Protein Arginine Methyltransferases

Protein arginine methyltransferases are enyzmes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to the arginine residues on histones and other proteins. The dysregulation of this methylation is critical in the development of certain cancers.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5128 C 21
Selective PRMT1 inhibitor
5202 Furamidine dihydrochloride
Selective PRMT1 inhibitor
5777 GSK 591 dihydrochloride
Potent and selective PRMT5 inhibitor
5713 MS 023 dihydrochloride
Potent and selective type I PRMT inhibitor
5685 MS049 oxalate salt
Potent and selective PRMT4 and PRMT6 inhibitor
5367 SGC 707
Potent and selective allosteric inhibitor of PRMT3
5099 TC-E 5003
Selective PRMT1 inhibitor
6008 TP 064
Potent and selective PRMT 4 inhibitor
5057 UNC 2327
Allosteric inhibitor of PRMT3
5450 XY1
Negative control of SGC 707 (Cat. No. 5367)

Protein Arginine methyltransferases, or PRMTs, are a family of enyzmes that catalyze the transfer of methyl groups from S-adenosylmethionine (SAM) to arginine residues on histones. PRMTs belong to the histone methyltransferase group of enzymes, which also includes lysine methyltransferases. They are also closely related in biological activity to the DNA methyltransferases and are ubiquitously expressed. Histone methylation of arginine residues occurs predominantly on histones H2A, H3 and H4, and multiple methyl groups may be added to each residue.

Histones represent the major protein component of chromatin, around which DNA is coiled within the nucleus. Modification of histone protein by methylation induces chromatin remodeling which in turn alters gene expression. Histone methylation is an integral epigenetic process during development that represents an important mechanism of transcriptional regulation and chromatin remodeling. Dysregulation of histone methylation has been implicated in diseases, including cancer.

The epigenetic effects of histone methylation are dependent on the residue undergoing methylation, the degree of methylation and the modifying enzyme. PRMT methylation of histones may induce or inhibit transcription. In addition to histone methylation PRMTs have other effects including methylating and modulating transcription factors and effects on RNA stability and splicing

External sources of pharmacological information for Protein Arginine Methyltransferases :

    Literature for Protein Arginine Methyltransferases

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    Epigenetics

    Epigenetics Scientific Review

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    Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

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    Protein Arginine Methyltransferase Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    Protein arginine methyltransferase 1 Human PRMT1 NM_001207042 Q99873
    Mouse Prmt1 NP_062804 Q9JIF0
    Rat Prmt1 NM_024363 Q63009
    Protein arginine methyltransferase 2 Human PRMT2 NM_001535 P55345
    Mouse Prmt2 NP_001071106 Q9R144
    Rat Prmt2 NM_001025144 Q6AYB9
    Protein arginine methyltransferase 3 Human PRMT3 NM_005788 O60678
    Mouse Prmt3 NP_598501 Q922H1
    Rat Prmt3 NM_053557 O70467
    Coactivator-associated arginine methyltransferase 1 (PRMT4) Human CARM1 XM_032719 Q86X55
    Mouse Carm1 NP_067506 Q9WVG6
    Rat Carm1 NM_0010300414 Q4AE70
    Protein arginine methyltransferase 5 Human PRMT5 NM_001039619 O14744
    Mouse Prmt5 NP_038796 Q8CIG8
    Rat Prmt5 NM_001108867 D4A0E8
    Protein arginine methyltransferase 6 Human PRMT6 NM_018137 Q96LA8
    Mouse Prmt6 NM_178891 Q6NZB1
    Rat Prmt6 NM_001106466 D4A307
    Protein arginine methyltransferase 7 Human PRMT7 NM_019023 Q9NVM4
    Mouse Prmt7 NM_145404 Q922X9
    Rat Prmt7 NM_001014153 Q5U4E8
    Protein arginine methyltransferase 8 Human PRMT8 NM_019854 Q9NR22
    Mouse Prmt8 NM_201371 Q6PAK3
    Rat Prmt8 XM_002726433 F1LWG2