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Updated: May 24, 2026
A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
Published on: September 13, 2022
Novel MUC1 aptamer selectively delivers cytotoxic agent to cancer cells in vitro
Yan Hu1, Jinhong Duan, Qimin Zhan
1Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Abstract:
Chemotherapy is a primary treatment for cancer, but its efficacy is often limited by the adverse effects of cytotoxic agents. Targeted drug delivery may reduce the non-specific toxicity of chemotherapy by selectively directing anticancer drugs to tumor cells. MUC1 protein is an attractive target for tumor-specific drug delivery owning to its overexpression in most adenocarcinomas. In this study, a novel MUC1 aptamer is exploited as the targeting ligand for carrying doxorubicin (Dox) to cancer cells. We developed an 86-base DNA aptamer (MA3) that bound to a peptide epitope of MUC1 with a K(d) of 38.3 nM and minimal cross reactivity to albumin. Using A549 lung cancer and MCF-7 breast cancer cells as MUC1-expressing models, MA3 was found to preferentially bind to MUC1-positive but not MUC1-negative cells. An aptamer-doxorubicin complex (Apt-Dox) was formulated by intercalating doxorubicin into the DNA structure of MA3. Apt-Dox was found capable of carrying doxorubicin into MUC1-positive tumor cells, while significantly reducing the drug intake by MUC1-negative cells. Moreover, Apt-Dox retained the efficacy of doxorubicin against MUC1-positive tumor cells, but lowered the toxicity to MUC1-negative cells (P<0.01). The results suggest that the MUC1 aptamer may have potential utility as a targeting ligand for selective delivery of cytotoxic agent to MUC1-expressing tumors.
Insights
Researchers developed a novel MUC1 aptamer (MA3) for targeted cancer therapy. This aptamer selectively delivers doxorubicin (Dox) to MUC1-expressing tumors, reducing toxicity to healthy cells.
Area of Science:
- Biotechnology
- Molecular Biology
- Oncology
Background:
- Chemotherapy's efficacy is limited by cytotoxic agent side effects.
- Targeted drug delivery aims to reduce non-specific toxicity by directing drugs to tumor cells.
- MUC1 protein is overexpressed in most adenocarcinomas, making it a promising target for tumor-specific delivery.
Purpose of the Study:
- To develop and evaluate a novel MUC1 aptamer for targeted delivery of doxorubicin (Dox) to cancer cells.
- To assess the specificity and efficacy of the aptamer-drug complex in MUC1-positive versus MUC1-negative cells.
Main Methods:
- Development of an 86-base DNA aptamer (MA3) targeting a MUC1 peptide epitope.
- Formulation of an aptamer-doxorubicin complex (Apt-Dox) by intercalating doxorubicin into the MA3 DNA structure.
- Evaluation of MA3 binding specificity to MUC1-positive (A549, MCF-7) and MUC1-negative cells.
Main Results:
- MA3 demonstrated specific binding to MUC1-positive cells with a K(d) of 38.3 nM and minimal cross-reactivity to albumin.
- Apt-Dox successfully delivered doxorubicin into MUC1-positive tumor cells while reducing uptake in MUC1-negative cells.
- Apt-Dox maintained doxorubicin's efficacy against MUC1-positive cells and significantly lowered its toxicity to MUC1-negative cells (P<0.01).
Conclusions:
- The MUC1 aptamer (MA3) shows potential as a targeting ligand for selective delivery of cytotoxic agents.
- This targeted approach can enhance chemotherapy efficacy and reduce adverse effects in MUC1-expressing tumors.
