Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0D6OL)
Name
Integral membrane E16 (SLC7A5)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Large neutral amino acids transporter 1; 4F2 LC; 4F2 light chain; 4F2LC; CD98 light chain; CD98LC; E16; HLAT1; L-type amino acid transporter 1; L-type amino acid transporter LAT1; LAT1; Large neutral amino acids transporter small subunit 1; MPE16; Solute carrier family 7 member 5; y+ system cationic amino acid transporter
Family Potential-driven transporter (PDT)  >>  Amino-polyamine-organocation transporter (APC)
Organism
Homo sapiens (Human)
Gene Name SLC7A5 Gene ID
8140
UniProt ID LAT1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T48330 (click to find more therapeutic target data of this DBT)
VARIDT ID DTD0471 (click to find more drug transporter data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MAGAGPKRRALAAPAAEEKEEAREKMLAAKSADGSAPAGEGEGVTLQRNITLLNGVAIIV
GTIIGSGIFVTPTGVLKEAGSPGLALVVWAACGVFSIVGALCYAELGTTISKSGGDYAYM
LEVYGSLPAFLKLWIELLIIRPSSQYIVALVFATYLLKPLFPTCPVPEEAAKLVACLCVL
LLTAVNCYSVKAATRVQDAFAAAKLLALALIILLGFVQIGKGDVSNLDPNFSFEGTKLDV
GNIVLALYSGLFAYGGWNYLNFVTEEMINPYRNLPLAIIISLPIVTLVYVLTNLAYFTTL
STEQMLSSEAVAVDFGNYHLGVMSWIIPVFVGLSCFGSVNGSLFTSSRLFFVGSREGHLP
SILSMIHPQLLTPVPSLVFTCVMTLLYAFSKDIFSVINFFSFFNWLCVALAIIGMIWLRH
RKPELERPIKVNLALPVFFILACLFLIAVSFWKTPVECGIGFTIILSGLPVYFFGVWWKN
KPKWLLQGIFSTTVLCQKLMQVVPQET
Function
Involved in cellular amino acid uptake. Acts as an amino acid exchanger. Involved in the transport of L-DOPA across the blood-brain barrier, and that of thyroid hormones triiodothyronine (T3) and thyroxine (T4) across the cell membrane in tissues such as placenta. Plays a role in neuronal cell proliferation (neurogenesis) in brain. Involved in the uptake of methylmercury (MeHg) when administered as the L-cysteine or D,L-homocysteine complexes, and hence plays a role in metal ion homeostasis and toxicity.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Histidine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant; Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 20000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
          DIG Name: Leucine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antiadherent; Flavoring agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 85000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
          DIG Name: Phenylalanine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Solubilizing agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 69000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 55000 nM (tested by experiment) [3]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID LAT1_RAT
          DIG Name: Isoleucine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antiadherent; Flavoring agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 140000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
          DIG Name: Methionine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 120000 nM (estimated based on the structural similarity with CHEMBL1234268 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
          DIG Name: Tryptophan Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 160000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
          DIG Name: Valine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 68000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID LAT1_HUMAN
References
1 Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1). J Med Chem. 2018 Aug 23; 61(16):7358-7373.
2 l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan. Bioorg Med Chem Lett. 2019 Aug 15; 29(16):2254-2258.
3 Regiospecific and conformationally restrained analogs of melphalan and DL-2-NAM-7 and their affinities for the large neutral amino acid transporter (system LAT1) of the blood-brain barrier. Bioorg Med Chem Lett. 2010 Jun 15; 20(12):3688-91.

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