Preferred Label : Onametostat;
NCIt synonyms : Protein Arginine Methyltransferase 5 Inhibitor JNJ-64619178; PRMT5 Inhibitor JNJ-64619178;
NCIt definition : An orally available small molecule inhibitor of protein arginine methyltransferase
5 (PRMT5), with potential antiproliferative and antineoplastic activities. Upon oral
administration,onametostat selectively targets and irreversibly binds to the S-adenosylmethionine
(SAM)- and substrate-binding pockets of the PRMT5/methylosome protein 50 (MEP50) complex,
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.;
UNII : N8VKI8FPW0;
InChIKey : DBSMLQTUDJVICQ-CJODITQLSA-N;
CAS number : 2086772-26-9;
Molecule name : JNJ-64619178; JNJ 64619178;
NCI Metathesaurus CUI : CL977245;
Origin ID : C163980;
UMLS CUI : C5446348;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
