Английская Википедия:Excitatory amino acid transporter 1

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Шаблон:Short description Шаблон:Infobox gene

Excitatory amino acid transporter 1 (EAAT1) is a protein that, in humans, is encoded by the SLC1A3 gene.[1] EAAT1 is also often called the GLutamate ASpartate Transporter 1 (GLAST-1).

EAAT1 is predominantly expressed in the plasma membrane, allowing it to remove glutamate from the extracellular space.[2] It has also been localized in the inner mitochondrial membrane as part of the malate-aspartate shuttle.[3]

Mechanism

EAAT1 functions in vivo as a homotrimer.[4] 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.[5]

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Tissue distribution

EAAT1 is expressed throughout the CNS,[6] and is highly expressed in astrocytes and Bergmann glia in the cerebellum.[7][8] In the retina, EAAT1 is expressed in Muller cells.[9] EAAT1 is also expressed in a number of other tissues including cardiac myocytes.[3]

Clinical significance

It is associated with type 6 episodic ataxia.[10] EAAT1 expression may also be associated with osteoarthritis.[11]

Pharmacology

DL-threo-beta-benzyloxyaspartate (TBOA) is an inhibitor of the excitatory amino acid transporters.[12]

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.[13]

References

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Further reading

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External links

Шаблон:Membrane transport proteins Шаблон:Mitochondrial enzymes Шаблон:Glutamate metabolism and transport modulators