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- W4386822824 abstract "KRAS G12D mutation has been found in approximately 45% of pancreatic ductal adenocarcinoma (PDAC) cases, making it an attractive therapeutic target. Through structure-based drug design, a series of potent and selective KRAS G12D inhibitors were designed. The lead compound, ERAS-5024, inhibited ERK1/2 phosphorylation and cell proliferation in three-dimensional Cell-Titer Glo assays in AsPC-1 PDAC cells with single-digit nanomolar potency and caused tumor regression in the in vivo efficacy studies. We describe here the details of the design and synthesis program that led to the discovery of ERAS-5024." @default.
- W4386822824 created "2023-09-19" @default.
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- W4386822824 date "2023-09-18" @default.
- W4386822824 modified "2023-09-26" @default.
- W4386822824 title "Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors" @default.
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- W4386822824 doi "https://doi.org/10.1021/acsmedchemlett.3c00245" @default.
- W4386822824 hasPublicationYear "2023" @default.
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