ArticleProceedings of the National Academy of Sciences of the United States of America2006
Stargazin controls the pharmacology of AMPA receptor potentiators.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed, 69 citations in OpenAlex.
- Exploring the impact of the stargazin V143L mutation on the dynamics of the AMPA receptor: stargazin complex.Frontiers in cellular neuroscience · 2024Article
- Emerging trends in antipsychotic and antidepressant drug development: Targeting nonmonoamine receptors and innovative mechanisms.PCN reports : psychiatry and clinical neurosciences · 2023Review
- A pharmacogenetic study of perampanel: association between rare variants of glutamate receptor genes and outcomes.Frontiers in genetics · 2023Article
- Targeting prefrontal cortex GABAergic microcircuits for the treatment of alcohol use disorder.Frontiers in synaptic neuroscience · 2022Review
- Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.Pharmacological reviews · 2021Review
- Structural and functional insights into transmembrane AMPA receptor regulatory protein complexes.The Journal of general physiology · 2019Review
- Polyamine-mediated channel block of ionotropic glutamate receptors and its regulation by auxiliary proteins.The Journal of biological chemistry · 2018Review
- Physiological signature of a novel potentiator of AMPA receptor signalling.Molecular and cellular neurosciences · 2018Article
- Article
- The Inhibitory Effect of α/β-Hydrolase Domain-Containing 6 (ABHD6) on the Surface Targeting of GluA2- and GluA3-Containing AMPA Receptors.Frontiers in molecular neuroscience · 2017Article
- α/β-Hydrolase domain-containing 6 (ABHD6) negatively regulates the surface delivery and synaptic function of AMPA receptors.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- AMPA receptor potentiators: from drug design to cognitive enhancement.Current opinion in pharmacology · 2015Review
- Serine racemase regulated by binding to stargazin and PSD-95: potential N-methyl-D-aspartate-α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (NMDA-AMPA) glutamate neurotransmission cross-talk.The Journal of biological chemistry · 2014Article
- Mapping the interaction sites between AMPA receptors and TARPs reveals a role for the receptor N-terminal domain in channel gating.Cell reports · 2014Article
- A charge-inverting mutation in the "linker" region of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors alters agonist binding and gating kinetics independently of allosteric modulators.The Journal of biological chemistry · 2014Article
- Activity-mediated AMPA receptor remodeling, driven by alternative splicing in the ligand-binding domain.Neuron · 2012Article
- The regulation of glutamate receptor trafficking and function by TARPs and other transmembrane auxiliary subunits.Current opinion in neurobiology · 2012Review
- Autoinactivation of the stargazin-AMPA receptor complex: subunit-dependency and independence from physical dissociation.PloS one · 2012Article
- Structural and functional analysis of two new positive allosteric modulators of GluA2 desensitization and deactivation.Molecular pharmacology · 2011Article
- AKAP signaling complexes in regulation of excitatory synaptic plasticity.The Neuroscientist : a review journal bringing neurobiology, neurology and psychiatry · 2011Review
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glutamate is the major excitatory neurotransmitter in brain, and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors (AMPARs) mediate the majority of postsynaptic depolarization. AMPAR ion channels display rapid gating, and their deactivation and desensitization determine the timing of synaptic transmission. AMPAR potentiators slow channel deactivation and desensitization, and these compounds represent exciting therapies for mental and neurodegenerative diseases. Previous studies showed that the AMPAR potentiators cyclothiazide and 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluorophenoxyacetamide display a preference for flip and flop alternatively spliced versions of glutamate receptor subunits, respectively. Here, we find that the AMPAR auxiliary subunit stargazin changes this pharmacology and makes both spliced forms of glutamate receptor subunit 1 sensitive to both classes of potentiator. Stargazin also enhances the effect of AMPAR potentiators on channel deactivation. This work demonstrates that stargazin controls AMPAR potentiator pharmacology, which has important implications for development of AMPAR potentiators as therapeutic agents.
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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.