ArticleBiochemistry2010
Potent and selective inhibition of the open-channel conformation of AMPA receptors by an RNA aptamer.
Article in Biochemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- GluK2 kainate receptor subunit-selective, potentiating RNA aptamer.Scientific reports · 2025Article
- Deciphering the Biophysical Properties of Ion Channel Gating Pores by Coumarin-Benzodiazepine Hybrid Derivatives: Selective AMPA Receptor Antagonists.Molecular neurobiology · 2024Article
- Testing of the therapeutic efficacy and safety of AMPA receptor RNA aptamers in an ALS mouse model.Life science alliance · 2022Article
- RNA aptamers for AMPA receptors.Neuropharmacology · 2021Review
- A kainate receptor-selective RNA aptamer.The Journal of biological chemistry · 2020Article
- Nucleic Acid Aptamers for Molecular Therapy of Epilepsy and Blood-Brain Barrier Damages.Molecular therapy. Nucleic acids · 2020Review
- Developing RNA aptamers for potential treatment of neurological diseases.Future medicinal chemistry · 2019Review
- Identification and characterization of RNA aptamers: A long aptamer blocks the AMPA receptor and a short aptamer blocks both AMPA and kainate receptors.The Journal of biological chemistry · 2017Article
- RNA based antagonist of NMDA receptors.ACS chemical neuroscience · 2014Article
- Mechanism and site of inhibition of AMPA receptors: pairing a thiadiazole with a 2,3-benzodiazepine scaffold.ACS chemical neuroscience · 2014Article
- Mechanism of Inhibition of the GluA2 AMPA Receptor Channel Opening: the Role of 4-Methyl versus 4-Carbonyl Group on the Diazepine Ring of 2,3-Benzodiazepine Derivatives.ACS chemical neuroscience · 2011Article
- Potent and selective inhibition of a single alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor subunit by an RNA aptamer.The Journal of biological chemistry · 2011Article
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Authors and funding
4 authors.
Funding
Abstract
Inhibitors of AMPA receptors are useful as biochemical probes for structure-function studies and as drug candidates for a number of neurological disorders and diseases. Here we report the identification of an RNA inhibitor or aptamer by an in vitro evolution approach. Using a laser-pulse photolysis technique, we further characterized the mechanism of inhibition of this aptamer on the AMPA receptor channel-opening rate process in the microsecond-to-millisecond time domain. Our results show that the aptamer we isolated is a noncompetitive inhibitor that selectively inhibits the open-channel conformation of AMPA receptors with nanomolar affinity. The potency and the selectivity of this noncompetitive aptamer rival those of small molecule inhibitors. Our results therefore demonstrate the utility of this approach in developing water-soluble, highly potent, and conformation-selective noncompetitive inhibitors of AMPA receptors.
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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 OpenQuestion graph.