An MMP-2 sensitive and reduction-responsive prodrug amphiphile for actively targeted therapy of cancer by hierarchical cleavage

Xueni Zhang; Lihui Dai; Yumeng Ding; Qian Liu; Xiaoya Li; Mengting Liu; Meng Meng; Jie Pan; Rimo Xi; Yongmei Yin

doi:10.1039/D2CC05586D

An MMP-2 sensitive and reduction-responsive prodrug amphiphile for actively targeted therapy of cancer by hierarchical cleavage†

Xueni Zhang,^a Lihui Dai,^a Yumeng Ding,^a Qian Liu,^a Xiaoya Li,^a Mengting Liu,^a Meng Meng,^a Jie Pan,

*^b Rimo Xi*^a and Yongmei Yin

*^a

Author affiliations

* Corresponding authors

^a State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Haihe Education Park, 38 Tongyan Road, Tianjin 300353, China
E-mail: xirimo@nankai.edu.cn, yinyongmei@nankai.edu.cn

^b School of Chemical Engineering and Technology, Tiangong University, Tianjin 300387, China
E-mail: panjie@tiangong.edu.cn

Abstract

A hierarchically cleaved amphiphile, mPEG-pep-etcSS-CPT, was synthesized to pursue actively targeted cancer therapy through self-assembly. This micelle can respond to MMP-2 achieving dePEGylation and releasing RGD peptides to be internalized into targetable tumor cells. Inside the cell, free CPT could be released by reduction-response leading to cytotoxicity.

Chemical Communications

An MMP-2 sensitive and reduction-responsive prodrug amphiphile for actively targeted therapy of cancer by hierarchical cleavage†

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An MMP-2 sensitive and reduction-responsive prodrug amphiphile for actively targeted therapy of cancer by hierarchical cleavage

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