Drug Transporter (DT) Information

General Information of DT
DT ID DTD0133
Gene Name SLC1A5
Protein Name Alanine/serine/cysteine/threonine transporter 2
Gene ID
6510
UniProt ID
Q15758
TCDB ID
2.A.23.3.3
3D Structure

Modelled DT Structure

Method:loop building

Template PDB:6GCT_A

Identity:100%

Minimized Score:-1199.518 kcal/mol

Detail: Structure Info

Synonyms AAAT; ASCT2; ATB(0); ATBO; Baboon M7 virus receptor; M7V1; M7VS1; Neutral amino acid transporter B(0); R16; RD114/simian type D retrovirus receptor; RDR; RDRC; SLC1A5; Sodium-dependent neutral amino acid transporter type 2; Solute carrier family 1 member 5
DT Family Dicarboxylate/Amino Acid:Cation (Na(+) Or H(+)) Symporter (DAACS) Family ;
Tissue Specificity Placenta, lung, skeletal muscle, kidney,pancreas, and intestine.
Function This sodium-dependent amino acids transporter that has a broad substrate specificity, with a preference for zwitterionic amino acids. It accepts as substrates all neutral amino acids, including glutamine, asparagine, and branched-chain and aromatic amino acids, and excludes methylated, anionic, and cationic amino acids. Through binding of the fusogenic protein syncytin-1/ERVW-1 may mediate trophoblasts syncytialization, the spontaneous fusion of their plasma membranes, an essential process in placental development.
Disease(s) Dietary shortage [ICD-11:5B7Z]
Nutritional deficiency [ICD-11:5B7Z]
Herpes simplex virus infection [ICD-11:1F00]
Shingles [ICD-11:1.00E+91]
Endogenous Substrate(s) Thyroid hormones; Thyroid hormone derivatives
Variability Data of This Drug Transporter (DT)

Regulatory Variability Data of This DT (VARIDT 4.0)

(α) Tissue Distribution Level of Alanine/serine/cysteine/threonine transporter 2
Tissue Distribution Level (TD)

(β) Cell Distribution Level of Alanine/serine/cysteine/threonine transporter 2
Cell Distribution Level (CD)

(γ) Organelle Distribution Level of Alanine/serine/cysteine/threonine transporter 2
Organelle Distribution Level (Subc)

Regulatory Variability Data of This DT

(β) Post-translational Modification of Alanine/serine/cysteine/threonine transporter 2
Post-translational Modification (PTM)

(γ) Transcriptional Regulation of Alanine/serine/cysteine/threonine transporter 2
Transcriptional Regulation (TSR)

(δ) Epigenetic Regulation of Alanine/serine/cysteine/threonine transporter 2
Epigenetic Regulation (EGR)

(ε) Exogenous Modulation of Alanine/serine/cysteine/threonine transporter 2
Exogenous Modulation (EGM)

Structural Variability Data of This DT

(α) Mutation-induced Structural Variation
Mutation-induced Structural Variation (MSV)

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

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

(δ) Xenobiotics-regulated Structural Variability
Xenobiotics-regulated Structural Variability (XSV)

General Variability Data of This DT

(α) Genetic Polymorphisms of Alanine/serine/cysteine/threonine transporter 2
Genetic Polymorphisms of This DT (GPD)

(β) Disease-specific Protein Abundances of Alanine/serine/cysteine/threonine 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:           7 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
Acyclovir
 Approved Drug Info Shingles 1.00E+91 [1]
Ganciclovir
 Approved Drug Info Cytomegalovirus infections 1D82 [1]
Glycine
 Approved Drug Info Dietary shortage 5B7Z [2]
L-carnitine
 Approved Drug Info Nutritional deficiency 5B7Z [3]
L-glutamine
 Approved Drug Info Short bowel syndrome KB89.1 [4]
Valacyclovir
 Approved Drug Info Shingles 1.00E+91 [5]
Valganciclovir
 Approved Drug Info Cytomegalovirus infections 1D82 [6]

 Clinical Trial Drug

 Click to Show/Hide the Full List of Drug:           2 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
D-serine
 Phase 4 Drug Info Serine deficiency disorder 5C50.6 [7]
Nitric oxide
 Phase 2/3 Drug Info Platelet dysfunction 3B62 [8]

 Withdrawn, Discontinued or Preclinical Drug

 Click to Show/Hide the Full List of Drug:           1 Drugs in Total
Drug Name Highest Status Detail Indication ICD 11 Ref
L-threonine
 Preclinical Drug Info Ulcerative colitis DD71 [7]

Drug-DT Affinity Assessed by Cell Line

 Approved Drug

 Click to Show/Hide the Full List of Drug:           6 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]
Glycine Approved Drug Info HRPE cells-ASCT2 Km =320 microM [2]

 Clinical Trial Drug

 Click to Show/Hide the Full List of Drug:           2 Drugs in Total
Drug Name Highest Status Detail Cell Line Affinity Ref
D-serine Phase 4 Drug Info Oocytes-ASCT2 Km =167 microM [7]
D-serine Phase 4 Drug Info Oocytes-ASCT2 Km =167 microM [7]
References
1 Amino Acid Transporter ATB0,+ as a delivery system for drugs and prodrugs. Curr Drug Targets Immune Endocr Metabol Disord. 2005 Dec;5(4):357-64.
2 Transport of butyryl-L-carnitine, a potential prodrug, via the carnitine transporter OCTN2 and the amino acid transporter ATB(0,+). Am J Physiol Gastrointest Liver Physiol. 2007 Nov;293(5):G1046-53.
3 A polarized localization of amino acid/carnitine transporter B(0,+) (ATB(0,+)) in the blood-brain barrier. Biochem Biophys Res Commun. 2008 Nov 14;376(2):267-70.
4 High-affinity glutamate transporter GLAST/EAAT1 regulates cell surface expression of glutamine/neutral amino acid transporter ASCT2 in human fetal astrocytes. Neurochem Int. 2006 May-Jun;48(6-7):611-5.
5 Transport of amino acid-based prodrugs by the Na+- and Cl(-) -coupled amino acid transporter ATB0,+ and expression of the transporter in tissues amenable for drug delivery. J Pharmacol Exp Ther. 2004 Mar;308(3):1138-47.
6 Transport of amino acid esters and the amino-acid-based prodrug valganciclovir by the amino acid transporter ATB(0,+). Pharm Res. 2004 Jul;21(7):1303-10.
7 D-Serine Is a Substrate for Neutral Amino Acid Transporters ASCT1/SLC1A4 and ASCT2/SLC1A5, and Is Transported by Both Subtypes in Rat Hippocampal Astrocyte Cultures. PLoS One. 2016 Jun 7;11(6):e0156551.
8 Functional regulation of Na+-dependent neutral amino acid transporter ASCT2 by S-nitrosothiols and nitric oxide in Caco-2 cells. FEBS Lett. 2005 Apr 25;579(11):2499-506.

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