Drug Transporter (DT) Information

General Information of DT
DT ID DTD0130
Gene Name SLC1A2
Protein Name Excitatory amino acid transporter 2
Gene ID
6506
UniProt ID
P43004
TCDB ID
2.A.23.2.7
3D Structure

Modelled DT Structure

Method:homology modeling

Template PDB:5LLU_A

Identity:59.959%

Minimized Score:-1271.034 kcal/mol

Detail: Structure Info

Synonyms EAAT2; EIEE41; GLT-1; GLT1; Glutamate/aspartate transporter II; HBGT; SLC1A2; Sodium-dependent glutamate/aspartate transporter 2; Solute carrier family 1 member 2
DT Family Dicarboxylate/Amino Acid:Cation (Na(+) Or H(+)) Symporter (DAACS) Family ;
Function This sodium-dependent, high-affinity amino acid transporter functions as a symporter and mediates the uptake of L-glutamate and also L-aspartate and D-aspartate. Mediates Cl(-) flux that is not coupled to amino acid transport; this avoids the accumulation of negative charges due to aspartate and Na(+) symport. Essential for the rapid removal of released glutamate from the synaptic cleft, and for terminating the postsynaptic action of glutamate.
Endogenous Substrate(s) Na+; Aspartate
Variability Data of This Drug Transporter (DT)

Regulatory Variability Data of This DT (VARIDT 4.0)

(α) Tissue Distribution Level of Excitatory amino acid transporter 2
Tissue Distribution Level (TD)

(β) Cell Distribution Level of Excitatory amino acid transporter 2
Cell Distribution Level (CD)

(γ) Organelle Distribution Level of Excitatory amino acid transporter 2
Organelle Distribution Level (Subc)

Regulatory Variability Data of This DT

(β) Post-translational Modification of Excitatory amino acid transporter 2
Post-translational Modification (PTM)

(γ) Transcriptional Regulation of Excitatory amino acid transporter 2
Transcriptional Regulation (TSR)

(δ) Epigenetic Regulation of Excitatory amino acid transporter 2
Epigenetic Regulation (EGR)

(ε) Exogenous Modulation of Excitatory amino acid transporter 2
Exogenous Modulation (EGM)

Structural Variability Data of This DT

(β) Inter-species Structural Differences
Inter-species Structural Differences (ISD)

(γ) Outward/inward-facing Conformation
Outward/inward-facing Conformation (OIC)

General Variability Data of This DT

(α) Genetic Polymorphisms of Excitatory amino acid transporter 2
Genetic Polymorphisms of This DT (GPD)

(β) Disease-specific Protein Abundances of Excitatory amino acid transporter 2
Disease-specific Protein Abundances of This DT (DPAD)

(γ) Species- and Tissue-specific DT Abundances
Species/Tissue-specific Protein Abundances of This DT (S/TPAD)
Molecular Transporting Profile of This DT

Full List of Drug(s) Transported by This DT

 Approved Drug

 Click to Show/Hide the Full List of Drug:           1 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
L-glutamic acid
 Approved Drug Info Schizophrenia 6A20 [1]

Endogenous Metabolites (EMs) Handled by This DT

 Endogenous Metabolites (EMs)

 Click to Show/Hide the Full List of EMs:           1 EMs in Total
EM Name PubChem CID Detail Experimental Material Ref
Glutamate
33032
EM Info Identified using SIRT5 knockout mice [2]

Drug-DT Affinity Assessed by Cell Line

 Approved Drug

 Click to Show/Hide the Full List of Drug:         38 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [3]
L-glutamic acid Approved Drug Info Human embryonic kidney cells (HEK293)-EAAT2 Km =21 microM [4]
References
1 EAAT2 (GLT-1; slc1a2) glutamate transporters reconstituted in liposomes argues against heteroexchange being substantially faster than net uptake. J Neurosci. 2014 Oct 1;34(40):13472-85.
2 Metabolomics Based Identification of SIRT5 and Protein Kinase C Epsilon Regulated Pathways in Brain. Front Neurosci. 2018 Jan 30;12:32.
3 Chemoenzymatic synthesis of a series of 4-substituted glutamate analogues and pharmacological characterization at human glutamate transporters subtypes 1-3. J Med Chem. 2005 Dec 15;48(25):7980-92.
4 Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3. J Med Chem. 2006 Nov 2;49(22):6532-8.

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