Research Papers:

Controlled release strategy of paclitaxel by conjugating to matrix metalloproteinases-2 sensitive peptide

Changjiang Huang, Xiulin Yi, Dexin Kong, Ligong Chen and Gong Min _

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Oncotarget. 2016; 7:52230-52238. https://doi.org/10.18632/oncotarget.10735

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Changjiang Huang1,2, Xiulin Yi2, Dexin Kong3, Ligong Chen1, Gong Min3,4

1School of Chemical Engineering and Technology, Tianjin University, Tianjin, China

2Tianjin Institute of Pharmaceutical Research, Tianjin, China

3School of Pharmacy, Tianjin Medical University, Tianjin, China

4Department of Oncology, University of Oxford, Oxford, UK

Correspondence to:

Gong Min, email: [email protected]

Ligong Chen, email: [email protected]

Keywords: matrix metalloproteinase, tumor targeting peptide, drug conjugate, paclitaxel, tumor metastasis

Received: April 25, 2016     Accepted: May 29, 2016     Published: July 20, 2016


Peptide drug conjugates offer a novel strategy to achieve controlled drug release. This approach avoids the clinical obstacles of non-specific toxicity and overall drug resistance of conventional cytotoxic agents, such as paclitaxel. MMP2 plays important functions in tumour proliferation and metastasis. Herein, we conjugated the paclitaxel with a hexapeptide which is specific recognized by MMP2 protein. The conjugate is dissociated upon the MMP2 specific proteolysis at COOH terminal of hexapeptide, PVGLIG.

The results clearly indicated that the PVGLIG-paclitaxel conjugate significantly enhanced the tumor specificity against HT-1080 and U87-MG tumour cells. Our finding suggested that the hexapeptide PVGLIG is capable to act as a controlled and sustained drug carrier of paclitaxel for the treatment against tumour proliferation and metastasis with high MMP2 expression.

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