Abstract 3452: TNG908, a brain-penetrant MTA-cooperative PRMT5 inhibitor, is efficacious in preclinical glioblastoma models
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DOI: 10.1158/1538-7445.am2023-3452
Abstract: Glioblastoma multiforme (GBM) is one of the most aggressive primary malignant brain tumors in adults. The median overall survival (OS) of GBM patients is poor (1-2 years) on standard of care therapies, which include surgery,… read more here.
Keywords: prmt5 inhibitor; tng908; brain; mta cooperative ... See more keywords
Abstract 6272: AZ-PRMT5i-1: A potent MTAP-selective PRMT5 inhibitor with pharmacodynamic and monotherapy anti-tumor activity in MTAP-deleted tumours
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DOI: 10.1158/1538-7445.am2023-6272
Abstract: Background: PRMT5 is an epigenetic enzyme that catalyzes symmetric dimethylation of arginine substrates (SDMA), regulating multiple cell processes. The PRMT5-MTAP collateral vulnerability describes the accumulation of the metabolite methylthioadenosine (MTA) in tumor cells (as a… read more here.
Keywords: mtap; mtap deleted; prmt5 inhibitor; tumor ... See more keywords
Abstract 3905: Translational efficacy and safety modeling and simulation to support the clinical development of JNJ-64619178, a PRMT5 inhibitor
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DOI: 10.1158/1538-7445.sabcs18-3905
Abstract: Protein arginine methyltransferase 5 (PRMT5) is an epigenetic enzyme with oncogenic properties. JNJ-64619178 (JNJ178) is a potent, selective, structurally unique PRMT5 inhibitor with good preclinical efficacy in inhibiting the growth of hematologic and solid tumor… read more here.
Keywords: efficacy; safety; tumor; prmt5 inhibitor ... See more keywords
Epigenetic drug screening defines a PRMT5 inhibitor–sensitive pancreatic cancer subtype
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DOI: 10.1172/jci.insight.151353
Abstract: Systemic therapies for pancreatic ductal adenocarcinoma (PDAC) remain unsatisfactory. Clinical prognosis is particularly poor for tumor subtypes with activating aberrations in the MYC pathway, creating an urgent need for novel therapeutic targets. To unbiasedly find… read more here.
Keywords: pancreatic cancer; drug; prmt5 inhibitor; inhibitor sensitive ... See more keywords