Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP-Deleted Cancers.
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DOI: 10.1021/acs.jmedchem.1c01900
Abstract: The PRMT5•MTA complex has recently emerged as a new synthetically lethal drug target for the treatment of MTAP-deleted cancers. Here, we report the discovery of development candidate MRTX1719. MRTX1719 is a potent and selective binder… read more here.
Keywords: mrtx1719; prmt5 mta; mta complex; mtap deleted ... See more keywords
Abstract 4970: TNG462 is a potential best-in-class MTA-cooperative PRMT5 inhibitor for the treatment of MTAP-deleted solid tumors
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DOI: 10.1158/1538-7445.am2023-4970
Abstract: MTAP deletions occur in 10-15% of all human cancers, which provides one of the largest precision oncology patient populations. MTA-cooperative PRMT5 inhibitors leverage the well-characterized synthetic lethal relationship between PRMT5 inhibition and MTAP deletion. TNG908… read more here.
Keywords: mtap; mta cooperative; cooperative prmt5; mtap deleted ... 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 6273: CTS3157, a novel MTA-cooperative PRMT5 inhibitor for targeting MTAP-deleted human tumors
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-6273
Abstract: MTAP deletion is common in about 15% of all human cancers and coincides with the deletion of tumor suppressor locus containing CDKN2A/B. Methylthioadenosine (MTA), the substrate of MTAP, accumulates as a result of MTAP deletion.… read more here.
Keywords: cell; mtap; mta; cts3157 ... See more keywords