Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target.  WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach.  The authors identify a lead compound, ERAS-5024, which demonstrates potent in vitro antiproliferative activities in a panel of cell lines harboring the G12D mutation and exhibits robust in vivo efficacy with regression activity in a PDAC-CDX model.

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