![conference banner](/images/conference-banner.jpeg)
Abstract
L-Glutamate is the major excitatory neurotransmitter in mammalian central nervous system, and excitatory amino acid transporters (EAATs) are essential for terminating synaptic excitation and for maintaining extracellular glutamate concentration below toxic levels. Although the structure of these channel-like proteins has not been yet reported, their membrane topology has been hypothesised based on biochemical and protein sequence analyses. In the case of an inadequate clearance from synaptic cleft and from the extrasynaptic space, glutamate behaves as a potent neurotoxin, and it may be related to several neurodegenerative pathologies including epilepsy, ischemia, amyotrophic lateral sclerosis, and Alzheimer disease. The recent boom of glutamate is demonstrated by the enormous amount of publications dealing with the function of glutamate, with its role on modulation of synaptic transmission throughout the brain, mainly focusing: i) on the structure of its receptors, ii) on molecular biology and pharmacology of Glu transporters, and iii) on the role of glutamate uptake and reversal uptake in several neuropathologies. This review will deal with the recent and most interesting published results on Glu transporters membrane topology, Glu transporters physiopathological role and Glu transporters medicinal chemistry, highlighting the guidelines for the development of potential neuroprotective agents targeting neuronal high-affinity sodium-dependent glutamate transporters.
Keywords: l-glutamake transporter, eaats, neurodegenerative disorder, neurotransmitter, glu, excitatory amino acid transporter
Current Pharmaceutical Design
Title: Neuronal High-Affinity Sodium-Dependent Glutamate Transporters (EAATs): Targets for the Development of Novel Therapeutics Against Neurodegenerative Diseases
Volume: 9 Issue: 8
Author(s): Giuseppe Campiani, Caterina Fattorusso, Meri De Angelis, Bruno Catalanotti, Stefania Butini, Roberto Fattorusso, Isabella Fiorini, Vito Nacci and Ettore Novellino
Affiliation:
Keywords: l-glutamake transporter, eaats, neurodegenerative disorder, neurotransmitter, glu, excitatory amino acid transporter
Abstract: L-Glutamate is the major excitatory neurotransmitter in mammalian central nervous system, and excitatory amino acid transporters (EAATs) are essential for terminating synaptic excitation and for maintaining extracellular glutamate concentration below toxic levels. Although the structure of these channel-like proteins has not been yet reported, their membrane topology has been hypothesised based on biochemical and protein sequence analyses. In the case of an inadequate clearance from synaptic cleft and from the extrasynaptic space, glutamate behaves as a potent neurotoxin, and it may be related to several neurodegenerative pathologies including epilepsy, ischemia, amyotrophic lateral sclerosis, and Alzheimer disease. The recent boom of glutamate is demonstrated by the enormous amount of publications dealing with the function of glutamate, with its role on modulation of synaptic transmission throughout the brain, mainly focusing: i) on the structure of its receptors, ii) on molecular biology and pharmacology of Glu transporters, and iii) on the role of glutamate uptake and reversal uptake in several neuropathologies. This review will deal with the recent and most interesting published results on Glu transporters membrane topology, Glu transporters physiopathological role and Glu transporters medicinal chemistry, highlighting the guidelines for the development of potential neuroprotective agents targeting neuronal high-affinity sodium-dependent glutamate transporters.
Export Options
About this article
Cite this article as:
Campiani Giuseppe, Fattorusso Caterina, Angelis De Meri, Catalanotti Bruno, Butini Stefania, Fattorusso Roberto, Fiorini Isabella, Nacci Vito and Novellino Ettore, Neuronal High-Affinity Sodium-Dependent Glutamate Transporters (EAATs): Targets for the Development of Novel Therapeutics Against Neurodegenerative Diseases, Current Pharmaceutical Design 2003; 9 (8) . https://dx.doi.org/10.2174/1381612033391261
DOI https://dx.doi.org/10.2174/1381612033391261 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
Blood-based biomarkers in large-scale screening for neurodegenerative diseases
Disease biomarkers are necessary tools that can be employ in several clinical context of use (COU), ranging from the (early) diagnosis, prognosis, prediction, to monitor of disease state and/or drug efficacy. Regarding neurodegenerative diseases, in particular Alzheimer’s disease (AD), a battery of well-validated biomarkers are available, such as cerebrospinal fluid ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Diabetes mellitus: advances in diagnosis and treatment driving by precision medicine
Diabetes mellitus (DM) is a chronic degenerative metabolic disease with ever increasing prevalence worldwide which is now an epidemic disease affecting 500 million people worldwide. Insufficient insulin secretion from pancreatic β cells unable to maintain blood glucose homeostasis is the main feature of this disease. Multifactorial and complex nature of ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
GABAB Receptors as Potential Therapeutic Targets
Current Drug Targets - CNS & Neurological Disorders Computational Protein-Protein Docking Reveals the Therapeutic Potential of Kunitz-type Venom against hKv1.2 Binding Sites
CNS & Neurological Disorders - Drug Targets Editorial (Thematic Issue: Linkage of Neurodegenerative Disorders with Other Health Issues – Volume I)
CNS & Neurological Disorders - Drug Targets Physiology, Pharmacology and Pathophysiology of the pH Regulatory Transport Proteins NHE1 and NBCn1: Similarities, Differences, and Implications for Cancer Therapy
Current Pharmaceutical Design 1,2,4-Triazine Analogs as Novel Class of Therapeutic Agents
Mini-Reviews in Medicinal Chemistry The Role of Ionotropic Glutamate Receptors in Childhood Neurodevelopmental Disorders: Autism Spectrum Disorders and Fragile X Syndrome
Current Neuropharmacology Organic Lesions in the Brain MRI of Children with Febrile Seizure
Current Medical Imaging Editorial [Hot Topic: Membrane Channels as Therapeutic Targets (Executive Editor: Jean-Claude Herve)]
Current Pharmaceutical Design Reverse Iontophoretic Extraction of Gabapentin: A Mechanistic Study
Current Drug Delivery Conformational Changes Preceding Amyloid-Fibril Formation of Amyloid- Beta, Prion Protein and Stefin B; Parallels in pH Dependence
Medicinal Chemistry Reviews - Online (Discontinued) Editorial [Hot Topic: Membrane Channels as Therapeutic Targets (Executive Editor: Jean-Claude Herve)]
Current Pharmaceutical Design Cognitive Dysfunction in Major Depressive Disorder: A State-of-the-Art Clinical Review
CNS & Neurological Disorders - Drug Targets Recent Studies on Neural Tube Defects in Embryos of Diabetic Pregnancy: An Overview
Current Medicinal Chemistry Lifelong Endocrine Fluctuations and Related Cognitive Disorders
Current Pharmaceutical Design Cross-Cultural Comparison of Mild Cognitive Impairment between China and USA
Current Alzheimer Research Uncovering New Pharmacological Targets to Treat Neuropathic Pain by Understanding How the Organism Reacts to Nerve Injury
Current Pharmaceutical Design Editorial [Hot Topic: Analysis of Progenitor Cells in the Brain before and after Treatment (Guest Editors: M.A. Curtis and L. Paulson)]
Current Pharmaceutical Biotechnology Migraine and Central Sensitization: Clinical Features, Main Comorbidities and Therapeutic Perspectives
Current Rheumatology Reviews Use of Non-steroidal Anti-inflammatory Drugs in Pregnancy: Impact on the Fetus and Newborn
Current Drug Metabolism Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives
Current Medicinal Chemistry