Insilico Medicine reported the discovery of an AI‑designed PROTAC degrader, D16‑M1P2, targeting PKMYT1, a kinase implicated in cell‑cycle control and synthetic‑lethality vulnerabilities in certain tumors. The team used Insilico’s Chemistry42 generative platform to design the bifunctional molecule linking a novel PKMYT1 inhibitor to a cereblon binder. Preclinical studies showed potency in cell lines with CCNE1 amplification and FBXW7 mutations and efficacy in a CCNE1‑amplified breast cancer xenograft model. Insilico highlighted the biomarker‑driven strategy, proposing future clinical development focused on tumors with the genomic alterations that confer PKMYT1 dependency. The work, published in Nature Communications, illustrates how generative AI platforms can produce complex bifunctional modalities and accelerate preclinical lead identification for targeted oncology programs.
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