Excitatory amino acid transporter 1 (EAAT1) is a
protein that, in humans, is encoded by the SLC1A3gene.[5] EAAT1 is also often called the GLutamate ASpartate Transporter 1 (GLAST-1).
EAAT1 functions in vivo as a
homotrimer.[8] EAAT1 mediates the transport of
glutamic and
aspartic acid with the
cotransport of three
Na+ and one
H+cations and counter transport of one
K+ cation. This co-transport coupling (or
symport) allows the transport of glutamate into cells against a concentration gradient.[9]
"Diagram Illustrating the Malate-Aspartate Shuttle Pathway". (Glutamate aspartate transporter labeled at bottom center.)
Expression of SLC1A3 in the Bergmann glia fibers. Mouse brain at 7th postnatal day, sagittal section; GENSAT database.
DL-threo-beta-benzyloxyaspartate (TBOA) is an inhibitor of the excitatory amino acid transporters.[16]
Selective inhibitors for EAAT1 have recently been discovered based on 25 combinations of substitutions at the 4 and 7 positions of 2-amino-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitril.[17]
^
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^Rauen T, Taylor WR, Kuhlbrodt K, Wiessner M (January 1998). "High-affinity glutamate transporters in the rat retina: a major role of the glial glutamate transporter GLAST-1 in transmitter clearance". Cell and Tissue Research. 291 (1): 19–31.
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^Jen JC, Wan J, Palos TP, Howard BD, Baloh RW (August 2005). "Mutation in the glutamate transporter EAAT1 causes episodic ataxia, hemiplegia, and seizures". Neurology. 65 (4): 529–34.
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^Shimamoto K, Lebrun B, Yasuda-Kamatani Y, Sakaitani M, Shigeri Y, Yumoto N, Nakajima T (February 1998). "DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters". Molecular Pharmacology. 53 (2): 195–201.
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^Jensen AA, Erichsen MN, Nielsen CW, Stensbøl TB, Kehler J, Bunch L (February 2009). "Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1". Journal of Medicinal Chemistry. 52 (4): 912–5.
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Mordrelle A, Jullian E, Costa C, Cormet-Boyaka E, Benamouzig R, Tomé D, Huneau JF (August 2000). "EAAT1 is involved in transport of L-glutamate during differentiation of the Caco-2 cell line". American Journal of Physiology. Gastrointestinal and Liver Physiology. 279 (2): G366-73.
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