PRMT1 inhibitor GSK3368715
Term · Oncology and biomedicine · MLC-T-ONC-016222
An orally available inhibitor of protein arginine N-methyltransferase 1 (PRMT1; Histone-arginine N-methyltransferase PRMT1; Interferon receptor 1-bound protein 4) with potential antineoplastic activity. Upon administration, GSK3368715 inhibits monomethylation and asymmetric dimethylation of arginine-bearing substrates, including histones, estrogen receptors, RNA-binding proteins, and numerous non-histone substrates catalyzed by PRMT1. This may inhibit tumor cell proliferation, migration, and invasion that is potentially driven by PRMT1 overexpression or dysregulation. PRMT1-mediated methylation plays a key role in the modulation of protein function, gene expression and cellular signaling. Dysregulation and overexpression of PRMT1 has been associated with a number of solid and hematopoietic cancers.
| Identifier | MLC-T-ONC-016222 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | protein arginine methyltransferase 1 inhibitor GSK3368715 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-016222",
"term": "PRMT1 inhibitor GSK3368715",
"field": "Oncology and biomedicine",
"definition": "An orally available inhibitor of protein arginine N-methyltransferase 1 (PRMT1; Histone-arginine N-methyltransferase PRMT1; Interferon receptor 1-bound protein 4) with potential antineoplastic activity. Upon administration, GSK3368715 inhibits monomethylation and asymmetric dimethylation of arginine-bearing substrates, including histones, estrogen receptors, RNA-binding proteins, and numerous non-histone substrates catalyzed by PRMT1. This may inhibit tumor cell proliferation, migration, and invasion that is potentially driven by PRMT1 overexpression or dysregulation. PRMT1-mediated methylation plays a key role in the modulation of protein function, gene expression and cellular signaling. Dysregulation and overexpression of PRMT1 has been associated with a number of solid and hematopoietic cancers.",
"synonyms": [
"protein arginine methyltransferase 1 inhibitor GSK3368715"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/prmt1-inhibitor-gsk3368715/"
}
Record 13,641 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.