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Updated: Apr 1, 2026
A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
Published on: September 13, 2022
Selection and Application of DNA Aptamer Against Oncogene Amplified in Breast Cancer 1
1State Key Laboratory of Physical Chemistry of Solid Surfaces, The MOE Key Laboratory of Spectrochemical Analysis & Instrumentation, Collaborative Innovation Center of Chemistry for Energy Materials, Key Laboratory for Chemical Biology of Fujian Province, and Department of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, 361005, People's Republic of China.
Abstract:
Amplified in breast cancer 1 (AIB1), also known as steroid receptor coactivator 3 (SRC-3), is a transcriptional coactivator that interacts with nuclear receptors and other transcription factors to enhance their effects on target gene transcription. AIB1, which acts as a major oncogene, is highly expressed in many human cancers, and has been demonstrated to be a key regulator for tumor initiation, progression, metastasis, invasion, and survival. Recruitment of the transcriptional factor CBP/p300 by CBP/p300-interaction domain (CID) of AIB1 is essential for its transcriptional activation function. In this research, we isolated a DNA aptamer AY-3 that binds to AIB1-CID from a random oligonucleotide library using in vitro screening technology-Systematic Evolution of Ligands by EXponential enrichment (SELEX). The binding affinity of the aptamer to AIB1-CID fusion protein is in the nanomolar range. More importantly, the aptamer was found to disrupt in the interaction between p300 and AIB1. This aptamer has great potential to serve as a therapeutic agent for cancer by inhibiting the coactivation of AIB1.
Insights
Researchers developed a DNA aptamer, AY-3, that targets Amplified in breast cancer 1 (AIB1). This aptamer disrupts AIB1
Area of Science:
- Molecular Biology
- Cancer Research
- Drug Discovery
Background:
- Amplified in breast cancer 1 (AIB1), also known as steroid receptor coactivator 3 (SRC-3), is a transcriptional coactivator and oncogene.
- AIB1 is highly expressed in various cancers and promotes tumor initiation, progression, metastasis, invasion, and survival.
- The interaction between AIB1's CBP/p300-interaction domain (CID) and CBP/p300 is crucial for AIB1's transcriptional activation function.
Purpose of the Study:
- To isolate a novel molecule that specifically binds to the AIB1-CID.
- To evaluate the potential of this molecule as a therapeutic agent for cancer by inhibiting AIB1 coactivation.
Main Methods:
- Systematic Evolution of Ligands by EXponential enrichment (SELEX) was employed to screen a random oligonucleotide library.
- Isolation of a DNA aptamer, designated AY-3, that specifically binds to the AIB1-CID.
- Assessment of the binding affinity of the aptamer to the AIB1-CID fusion protein.
Main Results:
- The DNA aptamer AY-3 was successfully isolated, demonstrating specific binding to the AIB1-CID.
- The aptamer exhibits binding affinity in the nanomolar range.
- Crucially, AY-3 was shown to disrupt the interaction between AIB1 and the transcriptional factor p300.
Conclusions:
- The DNA aptamer AY-3 is a high-affinity binder to AIB1-CID.
- AY-3 effectively inhibits the critical interaction between AIB1 and p300.
- This aptamer holds significant therapeutic potential for treating cancers driven by AIB1 overexpression.
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