest for tumor-targeting drug delivery. Herein, we designed and synthesized a series of dual-ring RGD-peptide derivatives as a drug carrier for αv β3 targeting. Three novel peptides showed excellent cell adhesion inhibition effect, in which, P3 exhibited 7-fold enhancement in IC50 compared with cyclo(RGDfK). Drug-loaded cytotoxicity experiment and imaging experiment indicated that such dual-cyclic RGD peptides have good tumor targeting effects. This work provides a new strategy for the design of novel RGD peptides.
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