Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0IH5S)
Name
Urate exporter (BCRP)
Synonyms    Click to Show/Hide the Synonyms of This DBT
ATP-binding cassette G2; Placenta-specific ATP-binding cassette transporter; Mitoxantrone resistance-associated protein; MXR; CDw338; CD338; Breast cancer resistance protein; BCRP1; BCRP; ABCP; ABCG2
Family Primary active transporter (PAT)  >>  ATP-binding cassette transporter (ABC)
Organism
Homo sapiens (Human)
Gene Name ABCG2 Gene ID
9429
UniProt ID ABCG2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T56556 (click to find more therapeutic target data of this DBT)
VARIDT ID DTD0004 (click to find more drug transporter data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVE
KEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCN
SGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGT
QFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIF
SIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIING
DSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKK
ITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLP
MRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLL
MTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGN
NPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
Function
Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Oleic acid 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
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 60 % (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
          DIG Name: Polyoxyl 35 castor oil 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
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 40 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
          DIG Name: Polysorbate 20 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
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 84 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 50 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
          DIG Name: Sorbitan monolaurate 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
Dispersing agent; Emulsifying agent; Solubilizing agent; Surfactant; Suspending agent; Vaccine adjuvant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 30 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
          DIG Name: Laureth-4 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
Dispersing agent; Emulsifying agent; Gelling agent; Penetration agent; Solubilizing agent; Surfactant; Viscosity-controlling agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 50 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
          DIG Name: Pluronic P85 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
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 58 % (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition ratio > 70 % (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ABCG2_HUMAN
References
1 Oleic acid decreases BCRP mediated efflux of mitoxantrone in Caco-2 cell monolayers. Food Chem Toxicol. 2012 Oct;50(10):3635-45.
2 Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
3 Characterization of the inhibition of breast cancer resistance protein-mediated efflux of mitoxantrone by pharmaceutical excipients. Int J Pharm. 2009 Mar 31;370(1-2):216-9.

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