Tchem PRMT1 Protein arginine N-methyltransferase 1

Protein Summary

Description

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, PIAS1, HNRNPA1, HNRNPD, NFATC2IP, SUPT5H, TAF15, EWS, HABP4 and SERBP1 (PubMed:16879614, PubMed:26876602). 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. Together with dimethylated PIAS1, represses STAT1 transcriptional activity, in the late phase of interferon gamma (IFN-gamma) signaling. 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. Methylates CHTOP and this methylation is critical for its 5-hydroxymethylcytosine (5hmC)-binding activity (PubMed:25284789). Methylates H4R3 in genes involved in glioblastomagenesis in a CHTOP- and/or TET1-dependent manner (PubMed:25284789). This gene encodes a member of the protein arginine N-methyltransferase (PRMT) family. Post-translational modification of target proteins by PRMTs plays an important regulatory role in many biological processes, whereby PRMTs methylate arginine residues by transferring methyl groups from S-adenosyl-L-methionine to terminal guanidino nitrogen atoms. The encoded protein is a type I PRMT and is responsible for the majority of cellular arginine methylation activity. Increased expression of this gene may play a role in many types of cancer. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene, and a pseudogene of this gene is located on the long arm of chromosome 5. [provided by RefSeq, Dec 2011]

Uniprot Accession IDs

• Q99873
• A0A087X1W2
• B4E3C3
• G5E9B6
• H7C2I1
• Q15529
• Q2VP93
• Q6LEU5
• Q8WUW5
• Q99872
• Q99874
• Q9NZ04
• Q9NZ05
• Q9NZ06

Gene Name

• PRMT1

Ensembl ID

• ENST00000391851
• ENSP00000375724
• ENSG00000126457
• ENST00000454376
• ENSP00000406162
• ENST00000610806
• ENSP00000484505

Symbol

• HMT2
• HRMT1L2
• IR1B4
• ANM1
• HCP1
• IR1B4
• HRMT1L2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
co-expressed gene	0.99
hub protein	0.92
transcription factor binding site profile	0.9
transcription factor	0.89
interacting protein	0.76

Protein Classes

DTO Classes

Protein / Epigenetic Regulator / Writer / Protein Methyltransferase / Protein Arginine Methyltransferase / Protein Arginine N-methyltransferase 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 398.92   (req: < 5)

Gene RIFs: 195   (req: <= 3)

Antibodies: 509   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 398.92   (req: >= 5)

Gene RIFs: 195   (req: > 3)

Antibodies: 509   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 33

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 28

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1