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.
Protein Arginine Methyltransferase Inhibitors |
|
|---|---|
| Cat. No. | Product Name / Activity |
| 6516 | EPZ 015666 |
| Potent and selective PRMT5 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 | |
| 6825 | SGC 3027 |
| Potent and selective PRMT7 inhibitor | |
| 7182 | SGC 6870 |
| Potent and selective PRMT6 allosteric inhibitor | |
| 5367 | SGC 707 |
| Potent and selective allosteric inhibitor of PRMT3 | |
| 6008 | TP 064 |
| Potent and selective PRMT 4 inhibitor | |
| 5057 | UNC 2327 |
| Allosteric inhibitor of PRMT3 | |
Degraders |
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| Cat. No. | Product Name / Activity |
| 8080 | MS 4322 New |
| Selective PRMT5 Degrader (PROTAC®); potent PRMT5 inhibitor | |
Controls |
|
| Cat. No. | Product Name / Activity |
| 6838 | SGC 3027N |
| Negative control for SGC 3027 (Cat. No. 6825) | |
| 7184 | SGC 6870N |
| Negative control for SGC 6870 (Cat. No. 7182) | |
| 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
Tocris offers the following scientific literature for Protein Arginine Methyltransferases to showcase our products. We invite you to request* your copy today!
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
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 |
Our Epigenetics review gives an overview of the development of chemical probes for epigenetic targets, and discusses their biological effects.
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