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Novel Aptamer-Drug Conjugate for Targeted Therapy in Triple-Negative Breast Cancer
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DOI：10.1021/acs.jmedchem.5c00492.png)
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Abstract
En 中文
Triple-negative breast cancer (TNBC) is a highly aggressive malignancy lacking targeted therapeutic modalities. Aptamers are promising targeting agents with high specificity and affinity. In this study, we identified a chemically modified nucleic acid aptamer (AptT1) that specifically recognized and internalized into TNBC cells. Mechanistic studies revealed that ANXA2 was an essential protein in facilitating AptT1 internalization via clathrin-mediated endocytosis. Furthermore, we constructed an aptamer-drug conjugate (ApDC) to selectively deliver a cytotoxic agent (SN38) to TNBC cells and demonstrated significant efficacy and safety in a TNBC xenograft model. These findings suggest that AptT1-based ApDC holds great potential as an innovative targeted strategy for TNBC.
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