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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Ligands Targeting the Excitatory Amino Acid Transporters (EAATs)

Author(s): John Dunlop and John A. Butera

Volume 6, Issue 17, 2006

Page: [1897 - 1906] Pages: 10

DOI: 10.2174/156802606778249829

Price: $65


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

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