ArticleProtein science : a publication of the Protein Society2007
Docking and homology modeling explain inhibition of the human vesicular glutamate transporters.
Article in Protein science : a publication of the Protein Society, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 47 citations in OpenAlex.
- Genes of the Glutamatergic System and Tardive Dyskinesia in Patients with Schizophrenia.Diagnostics (Basel, Switzerland) · 2022Article
- Inhibition of the Vesicular Glutamate Transporter (VGLUT) with Congo Red Analogs: New Binding Insights.Neurochemical research · 2021Article
- Layer-Specific Vesicular Glutamate Transporter 1 Immunofluorescence Levels Delineate All Layers of the Human Hippocampus Including theFrontiers in cellular neuroscience · 2021Article
- VGLUT substrates and inhibitors: A computational viewpoint.Biochimica et biophysica acta. Biomembranes · 2020Review
- Molecular, Structural, Functional, and Pharmacological Sites for Vesicular Glutamate Transporter Regulation.Molecular neurobiology · 2020Review
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- A proline-rich motif on VGLUT1 reduces synaptic vesicle super-pool and spontaneous release frequency.eLife · 2019Article
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- Characterization of a Human Point Mutation of VGLUT3 (p.A211V) in the Rodent Brain Suggests a Nonuniform Distribution of the Transporter in Synaptic Vesicles.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2017Article
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- Screening of the SLC17A8 gene as a causative factor for autosomal dominant non-syndromic hearing loss in Koreans.BMC medical genetics · 2016Article
- VGLUTs and Glutamate Synthesis-Focus on DRG Neurons and Pain.Biomolecules · 2015Review
- Vesicular glutamate transporter expression level affects synaptic vesicle release probability at hippocampal synapses in culture.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- The development of benzo- and naphtho-fused quinoline-2,4-dicarboxylic acids as vesicular glutamate transporter (VGLUT) inhibitors reveals a possible role for neuroactive steroids.Bioorganic & medicinal chemistry letters · 2014Article
- Are vesicular neurotransmitter transporters potential treatment targets for temporal lobe epilepsy?Frontiers in cellular neuroscience · 2013Review
- Astrocytic vesicle mobility in health and disease.International journal of molecular sciences · 2013Review
- Successful prediction of substrate-binding pocket in SLC17 transporter sialin.The Journal of biological chemistry · 2012Article
- From glutamate co-release to vesicular synergy: vesicular glutamate transporters.Nature reviews. Neuroscience · 2011Review
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
As membrane transporter proteins, VGLUT1-3 mediate the uptake of glutamate into synaptic vesicles at presynaptic nerve terminals of excitatory neural cells. This function is crucial for exocytosis and the role of glutamate as the major excitatory neurotransmitter in the central nervous system. The three transporters, sharing 76% amino acid sequence identity in humans, are highly homologous but differ in regional expression in the brain. Although little is known regarding their three-dimensional structures, hydropathy analysis on these proteins predicts 12 transmembrane segments connected by loops, a topology similar to other members in the major facilitator superfamily, where VGLUT1-3 have been phylogenetically classified. In this work, we present a three-dimensional model for the human VGLUT1 protein based on its distant bacterial homolog in the same superfamily, the glycerol-3-phosphate transporter from Escherichia coli. This structural model, stable during molecular dynamics simulations in phospholipid bilayers solvated by water, reveals amino acid residues that face its pore and are likely to affect substrate translocation. Docking of VGLUT1 substrates to this pore localizes two different binding sites, to which inhibitors also bind with an overall trend in binding affinity that is in agreement with previously published experimental data.
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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.