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. 2021 Mar 3;13(8):9436-9444.
doi: 10.1021/acsami.0c18282. Epub 2020 Dec 11.

Aptamer-Peptide Conjugates as _targeted Chemosensitizers for Breast Cancer Treatment

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Aptamer-Peptide Conjugates as _targeted Chemosensitizers for Breast Cancer Treatment

Yan Tan et al. ACS Appl Mater Interfaces. .

Abstract

High levels of heat shock protein 70 (HSP70) in tumors are commonly associated with poor prognosis, enhanced doxorubicin (DOX)-induced cardiotoxicity, and even drug resistance in DOX-related cancer chemotherapy. Several peptides possess remarkable protein inhibition and chemosensitization effects, which are attributed to their specific _targeting ability against HSP70. However, the inherent poor cell penetration capacity considerably restricts the biomedical applications of these peptides. We herein describe the design and development of anti-MUC1 aptamer-peptide conjugates (ApPCs) as _targeted chemosensitizers to overcome the above-mentioned issues. Moreover, DOX could be loaded on the ApPC to deliver the DOX-enclosed agent ApPC-DOX, which simultaneously acts as a _targeted chemosensitizer and anticancer agent for combating drug resistance in breast cancer therapy. This innovative, engineered biocompatible conjugate not only enhances the sensitivity of DOX-resistant cells but also alleviates cardiotoxicity of DOX in vivo, highlighting the success of this _targeted chemosensitizer strategy.

Keywords: HSP70; aptamer; cardiotoxicity; peptide; _targeted chemosensitizer; _targeted drug delivery.

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