General Information of the Protein
Protein ID
PT02218
Protein Name
Protein arginine N-methyltransferase 1
Secondarily
Protein Name
Histone-arginine N-methyltransferase PRMT1
Interferon receptor 1-bound protein 4
Gene Name
PRMT1
Secondarily
Gene Name
HMT2
HRMT1L2
IR1B4
Sequence
MAAAEAANCIMENFVATLANGMSLQPPLEEVSCGQAESSEKPNAEDMTSKDYYFDSYAHFGIHEEMLKDEVRTLTYRNSMFHNRHLFKDKVVLDVGSGTGILCMFAAKAGARKVIGIECSSISDYAVKIVKANKLDHVVTIIKGKVEEVELPVEKVDIIISEWMGYCLFYESMLNTVLYARDKWLAPDGLIFPDRATLYVTAIEDRQYKDYKIHWWENVYGFDMSCIKDVAIKEPLVDVVDPKQLVTNACLIKEVDIYTVKVEDLTFTSPFCLQVKRNDYVHALVAYFNIEFTRCHKRTGFSTSPESPYTHWKQTVFYMEDYLTVKTGEEIFGTIGMRPNAKNNRDLDFTIDLDFKGQLCELSCSTDYRMR
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Writer
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Protein methyltransferase
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Protein arginine methyltransferase
Function
Arginine methyltransferase that methylates (mono and asymmetric dimethylation) the guanidino nitrogens of arginyl residues present in proteins such as ESR1, histone H2, H3 and H4, FMR1, ILF3, HNRNPA1, HNRNPD, NFATC2IP, SUPT5H, TAF15, EWS, HABP4, SERBP1, RBM15, FOXO1, CHTOP and MAP3K5/ASK1 (PubMed:10749851, PubMed:16879614, PubMed:26876602, PubMed:22095282, PubMed:26575292, PubMed:18951090, PubMed:25284789, PubMed:30765518). 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. Methylates RBM15, promoting ubiquitination and degradation of RBM15 (PubMed:26575292). Methylates FOXO1 and retains it in the nucleus increasing its transcriptional activity (PubMed:18951090). Methylates CHTOP and this methylation is critical for its 5-hydroxymethylcytosine (5hmC)-binding activity (PubMed:25284789). Methylates MAP3K5/ASK1 at 'Arg-78' and 'Arg-80' which promotes association of MAP3K5 with thioredoxin and negatively regulates MAP3K5 association with TRAF2, inhibiting MAP3K5 stimulation and MAP3K5-induced activation of JNK (PubMed:22095282). Methylates H4R3 in genes involved in glioblastomagenesis in a CHTOP- and/or TET1-dependent manner (PubMed:25284789). Plays a role in regulating alternative splicing in the heart (By similarity).
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Uniprot ID
Primary ID:
Q99873

Secondarily ID:
A0A087X1W2
B4E3C3
G5E9B6
H7C2I1
Q15529
Q2VP93
Q6LEU5
Q8WUW5
Q99872
Q99874
Q9NZ04
Q9NZ05
Q9NZ06
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Ensembl ID
ENSG00000126457
HGNC ID
HGNC:5187
Subcellular Location
Nucleus
Nucleus
Nucleoplasm
Cytoplasm
Cytoplasm
Cytosol
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000045 , A-375
Compound ID Compound Name Compound Formula
CP0849394
(trans)-N1,N2-dimethyl-N1-((3-(4-(3-(2-(tetrahydro-2H-pyran-4-yl)ethoxy)cyclobutoxy)phenyl)-1H-pyrazol-4-yl)methyl)ethane-1,2-diamine
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C25H38N4O3
 1
1
IC50 = 7100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0032519
N-[3-[4-[[2-aminoethyl(methyl)amino]methyl]-1H-pyrrol-3-yl]phenyl]prop-2-enamide
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C17H22N4O
 1
1 IC50 = 100 nM
CP0134320
N-[3-[4-[[2-aminoethyl(methyl)amino]methyl]-1H-pyrrol-3-yl]phenyl]propanamide
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C17H24N4O
 1
1 IC50 = 170 nM
CP0011023
AdoHcy
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C14H20N6O5S
 3
1 IC50 = 250 nM
2 IC50 = 500 nM
3 Ki = 400 nM
CP0800560
sodium 7,7'-carbonylbis(azanediyl)bis(4-hydroxynaphthalene-2-sulfonate)
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C21H14N2Na2O9S2
 3
1 IC50 = 8800 nM
2 IC50 = 9000 nM
3 IC50 = 22000 nM
Clinical Information about the Protein
Target 1 ( Protein arginine methyltransferase 1 (PRMT1) )
Target Type Clinical trial Target