General Information of Target

Target ID LDTP04010
Target Name Excitatory amino acid transporter 1 (SLC1A3)
Gene Name SLC1A3
Gene ID 6507
Synonyms
EAAT1; GLAST; GLAST1; Excitatory amino acid transporter 1; Sodium-dependent glutamate/aspartate transporter 1; GLAST-1; Solute carrier family 1 member 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTKSNGEEPKMGGRMERFQQGVRKRTLLAKKKVQNITKEDVKSYLFRNAFVLLTVTAVIV
GTILGFTLRPYRMSYREVKYFSFPGELLMRMLQMLVLPLIISSLVTGMAALDSKASGKMG
MRAVVYYMTTTIIAVVIGIIIVIIIHPGKGTKENMHREGKIVRVTAADAFLDLIRNMFPP
NLVEACFKQFKTNYEKRSFKVPIQANETLVGAVINNVSEAMETLTRITEELVPVPGSVNG
VNALGLVVFSMCFGFVIGNMKEQGQALREFFDSLNEAIMRLVAVIMWYAPVGILFLIAGK
IVEMEDMGVIGGQLAMYTVTVIVGLLIHAVIVLPLLYFLVTRKNPWVFIGGLLQALITAL
GTSSSSATLPITFKCLEENNGVDKRVTRFVLPVGATINMDGTALYEALAAIFIAQVNNFE
LNFGQIITISITATAASIGAAGIPQAGLVTMVIVLTSVGLPTDDITLIIAVDWFLDRLRT
TTNVLGDSLGAGIVEHLSRHELKNRDVEMGNSVIEENEMKKPYQLIAQDNETEKPIDSET
KM
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Dicarboxylate/amino acid:cation symporter (DAACS) (TC 2.A.23) family, SLC1A3 subfamily
Subcellular location
Cell membrane
Function
Sodium-dependent, high-affinity amino acid transporter that mediates the uptake of L-glutamate and also L-aspartate and D-aspartate . Functions as a symporter that transports one amino acid molecule together with two or three Na(+) ions and one proton, in parallel with the counter-transport of one K(+) ion. Mediates Cl(-) flux that is not coupled to amino acid transport; this avoids the accumulation of negative charges due to aspartate and Na(+) symport. Plays a redundant role in the rapid removal of released glutamate from the synaptic cleft, which is essential for terminating the postsynaptic action of glutamate.
TTD ID
T86582
Uniprot ID
P43003
DrugMap ID
TTNJS0A
Ensemble ID
ENST00000265113.9
HGNC ID
HGNC:10941
ChEMBL ID
CHEMBL3085

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HT115 SNV: p.A115V .
JURKAT SNV: p.Y44H .
MEWO SNV: p.Q19Ter; p.P392L .
OVK18 SNV: p.V58I DBIA    Probe Info 
PANC1 SNV: p.K38N .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C375(0.91)  LDD3314  [1]
IPM
 Probe Info 
N.A.  LDD2156  [2]
TFBX
 Probe Info 
N.A.  LDD0148  [3]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-2
 Probe Info 
N.A.  LDD0138  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 8305C C375(1.44)  LDD2248  [1]
 LDCM0023  KB03 8305C C375(1.28)  LDD2665  [1]
 LDCM0024  KB05 IGR37 C375(0.91)  LDD3314  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Glutathione S-transferase 3, mitochondrial (MGST3) MAPEG family O14880
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Butyrophilin subfamily 2 member A2 (BTN2A2) BTN/MOG family Q8WVV5
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transmembrane protein 120B (TMEM120B) TMEM120 family A0PK00

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fingolimod Small molecular drug DB08868
Glutamic Acid Small molecular drug DB00142
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
D-aspartic Acid Small molecular drug D08CAB
Dl-tboa Small molecular drug D07GUB
Sym2081 Small molecular drug D0S8AN
Ucph-101 Small molecular drug D0I3EE
[3h]Etb-tboa Small molecular drug D07CIW

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
4 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.