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Curr Opin Pharmacol. 2015 Feb;20:116-23. doi: 10.1016/j.coph.2014.10.008. Epub 2014 Nov 5.

Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities.

Author information

1
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2100 Copenhagen OE, Denmark. Electronic address: aaj@sund.ku.dk.
2
Institute of Complex Systems, Zelluläre Biophysik (ICS-4), Forschungszentrum Jülich, Germany.
3
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, DK-2100 Copenhagen OE, Denmark.

Abstract

The five excitatory amino acid transporters (EAAT1-5) mediating the synaptic uptake of the major excitatory neurotransmitter glutamate are differently expressed throughout the CNS and at the synaptic level. Although EAATs are crucial for normal excitatory neurotransmission, explorations into the physiological functions mediated by the different transporter subtypes and their respective therapeutic potential have so far been sparse, in no small part due to the limited selection of pharmacological tools available. In the present update, we outline important new insights into the molecular compositions of EAATs and their intricate transport process, the novel approaches to pharmacological modulation of the transporters that have emerged, and interesting new perspectives in EAAT as drug targets proposed in recent years.

PMID:
25466154
DOI:
10.1016/j.coph.2014.10.008
[Indexed for MEDLINE]

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