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Alanine/serine/cysteine transporter 2

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Target id: 874

Nomenclature: Alanine/serine/cysteine transporter 2

Abbreviated Name: ASCT2

Systematic Nomenclature: SLC1A5

Family: Alanine/serine/cysteine transporter subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 8 541 19q13.32 SLC1A5 solute carrier family 1 member 5
Mouse 8 553 7 A2 Slc1a5 solute carrier family 1 (neutral amino acid transporter), member 5
Rat - - Slc1a5 solute carrier family 1 member 5
Previous and Unofficial Names Click here for help
AAAT | hATB0 | Neutral amino acid transporter B(0) | ASCT2 | RDRC | CAZ-associated structural protein | H4-ASCT2 | H4-system ASC-like transporter | Slc1a7 | sodium-dependent neutral amino acid transporter ASCT2 | solute carrier family 1, member 7 | solute carrier family 1 (neutral amino acid transporter), member 5 | solute carrier family 1 (neutral amino acid transporter)
Database Links Click here for help
Specialist databases
Bioparadigms SLC Tables SLC1A5 (Hs)
RESOLUTE SLC1A5 (Hs)
Other databases
Alphafold Q15758 (Hs), P51912 (Mm)
CATH/Gene3D 1.10.3860.10
ChEMBL Target CHEMBL3562162 (Hs)
Ensembl Gene ENSG00000105281 (Hs), ENSMUSG00000001918 (Mm), ENSRNOG00000015948 (Rn)
Entrez Gene 6510 (Hs), 20514 (Mm), 292657 (Rn)
Human Protein Atlas ENSG00000105281 (Hs)
KEGG Gene hsa:6510 (Hs), mmu:20514 (Mm), rno:292657 (Rn)
OMIM 109190 (Hs)
Pharos Q15758 (Hs)
UniProtKB Q15758 (Hs), P51912 (Mm)
Wikipedia SLC1A5 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Cryo-EM structure of the human neutral amino acid transporter ASCT2
PDB Id:  6GCT
Resolution:  3.85Å
Species:  Human
References:  3
Stoichiometry Click here for help
1 Na+: 1 amino acid (in): 1 Na+: 1 amino acid (out); (homo-, or hetero-exchange; [1])
Endogenous substrates (Human)
L-alanine = L-serine = L-cysteine (low Vmax) = L-threonine = L-glutamine = L-asparagine >> L-methionine ≅ glycine ≅ L-leucine > L-valine > L-glutamic acid (enhanced at low pH)

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
p-nitrophenyl glutamyl anilide Small molecule or natural product Rn Inhibition 4.3 pKi 2
⤷ pKi 4.3 (Ki 5.5x10-5 M) [2]
benzylcysteine Small molecule or natural product Ligand has a PDB structure Hs Inhibition 3.1 pKi 4
⤷ pKi 3.1 (Ki 7.8x10-4 M) [4]
benzylserine Small molecule or natural product Ligand has a PDB structure Hs Inhibition 3.0 pKi 4
⤷ pKi 3.0 (Ki 9x10-4 M) [4]
compound 25e [PMID: 38217503] Small molecule or natural product Hs Inhibition 5.3 pIC50 5
⤷ pIC50 5.3 (IC50 5.14x10-6 M) [5]
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Barrier integrity

References

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1. Bröer A, Brookes N, Ganapathy V, Dimmer KS, Wagner CA, Lang F, Bröer S. (1999) The astroglial ASCT2 amino acid transporter as a mediator of glutamine efflux. J Neurochem, 73 (5): 2184-94. [PMID:10537079]

2. Esslinger CS, Cybulski KA, Rhoderick JF. (2005) Ngamma-aryl glutamine analogues as probes of the ASCT2 neutral amino acid transporter binding site. Bioorg Med Chem, 13 (4): 1111-8. [PMID:15670919]

3. Garaeva AA, Oostergetel GT, Gati C, Guskov A, Paulino C, Slotboom DJ. (2018) Cryo-EM structure of the human neutral amino acid transporter ASCT2. Nat Struct Mol Biol, 25 (6): 515-521. [PMID:29872227]

4. Grewer C, Grabsch E. (2004) New inhibitors for the neutral amino acid transporter ASCT2 reveal its Na+-dependent anion leak. J Physiol (Lond.), 557 (Pt 3): 747-59. [PMID:15107471]

5. Qin L, Cheng X, Wang S, Gong G, Su H, Huang H, Chen T, Damdinjav D, Dorjsuren B, Li Z et al.. (2024) Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem, 67 (2): 988-1007. [PMID:38217503]

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