Design and synthesis of novel dual-cyclic RGD peptides for αvβ3 integrin targeting
Design and synthesis of novel dual-cyclic RGD peptides for αvβ3 integrin targeting
复制标题
用于α(v)β(3)整合素靶向的新型双环RGD肽的设计和合成
DOI：
10.1016/j.bmcl.2019.01.043
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发表时间：
2019-04-01
影响因子：
2.7
通讯作者：
Le, Zhiping
中科院分区：
文献类型：
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作者：
Liu, Junjie;Cheng, Xiaozhong;Le, Zhiping
RGD环肽与整合素α（v）β（3）的特异性结合在肿瘤靶向给药方面引起了广泛的研究兴趣。本文设计并合成了一系列双环RGD-肽衍生物作为药物载体，用于alpha（v）beta（3）靶向。三种新的肽显示出良好的细胞粘附抑制作用，其中，P3显示出7倍的IC 50相比，环（RGDfK）。载药细胞毒性实验和显像实验表明，双环RGD肽具有良好的肿瘤靶向性。本工作为设计新型RGD肽提供了一种新的策略。
The specific binding of RGD cyclic peptide with integrin alpha(v)beta(3 )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 alpha(v)beta(3) 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.