Web3410 - METEOR-1: A Phase I Study of GSK3326595, a First-In-Class Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor, in Advanced Solid Tumors Presenter: Lillian Siu Session: Proffered Paper – Developmental therapeutics Resources: Abstract Slides Webcast 29 Sep 2024 WebJul 1, 2024 · GSK3326595 is a potent, specific, and reversible inhibitor of PRMT5 that inhibits proliferation and induces cell death in a broad range of solid and hematologic …
PRMT5: a putative oncogene and therapeutic target in prostate …
WebJul 8, 2024 · GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases • GSK3368715 alters exon usage and has activity against multiple cancer models • GSK3368715 synergizes with the PRMT5 inhibitor GSK3326595 to inhibit tumor growth • MTAP gene deficiency impairs PRMT5 activity, sensitizing cancer cells to GSK3368715 … WebOct 1, 2024 · METEOR-1 is a phase I study to assess the safety, pharmacokinetics (PK), pharmacodynamics (PD), and efficacy of GSK3326595 in adults with solid tumors. Methods Eligible participants (pts) were >18 years with advanced or metastatic solid tumors. Pts were enrolled in a modified toxicity probability interval design. channing double sconce
A Phase II Window of Opportunity Trial of PRMT5 Inhibitor, GSK3326595 ...
WebGSK3326595 has efficacy in solid and heme cancer models • GSK3326595 is a selective inhibitor of PRMT5 • GSK3326595 inhibits global cellular SDMA, including SDMA on splicing proteins, regulators of translation, and transcription • PRMT5 inhibition leads to alternative splicing of . MDM4. and subsequent activation of p53 Webitor GSK3326595 in solid tumors and non-Hodgkin lymphoma (NCT02783300). This study was initiated 2 years' ago and is expected to be completed in 2024. However, the current PRMT5 inhibitors de-signed against its enzymatic activity lacks specificity for the individual downstream substrate. We have recently demonstrated that KLF4 is a rapidly ... WebJul 13, 2024 · In all, a methyl (-CH3) group from the methyl donor S-adenosylmethionine (SAM or AdoMet) is transferred to a guanidinium nitrogen of arginine on a target protein, generating a methylated guanidinium moiety and S-adenosylhomocysteine (SAH or AdoHcy), which is salvaged and re-used for methionine biosynthesis. channing disco