Abstract
This review provides an overview of ligands for the excitatory amino acid transporters (EAATs), a family of high-affinity glutamate transporters localized to the plasma membrane of neurons and astroglial cells. Ligand development from the perspective of identifying novel and more selective tools for elucidating transporter subtype function, and the potential of transporter ligands in a therapeutic setting are discussed. Acute pharmacological modulation of EAAT activity in the form of linear and conformationally restricted glutamate and aspartate analogs is presented, in addition to recent strategies aimed more toward modulating transporter expression levels, the latter of particular significance to the development of transporter based therapeutics.
Keywords: Excitatory amino acid transporters, EAAT, glutamate
Current Topics in Medicinal Chemistry
Title: Ligands Targeting the Excitatory Amino Acid Transporters (EAATs)
Volume: 6 Issue: 17
Author(s): John Dunlop and John A. Butera
Affiliation:
Keywords: Excitatory amino acid transporters, EAAT, glutamate
Abstract: This review provides an overview of ligands for the excitatory amino acid transporters (EAATs), a family of high-affinity glutamate transporters localized to the plasma membrane of neurons and astroglial cells. Ligand development from the perspective of identifying novel and more selective tools for elucidating transporter subtype function, and the potential of transporter ligands in a therapeutic setting are discussed. Acute pharmacological modulation of EAAT activity in the form of linear and conformationally restricted glutamate and aspartate analogs is presented, in addition to recent strategies aimed more toward modulating transporter expression levels, the latter of particular significance to the development of transporter based therapeutics.
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Cite this article as:
Dunlop John and Butera A. John, Ligands Targeting the Excitatory Amino Acid Transporters (EAATs), Current Topics in Medicinal Chemistry 2006; 6 (17) . https://dx.doi.org/10.2174/156802606778249829
DOI https://dx.doi.org/10.2174/156802606778249829 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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