ArticleNature communications2024
Blocker-SELEX: a structure-guided strategy for developing inhibitory aptamers disrupting undruggable transcription factor interactions.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Nucleic acid aptamers: new methods for selection, target validation, molecular diagnostics and therapeutics.Signal transduction and targeted therapy · 2026Review
- Multiple myeloma: A tale of deregulated transcription factors.HemaSphere · 2026Review
- Targeting Undruggable Protein Interactions with DNA Aptamers: Inhibition of the Interaction BetweenInternational journal of molecular sciences · 2026Article
- De novo design of functional nucleic acids of aptamers.Nature computational science · 2026Article
- Identifying a cancer therapeutic target: Cell-SELEX identifies a membrane protein for aptamer-mediated growth suppression.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Universal Baseline forbioRxiv : the preprint server for biology · 2026Article
- Advances in aptamer technology for target-based drug discovery.Journal of pharmaceutical analysis · 2026Review
- TSHR-Targeting Nucleic Acid Aptamer Treats Graves' Ophthalmopathy via Novel Allosteric Inhibition.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- L-RNA Aptamer-Based Tools for G-Quadruplex Structure: Identification, Characterization, and Application.Accounts of chemical research · 2025Article
- Selection and characterization of novel DNA aptamers targeting colorectal cancer cells with malignant potential.Analytical and bioanalytical chemistry · 2025Article
- Probing three-dimensional cyclooctatetraene for nucleobase modification in aptamer selection.Communications chemistry · 2025Article
- PTAdvanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Targeting eIF4A with RNA Aptamers Enhances Salt Stress Tolerance in Rice Through Modulation of Translation Initiation.Rice (New York, N.Y.) · 2025Article
- Aptamers as a New Frontier in Molecular Cancer Imaging Technologies.Chemical & biomedical imaging · 2025Review
- An eighteen-organ microphysiological system coupling a vascular network and excretion system for drug discovery.Microsystems & nanoengineering · 2025Article
Corrections and comments
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Authors and funding
21 authors.
Funding
Abstract
Despite the well-established significance of transcription factors (TFs) in pathogenesis, their utilization as pharmacological targets has been limited by the inherent challenges in modulating their protein interactions. The lack of defined small-molecule binding pockets and the nuclear localization of TFs do not favor the use of traditional tools. Aptamers possess large molecular weights, expansive blocking surfaces and efficient cellular internalization, making them compelling tools for modulating TF interactions. Here, we report a structure-guided design strategy called Blocker-SELEX to develop inhibitory aptamers (iAptamers) that selectively block TF interactions. Our approach leads to the discovery of iAptamers that cooperatively disrupt SCAF4/SCAF8-RNAP2 interactions, dysregulating RNAP2-dependent gene expression, which impairs cell proliferation. This approach is further applied to develop iAptamers blocking WDR5-MYC interactions. Overall, our study highlights the potential of iAptamers in disrupting pathogenic TF interactions, implicating their potential utility in studying the biological functions of TF interactions and in nucleic acids drug discovery.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.