Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0F6ME)
Name
Arginine methyltransferase 1 (PRMT1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Histone-arginine N-methyltransferase PRMT1; Protein arginine methyltransferase 1; Protein arginine N-methyltransferase 1; Interferon receptor 1-bound protein 4; IR1B4; HRMT1L2; HMT2
Family Transferase (TFase)  >>  Methylase (EC 2.1)
Organism
Homo sapiens (Human)
Gene Name PRMT1 Gene ID
3276
UniProt ID ANM1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T16808 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MAAAEAANCIMENFVATLANGMSLQPPLEEVSCGQAESSEKPNAEDMTSKDYYFDSYAHF
GIHEEMLKDEVRTLTYRNSMFHNRHLFKDKVVLDVGSGTGILCMFAAKAGARKVIGIECS
SISDYAVKIVKANKLDHVVTIIKGKVEEVELPVEKVDIIISEWMGYCLFYESMLNTVLYA
RDKWLAPDGLIFPDRATLYVTAIEDRQYKDYKIHWWENVYGFDMSCIKDVAIKEPLVDVV
DPKQLVTNACLIKEVDIYTVKVEDLTFTSPFCLQVKRNDYVHALVAYFNIEFTRCHKRTG
FSTSPESPYTHWKQTVFYMEDYLTVKTGEEIFGTIGMRPNAKNNRDLDFTIDLDFKGQLC
ELSCSTDYRMR
Function
Constitutes the main enzyme that mediates monomethylation and asymmetric dimethylation of histone H4 'Arg-4' (H4R3me1 and H4R3me2a, respectively), a specific tag for epigenetic transcriptional activation. May be involved in the regulation of TAF15 transcriptional activity, act as an activator of estrogen receptor (ER)-mediated transactivation, play a key role in neurite outgrowth and act as a negative regulator of megakaryocytic differentiation, by modulating p38 MAPK pathway.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: D&C red no. 27 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1400 nM (estimated based on the structural similarity with CHEMBL376503 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.781914894
                   Tested Species Homo sapiens (Human)
                   UniProt ID ANM1_HUMAN
          DIG Name: D&C red no. 28 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 0.7 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ANM1_HUMAN
          DIG Name: Diiodofluorescein 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 75000 nM (estimated based on the structural similarity with CHEMBL177756 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.898648649
                   Tested Species Homo sapiens (Human)
                   UniProt ID ANM1_HUMAN
          DIG Name: FD&C red no. 3 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 0.46 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ANM1_HUMAN
References
1 Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations. J Med Chem. 2007 Mar 22; 50(6):1241-53.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.

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