Preferred Label : Anvumetostat;
NCIt synonyms : Protein Arginine Methyltransferase 5 Inhibitor AMG 193; PRMT5 Inhibitor AMG 193;
NCIt definition : An orally available small molecule inhibitor of protein arginine methyltransferase
5 (PRMT5), with potential antiproliferative and antineoplastic activities. Upon oral
administration, anvumetostat 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.;
UNII : QAT649EJ5E;
CAS number : 2790567-82-5;
Molecule name : AMG 193; AMG-193;
NCI Metathesaurus CUI : CL1773826;
Origin ID : C185417;
UMLS CUI : C5666988;
Semantic type(s)
- concept_is_in_subset
- has_target
