Preferred Label : Protein Arginine Methyltransferase 5 Inhibitor PF-06939999;
NCIt synonyms : PRMT5 Inhibitor PF-06939999;
NCIt related terms : PF-06939999;
NCIt definition : An orally available inhibitor of protein arginine N-methyltransferase 5 (histone-arginine
N-methyltransferase PRMT5; PRMT5) with potential antiproliferative and antineoplastic
activities. Although the mechanism of action has not yet been fully elucidated, orally
administered PRMT5 inhibitor PF-06939999 inhibits the methyltransferase activity of
PRMT5, thereby decreasing the levels of monomethylated and dimethylated arginine residues
in histones H2A, H3, and H4, and modulating the expression of genes involved in several
cellular processes including cell proliferation. This may increase the expression
of antiproliferative genes and/or decrease the expression of genes that promote cell
proliferation, and may decrease the 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 : JY9FEZ3ZDX;
CAS number : 2159123-14-3; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2159123-14-3
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G-SRS /a ;
Molecule name : PF-06939999; PF 06939999;
NCI Metathesaurus CUI : CL937738;
Origin ID : C158100;
UMLS CUI : C4764049;
Semantic type(s)
- concept_is_in_subset
- has_target
