ArticleThe Journal of physiology2002
Binding site stoichiometry and the effects of phosphorylation on human alpha1 homomeric glycine receptors.
Article in The Journal of physiology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 45 citations in OpenAlex.
- Human GlyRα2 pore dynamics in gating and inhibition.Structure (London, England : 1993) · 2026Article
- Positive Allosteric Modulators of Glycine Receptors and Their Potential Use in Pain Therapies.Pharmacological reviews · 2022Review
- Principal Neurons in the Anteroventral Cochlear Nucleus Express Cell-Type Specific Glycine Receptor α Subunits.Neuroscience · 2019Article
- Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice.The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2019Article
- PKA and PKC Modulators Affect Ion Channel Function and Internalization of Recombinant Alpha1 and Alpha1-Beta Glycine Receptors.Frontiers in molecular neuroscience · 2018Article
- The Intracellular Loop of the Glycine Receptor: It's not all about the Size.Frontiers in molecular neuroscience · 2016Review
- The role of intracellular linkers in gating and desensitization of human pentameric ligand-gated ion channels.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- Glycinergic synaptic transmission in the cochlear nucleus of mice with normal hearing and age-related hearing loss.Journal of neurophysiology · 2013Article
- Target-specific IPSC kinetics promote temporal processing in auditory parallel pathways.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- The long activations of α2 glycine channels can be described by a mechanism with reaction intermediates ("flip").The Journal of general physiology · 2011Article
- Article
- Single-channel kinetic analysis for activation and desensitization of homomeric 5-HT(3)A receptors.Biophysical journal · 2009Article
- Number and locations of agonist binding sites required to activate homomeric Cys-loop receptors.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2009Article
- Slow glycinergic transmission mediated by transmitter pooling.Nature neuroscience · 2009Article
- The time course of transmitter at glycinergic synapses onto motoneurons.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2008Article
- Extrasynaptic and postsynaptic receptors in glycinergic and GABAergic neurotransmission: a division of labor?Frontiers in molecular neuroscience · 2008Article
- Responses of rat P2X2 receptors to ultrashort pulses of ATP provide insights into ATP binding and channel gating.The Journal of general physiology · 2007Article
- The kinetics of inhibition of rat recombinant heteromeric alpha1beta glycine receptors by the low-affinity antagonist SR-95531.The Journal of physiology · 2007Article
- Protein kinases regulate glycine receptor binding in brain stem auditory nuclei after unilateral cochlear ablation.Brain research · 2007Article
- Modulating inhibitory ligand-gated ion channels.The AAPS journal · 2006Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The kinetic properties of the human alpha1 homomeric glycine receptor were investigated. Receptors were expressed in HEK 293 cells, and glycine was applied to outside-out membrane patches with sub-millisecond solution exchange. The activation time course of the glycine response was used to investigate receptor stoichiometry. The unbinding of three strychnine molecules and the cooperative binding of two glycine molecules were required to activate the channel. The effects of phosphorylation on glycine receptor kinetics were investigated by pretreating cells with phosphorylators or with phosphatases. Phosphorylation accelerated desensitisation, but slowed deactivation and recovery from desensitisation. A chemical-kinetic model was developed that reproduced the experimental observations. The model suggests that only three binding sites on the glycine channel are functional, while the remaining two binding sites are 'silent', possibly due to strong negative cooperativity.
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What OpenQuestion holds
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.