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- NCIT_C192819 IAO_0000115 "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." @default.
- NCIT_C192819 NCIT_A7 NCIT_C127857 @default.
- NCIT_C192819 NCIT_NHC0 "C192819" @default.
- NCIT_C192819 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C192819 NCIT_P108 "PRMT5 Inhibitor AUR-105" @default.
- NCIT_C192819 NCIT_P322 "GDC" @default.
- NCIT_C192819 NCIT_P399 "811660" @default.
- NCIT_C192819 normalizedInformationContent "100" @default.
- NCIT_C192819 referenceCount "1" @default.
- NCIT_C192819 hasExactSynonym "AUR 105" @default.
- NCIT_C192819 hasExactSynonym "AUR-105" @default.
- NCIT_C192819 hasExactSynonym "AUR105" @default.
- NCIT_C192819 hasExactSynonym "PRMT5 Inhibitor AUR-105" @default.
- NCIT_C192819 hasExactSynonym "Protein Arginine Methyltransferase 5 Inhibitor AUR-105" @default.
- NCIT_C192819 inSubset NCIT_C128784 @default.
- NCIT_C192819 inSubset NCIT_C157711 @default.
- NCIT_C192819 inSubset NCIT_C157712 @default.
- NCIT_C192819 inSubset NCIT_C176424 @default.
- NCIT_C192819 type Class @default.
- NCIT_C192819 isDefinedBy ncit.owl @default.
- NCIT_C192819 label "PRMT5 Inhibitor AUR-105" @default.
- NCIT_C192819 subClassOf NCIT_C163968 @default.
- NCIT_C192819 subClassOf NCIT_C1908 @default.
- NCIT_C192819 subClassOf NCIT_C1909 @default.
- NCIT_C192819 subClassOf NCIT_C192819 @default.
- NCIT_C192819 subClassOf NCIT_C471 @default.