设计并合成新型双环 RGD 肽以靶向 αβ 整合素。
Design and synthesis of novel dual-cyclic RGD peptides for αβ integrin targeting.
机构信息
Department of Chemistry, Nanchang University, 999 Xuefu Avenue, Nanchang 330031, PR China; 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.
Key Laboratory of Carbohydrate Chemistry & Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, PR China.
出版信息
Bioorg Med Chem Lett. 2019 Apr 1;29(7):896-900. doi: 10.1016/j.bmcl.2019.01.043. Epub 2019 Feb 1.
The specific binding of RGD cyclic peptide with integrin αβ 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 αβ targeting. Three novel peptides showed excellent cell adhesion inhibition effect, in which, P3 exhibited 7-fold enhancement in IC 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.
精氨酸-甘氨酸-天冬氨酸（RGD）环肽与整合素 αβ 的特异性结合引起了人们对肿瘤靶向药物传递的极大研究兴趣。在此，我们设计并合成了一系列作为靶向 αβ 的药物载体的双环 RGD-肽衍生物。三种新型肽表现出优异的细胞黏附抑制作用，其中 P3 与环（RGDfK）相比，IC 提高了 7 倍。载药细胞毒性实验和成像实验表明，这种双环 RGD 肽具有良好的肿瘤靶向作用。这项工作为新型 RGD 肽的设计提供了新策略。
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