Design and synthesis of novel dual-cyclic RGD peptides for αvβ3 integrin targeting |
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| Authors: | Junjie Liu Xiaozhong Cheng Xiaobo Tian Dongliang Guan Jiwei Ao Zhimeng Wu Wei Huang Zhiping Le |
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| Institution: | 1. Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, PR China;2. CAS Key Laboratory of Receptor Research, CAS Center for Excellence in Molecular Cell Science, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai 201203, PR China;3. Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, PR China;4. University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing 100049, PR China |
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| Abstract: | The specific binding of RGD cyclic peptide with integrin αvβ3 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 αvβ3 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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| Keywords: | RGD cyclic peptide Tumor-targeting Cyclo(RGDfK) Adhesion inhibition |
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