2. Academic Validation
  3. Novel Aptamer-Drug Conjugate for Targeted Therapy in Triple-Negative Breast Cancer

Novel Aptamer-Drug Conjugate for Targeted Therapy in Triple-Negative Breast Cancer

  • J Med Chem. 2025 Jul 20. doi: 10.1021/acs.jmedchem.5c00492.
Feng Xu 1,  Jingtong Xu 1,  Feng Han 2 3,  Ke Wang 1,  Fulong Wang 3,  Hanyang Yu 3,  Xiaoxiang Guan 1 4
Affiliations

Affiliations

  • 1 Department of Oncology, The First Affiliated Hospital of Nanjing Medical University, Nanjing 210029, China.
  • 2 State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing, Jiangsu 210023, China.
  • 3 State Key Laboratory of Coordination Chemistry, Department of Biomedical Engineering, College of Engineering and Applied Sciences, Chemistry and Biomedicine Innovation Center (ChemBIC), Nanjing University, Nanjing, Jiangsu 210023, China.
  • 4 Jiangsu Key Lab of Cancer Biomarkers, Prevention and Treatment, Collaborative Innovation Center for Personalized Cancer Medicine, Nanjing Medical University, Nanjing 210029, China.
PMID: 40685636 DOI: 10.1021/acs.jmedchem.5c00492
Abstract

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.

Figures
Products
Inhibitors & Agonists
Other Products