Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET08ZIK)
Name
NFE2-related factor 2 (NRF2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Nuclear factor erythroid 2-related factor 2; HEBP1; NF-E2-related factor 2; NFE2-related factor 2; NRF2; Nrf-2; Nuclear factor, erythroid derived 2, like 2; NFE2L2
Family Other protein families (OPF)  >>  Transcription factor (TF)
Organism
Homo sapiens (Human)
Gene Name NFE2L2 Gene ID
4780
UniProt ID NF2L2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T88505 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MMDLELPPPGLPSQQDMDLIDILWRQDIDLGVSREVFDFSQRRKEYELEKQKKLEKERQE
QLQKEQEKAFFAQLQLDEETGEFLPIQPAQHIQSETSGSANYSQVAHIPKSDALYFDDCM
QLLAQTFPFVDDNEVSSATFQSLVPDIPGHIESPVFIATNQAQSPETSVAQVAPVDLDGM
QQDIEQVWEELLSIPELQCLNIENDKLVETTMVPSPEAKLTEVDNYHFYSSIPSMEKEVG
NCSPHFLNAFEDSFSSILSTEDPNQLTVNSLNSDATVNTDFGDEFYSAFIAEPSISNSMP
SPATLSHSLSELLNGPIDVSDLSLCKAFNQNHPESTAEFNDSDSGISLNTSPSVASPEHS
VESSSYGDTLLGLSDSEVEELDSAPGSVKQNGPKTPVHSSGDMVQPLSPSQGQSTHVHDA
QCENTPEKELPVSPGHRKTPFTKDKHSSRLEAHLTRDELRAKALHIPFPVEKIINLPVVD
FNEMMSKEQFNEAQLALIRDIRRRGKNKVAAQNCRKRKLENIVELEQDLDHLKDEKEKLL
KEKGENDKSLHLLKKQLSTLYLEVFSMLRDEDGKPYSPSEYSLQQTRDGNVFLVPKSKKP
DVKKN
Function
Important for the coordinated up-regulation of genes in response to oxidative stress and the regulation of cellular redox conditions. May be involved in the transcriptional activation of genes of the beta-globin cluster by mediating enhancer activity of hypersensitive site 2 of the beta-globin locus control region. Transcription activator that binds to antioxidant response (ARE) elements in the promoter regions of target genes.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Ethyl acrylate 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
Film/membrane-forming agent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 5110 nM (estimated based on the structural similarity with CHEMBL2107333 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.837837838
                   Tested Species Homo sapiens (Human)
                   UniProt ID NF2L2_HUMAN
          DIG Name: Tert-Butylhydroquinone 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
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 91530 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID NF2L2_HUMAN
References
1 A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model. Eur J Med Chem. 2020 Jan 1; 185:111777.
2 3-aroylmethylene-2,3,6,7-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4(11bH)-ones as potent Nrf2/ARE inducers in human cancer cells and AOM-DSS treated mice. J Med Chem. 2013 Oct 24; 56(20):7925-38.

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