Preferred Label : PRMT5 Inhibitor AUR-105;
NCIt synonyms : Protein Arginine Methyltransferase 5 Inhibitor AUR-105;
NCIt definition : An orally available inhibitor of protein arginine methyltransferase 5 (PRMT5), with
potential antiproliferative and antineoplastic activities. Upon oral administration,
PRMT5 inhibitor AUR-105 selectively binds to PRMT5 and inhibits its function. By inhibiting
its methyltransferase activity, levels of both monomethylated and dimethylated arginine
residues in histones H2A, H3 and H4 are decreased. This modulates the expression of
genes involved in several cellular processes, including cellular proliferation. This
may increase the expression of antiproliferative genes and/or decrease the expression
of genes that promote cell proliferation, which may lead to decreased growth of rapidly
proliferating cells, including cancer cells. PRMT5, a type II methyltransferase that
catalyzes the formation of both omega-N monomethylarginine (MMA) and symmetric dimethylarginine
(sDMA) on histones and a variety of other protein substrates involved in signal transduction
and cellular transcription, is overexpressed in several neoplasms. Elevated levels
are associated with decreased patient survival. Methylthioadenosine phosphorylase
(MTAP) is deleted in certain cancer cells leading to an accumulation of methylthioadenosine
(MTA). As MTA inhibits PRMT5, MTAP-null cancer cells are specifically sensitive to
PRMT5 inhibitors.;
Molecule name : AUR 105; AUR-105;
NCI Metathesaurus CUI : CL1912850;
Origin ID : C192819;
UMLS CUI : C5785440;
Semantic type(s)
- concept_is_in_subset
- has_target
