Self-assembly of CXCR4 antagonist peptide-docetaxel conjugates for breast tumor multi-organ metastasis inhibition.

Chen LI; Jiayan Lang; Yazhou Wang; Zhaoxia Cheng; Mali ZU; Fenfen LI; Jingyi Sun; Yating Deng; Tianjiao JI; Guangjun Nie; Ying Zhao

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Self-assembly of CXCR4 antagonist peptide-docetaxel conjugates for breast tumor multi-organ metastasis inhibition.

Author: Chen LI ¹ ; Jiayan LANG ¹ ; Yazhou WANG ² ; Zhaoxia CHENG ¹ ; Mali ZU ¹ ; Fenfen LI ¹ ; Jingyi SUN ¹ ; Yating DENG ¹ ; Tianjiao JI ¹ ; Guangjun NIE ¹ ; Ying ZHAO ¹
Author Information

1. CAS Key Laboratory for Biomedical Effects of Nanomaterials & Nanosafety, CAS Center of Excellence in Nanoscience, National Center for Nanoscience and Technology, Beijing 100190, China.
2. Pancreas Centre, the First Affiliated Hospital of Nanjing Medical University, Nanjing 210029, China.
Publication Type:Journal Article
Keywords: CXCR4; Docetaxel; Drug delivery; Drug formulation; Peptide–drug conjugates; Triple-negative breast cancer; Tumor metastasis
From: Acta Pharmaceutica Sinica B 2023;13(9):3849-3861
CountryChina
Language:English
Abstract: As a representative chemotherapeutic drug, docetaxel (DTX) has been used for breast cancer treatment for decades. However, the poor solubility of DTX limits its efficacy, and the DTX based therapy increases the metastasis risk due to the upregulation of C-X-C chemokine receptor type 4 (CXCR4) expression during the treatment. Herein, we conjugated CXCR4 antagonist peptide (CTCE) with DTX (termed CTCE-DTX) as an anti-metastasis agent to treat breast cancer. CTCE-DTX could self-assemble to nanoparticles, targeting CXCR4-upregulated metastatic tumor cells and enhancing the DTX efficacy. Thus, the CTCE-DTX NPs achieved promising efficacy on inhibiting both bone-specific metastasis and lung metastasis of triple-negative breast cancer. Our work provided a rational strategy on designing peptide-drug conjugates with synergistic anti-tumor efficacy.