ArticleProceedings of the National Academy of Sciences of the United States of America2021
Nucleic acid ligands act as a PAM and agonist depending on the intrinsic ligand binding state of P2RY2.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 14 citations in OpenAlex.
- Atomic, structural and molecular insights into GPCR ligand binding and signalling.Nature reviews. Molecular cell biology · 2026Review
- Efficient and specific selection of high-affinity DNA aptamers targeting μ-opioid receptor via functional extracellular vesicles.Communications biology · 2026Article
- Targeting tumor-associated G-protein coupled receptors: beyond single-axis inhibition toward multidimensional regulation.Cellular oncology (Dordrecht, Netherlands) · 2026Review
- Advances in aptamer technology for target-based drug discovery.Journal of pharmaceutical analysis · 2026Review
- Aptamers as target-specific recognition elements in drug delivery.Advanced drug delivery reviews · 2025Review
- Generation of RNA aptamers against chikungunya virus E2 envelope protein.Journal of virology · 2025Article
- A chimeric RNA consisting of siRNA and aptamer for inhibiting dengue virus replication.NAR molecular medicine · 2024Article
- Aptamer-functionalized nanomaterials (AFNs) for therapeutic management of hepatocellular carcinoma.Journal of nanobiotechnology · 2024Review
- Review
- Structure based innovative approach to analyze aptaprobe-GPC3 complexes in hepatocellular carcinoma.Journal of nanobiotechnology · 2022Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
G protein-coupled receptors (GPCRs) play diverse roles in physiological processes, and hence the ligands to modulate GPCRs have served as important molecules in biological and pharmacological approaches. However, the exploration of novel ligands for GPCR still remains an arduous challenge. In this study, we report a method for the discovery of nucleic acid ligands against GPCRs by an advanced RNA aptamer screening technology that employs a virus-like particle (VLP), exposing the GPCR of interest. An array of biochemical analyses coupled with a cell-based assay revealed that one of the aptamers raised against purinergic receptor P2Y2 (P2RY2), a GPCR, exhibits an activation potency to unliganded receptor and prohibits a further receptor activation by endogenous ligand, behaving like a partial agonist. However, the aptamer enhances the activity of intrinsic ligand-binding P2RY2, thereby acting as a positive allosteric modulator (PAM) to liganded receptor. Our findings demonstrate that the nucleic acid aptamer conditionally exerts PAM and agonist effects on GPCRs, depending on their intrinsic ligand binding state. These results indicate the validity of our VLP-based aptamer screening targeting GPCR and reemphasize the great potential of nucleic acid ligands for exploring the GPCR activation mechanism and therapeutic applications.
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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 OpenQuestion graph.