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- Frontier Medicines announced FMC-242, a covalent allosteric inhibitor that breaks the PI3Kα/RAS protein interaction to target major cancer drivers without metabolic side effects. - The compound was developed in just two years using the company's chemoproteomics and AI-powered platform, with IND filing anticipated for 2026. - FMC-242 shows potential as both monotherapy and combination treatment, potentially overcoming resistance to HER2, EGFR, and RAS inhibitors. - Preclinical and combination data will be presented at the AACR-NCI-EORTC International Conference on October 25, 2025.
- Frontier Medicines published groundbreaking research in Structure journal demonstrating that DCAF2 can be harnessed as a novel E3 ligase for targeted protein degradation. - The study presents the first high-resolution structures of DCAF2 complex using advanced cryogenic electron microscopy and the company's proprietary Frontier™ Platform. - DCAF2 shows frequent overexpression in various cancer types, offering new possibilities for developing tumor-targeted protein degraders against previously undruggable proteins. - This discovery expands the limited repertoire of E3 ligases available for therapeutic protein degradation beyond currently used targets like VHL and cereblon.
