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- NCIT_C200044 IAO_0000115 "A central nervous system (CNS)-penetrant, orally bioavailable small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), with potential antiproliferative and antineoplastic activities. Upon oral administration, PRMT5 inhibitor SKL27969 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_C200044 NCIT_NHC0 "C200044" @default.
- NCIT_C200044 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C200044 NCIT_P107 "PRMT5 Inhibitor SKL27969" @default.
- NCIT_C200044 NCIT_P108 "PRMT5 Inhibitor SKL27969" @default.
- NCIT_C200044 NCIT_P322 "CTRP" @default.
- NCIT_C200044 NCIT_P399 "812959" @default.
- NCIT_C200044 normalizedInformationContent "100" @default.
- NCIT_C200044 referenceCount "1" @default.
- NCIT_C200044 hasExactSynonym "PRMT5 Inhibitor SKL27969" @default.
- NCIT_C200044 hasExactSynonym "Protein Arginine Methyltransferase 5 Inhibitor SKL27969" @default.
- NCIT_C200044 hasExactSynonym "SKL 27969" @default.
- NCIT_C200044 hasExactSynonym "SKL-27969" @default.
- NCIT_C200044 hasExactSynonym "SKL27969" @default.
- NCIT_C200044 inSubset NCIT_C116977 @default.
- NCIT_C200044 inSubset NCIT_C116978 @default.
- NCIT_C200044 inSubset NCIT_C176424 @default.
- NCIT_C200044 type Class @default.
- NCIT_C200044 isDefinedBy ncit.owl @default.
- NCIT_C200044 label "PRMT5 Inhibitor SKL27969" @default.
- NCIT_C200044 subClassOf NCIT_C163968 @default.
- NCIT_C200044 subClassOf NCIT_C1908 @default.
- NCIT_C200044 subClassOf NCIT_C1909 @default.
- NCIT_C200044 subClassOf NCIT_C200044 @default.
- NCIT_C200044 subClassOf NCIT_C471 @default.