Preferred Label : PRMT5 Inhibitor BGB-58067;
NCIt synonyms : MTA-cooperative PRMT5 Inhibitor BGB-58067; PRMT5 Protein Inhibitor BGB-58067; MTA Cooperative PRMT5 Inhibitor BGB-58067; Protein Arginine Methyltransferase 5 Inhibitor BGB-58067;
NCIt definition : A methylthioadenosine (MTA)-selective inhibitor of the protein arginine methyltransferase
5 (PRMT5), with potential antineoplastic activity. Upon administration, PRMT5 inhibitor
BGB-58067 targets, binds to and inhibits PRMT5 in the presence of MTA, thereby specifically
inhibiting the function of PRMT5 solely within methylthioadenosine phosphorylase (MTAP)-deleted
cancer cells and not in normal, healthy cells. By inhibiting the methyltransferase
activity of PRMT5, levels of both monomethylated and dimethylated arginine residues
in certain histones and non-histone proteins are decreased. This modulates the expression
of genes involved in several cellular processes and 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 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 essential for the viability of cancer and normal cells. It is overexpressed in
several neoplasms. Elevated levels are associated with decreased patient survival.
MTAP is deleted in certain cancer cells leading to an accumulation of the metabolite
MTA. As MTA binds to and partially inhibits the activity of PRMT5, MTAP-deficient
cancer cells are specifically sensitive to PRMT5 inhibitors.;
Molecule name : BGB-58067; BGB 58067;
Origin ID : C212966;
concept_is_in_subset
- has_target
