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Self-delivery of a peptide-based prodrug for tumor- targeting therapy

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分类：Q279[生物学—细胞生物学] Q74[生物学—分子生物学]
作者机构：[1]Key Laboratory of Biomedical Polymers of Ministry of Education & Department of Chemistry, Wuhan University, Wuhan 430072, China, [2]School of Chemistry and Materials Science, South-Central University for Nationalities, Wuhan 430074, China, [3]Hubei Collaborative Innovation Center for Advanced Organic Chemical Materials, Key Laboratory for the Green Preparation and Application of Functional Materials of Ministry of Education, Hubei University, Wuhan 430062, China
相关基金：This work was supported by the National Natural Science Foundation of China （Nos. 51125014, 51503227 and 51233003） and Natural Science Foundation of Hubei Province of China （Nos. 2014CFB696 and 2013CFA003）.

作者： Mengyun Peng[1], Siyong Qin[1,2], Huizhen Jia[1], Diwei Zheng[1,3], Lei Rong[1], Xianzheng Zhang[1]

关键词：肿瘤细胞, 靶向治疗, 交付, 分子自组装, 肽, 纳米结构, 过度表达, 整联蛋白, self-assembly,self-delivery,prodrug,tumor-targeting therapy

中文摘要：

一个新奇自我交付的 prodrug 系统为指向肿瘤的治疗被制作。在这 nanosystem， Arg-Gly-Asp-Ser (问候) tetrapeptide 被用来改进治疗学的索引到 integrin-overexpressing 肿瘤房间。antitumorous 药 camptothecin 被 20-O-succinyl 连接进一步添加到离氨酸的氨基的组并且 controllably 经由 hydrolytic 释放了劈开。进纤丝状的 nano 建筑学自我装配的 Prodrug 分子并且在皮下地被注入老鼠以后完成了自我交货的能力。赞成的恐水病的肉豆蔻酸酸的介绍自己组装并且提高了 prodrugs 的细胞的成为主观。在 vitro 并且在 vivo，研究证明自我装配的 nanofibers 能有效地指向 integrinoverexpressing 肿胀的房间并且经由调停 RGD 的特定的指向禁止肿瘤生长。因此，纤丝状的结构由于差的房间举起使治疗学的功效保持低的传统的想法能被质问。

英文摘要：

A novel self-delivered prodrug system was fabricated for tumor-targeting therapy. In this nanosystem, the Arg-Gly-Asp-Ser （RGDS） tetrapeptide was used to improve the therapeutic index to integrin-overexpressing tumor cells. The antitumorous drug camptothecin was further appended to the ε-amino group of lysine by 20-O-succinyl linkage and controllably released via hydrolytic cleavage. Prodrug molecules self-assembled into fibrillar nano-architectures and achieved the capability of self-delivery after being injected subcutaneously into mice. Introduction of hydrophobic myristic add favored the self-assembly and enhanced the cellular internalization of the prodrugs. In vitro and in vivo studies demonstrated that the self-assembled nanofibers could effectively target integrin- overexpressing tumorous cells and inhibit tumor growth via RGD-mediated specific targeting. Therefore, the traditional idea that fibrillar structures hold low therapeutic efficacy due to poor cell uptake can be challenged.