General Information of the Protein
Protein ID
PT02223
Protein Name
Protein arginine N-methyltransferase 6
Secondarily
Protein Name
Heterogeneous nuclear ribonucleoprotein methyltransferase-like protein 6
Histone-arginine N-methyltransferase PRMT6
Gene Name
PRMT6
Secondarily
Gene Name
HRMT1L6
Sequence
MSQPKKRKLESGGGGEGGEGTEEEDGAEREAALERPRRTKRERDQLYYECYSDVSVHEEMIADRVRTDAYRLGILRNWAALRGKTVLDVGAGTGILSIFCAQAGARRVYAVEASAIWQQAREVVRFNGLEDRVHVLPGPVETVELPEQVDAIVSEWMGYGLLHESMLSSVLHARTKWLKEGGLLLPASAELFIAPISDQMLEWRLGFWSQVKQHYGVDMSCLEGFATRCLMGHSEIVVQGLSGEDVLARPQRFAQLELSRAGLEQELEAGVGGRFRCSCYGSAPMHGFAIWFQVTFPGGESEKPLVLSTSPFHPATHWKQALLYLNEPVQVEQDTDVSGEITLLPSRDNPRRLRVLLRYKVGDQEEKTKDFAMED
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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 can catalyze the formation of both omega-N monomethylarginine (MMA) and asymmetrical dimethylarginine (aDMA), with a strong preference for the formation of aDMA (PubMed:17898714, PubMed:18077460, PubMed:18079182, PubMed:19405910, PubMed:30420520). Preferentially methylates arginyl residues present in a glycine and arginine-rich domain and displays preference for monomethylated substrates (PubMed:17898714, PubMed:18077460, PubMed:18079182, PubMed:19405910). Specifically mediates the asymmetric dimethylation of histone H3 'Arg-2' to form H3R2me2a (PubMed:17898714, PubMed:18079182, PubMed:18077460). H3R2me2a represents a specific tag for epigenetic transcriptional repression and is mutually exclusive with methylation on histone H3 'Lys-4' (H3K4me2 and H3K4me3) (PubMed:17898714, PubMed:18077460). Acts as a transcriptional repressor of various genes such as HOXA2, THBS1 and TP53 (PubMed:19509293). Repression of TP53 blocks cellular senescence (By similarity). Also methylates histone H2A and H4 'Arg-3' (H2AR3me and H4R3me, respectively). Acts as a regulator of DNA base excision during DNA repair by mediating the methylation of DNA polymerase beta (POLB), leading to the stimulation of its polymerase activity by enhancing DNA binding and processivity (PubMed:16600869). Methylates HMGA1 (PubMed:16157300, PubMed:16159886). Regulates alternative splicing events. Acts as a transcriptional coactivator of a number of steroid hormone receptors including ESR1, ESR2, PGR and NR3C1. Promotes fasting-induced transcriptional activation of the gluconeogenic program through methylation of the CRTC2 transcription coactivator (By similarity). May play a role in innate immunity against HIV-1 in case of infection by methylating and impairing the function of various HIV-1 proteins such as Tat, Rev and Nucleocapsid protein p7 (NC) (PubMed:17267505). Methylates GPS2, protecting GPS2 from ubiquitination and degradation (By similarity). Methylates SIRT7, inhibiting SIRT7 histone deacetylase activity and promoting mitochondria biogenesis (PubMed:30420520).
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Uniprot ID
Primary ID:
Q96LA8

Secondarily ID:
A3KME1
B4DID8
Q5T5Y5
Q6DKI4
Q9NVR8
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Ensembl ID
ENSG00000198890
HGNC ID
HGNC:18241
Subcellular Location
Nucleus
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 = 637 nM
   TI
   LI
   LO
   TS
CP0873454
4-methyl-2-(3-(4-((methyl(2-(methylamino)ethyl)amino)methyl)-1H-pyrazol-5-yl)-5-(trifluoromethyl)phenoxy)pentan-1-ol
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C21H31F3N4O2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0021188
N-methyl-2-(4-phenylmethoxypiperidin-1-yl)ethanamine
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C15H24N2O
 3
1 IC50 = 34 nM
2 IC50 = 43 nM
3 Kd = 87 nM
CP0500197
(5R)-4-(5-bromofuran-2-carbonyl)-5-(4-fluorophenyl)-7-methyl-3,5-dihydro-1H-1,4-benzodiazepin-2-one
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C21H16BrFN2O3
 1
1 IC50 = 388 nM
CP0576665
4-(5-bromofuran-2-carbonyl)-5-(4-fluorophenyl)-7-methyl-3,5-dihydro-1H-1,4-benzodiazepin-2-one
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C21H16BrFN2O3
 1
1 IC50 = 755 nM
CP0032519
N-[3-[4-[[2-aminoethyl(methyl)amino]methyl]-1H-pyrrol-3-yl]phenyl]prop-2-enamide
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C17H22N4O
 1
1 Ki = 16 nM