Preferred Label : Pemrametostat;
NCIt synonyms : PRMT5 Inhibitor GSK3326595; Protein Arginine Methyltransferase 5 Inhibitor GSK3326595;
NCIt definition : An orally available, selective small molecule inhibitor of protein arginine methyltransferase
5 (PRMT5), with potential antiproliferative and antineoplastic activities. Although
the mechanism of action has not been completely determined, pemrametostat binds to
the substrate recognition site of PRMT5 following oral administration and inhibits
its methyltransferase activity, which decreases the levels of both monomethylated
and dimethylated arginine residues in histones H2A, H3 and H4 and modulates the expression
of genes involved in several cellular processes, including cell proliferation. Therefore,
this agent may increase the expression of antiproliferative genes and/or decrease
the expression of genes that promote cell proliferation and may lead to decreased
growth of rapidly proliferating cells, including cancer cells. PRTM5, an arginine
methyltransferase that can catalyze the formation of both omega-N monomethylarginine
(MMA) and symmetrical dimethylarginine (sDMA) on histones and a variety of other protein
substrates, is overexpressed in several neoplasms.;
UNII : VXT8SZ6875;
InChIKey : JLCCNYVTIWRPIZ-NRFANRHFSA-N;
CAS number : 1616392-22-3; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1616392-22-3
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G-SRS /a ;
Molecule name : EPZ015938; GSK-3326595;
NCI Metathesaurus CUI : CL540166;
Origin ID : C142177;
UMLS CUI : C5446314;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
