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Sponsored Artificial Intelligence: A Modern Approach, Global Edition Artificial Intelligence: A Modern Approach, Global Edition

Author

Wen-Hai Huang

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Sep 2026

Discovery of a Potent, Selective, and Orally Efficacious STAT6 PROTAC for the Treatment of Atopic Dermatitis

Signal transducer and activator of transcription 6 (STAT6), a key mediator of IL-4/IL-13 signaling, regulates Th2 differentiation, making it an attractive target for atopic dermatitis (AD). The reported phosphopeptide-based STAT6 proteolysis-targeting chimera (PROTAC) established proof of concept for targeted STAT6 d...

Wen-Tao Wang, Meng-Yu Zhao, Liu-Zhi Hu et al. · 0 citations
Sep 2026

Design, synthesis, and structural optimization of novel pan-KRAS degrader for the treatment of KRAS-mutant pancreatic cancer.

KRAS, a frequently mutated oncogene, has been demonstrated to harbor multiple mutant variants. Although KRAS G12C inhibitors have been successfully approved for clinical use, their efficacy remains limited by acquired resistance and narrow patient eligibility. Here, we leveraged the proteolysis-targeting chimera (PROTA...

Shen-Xin Zeng, Yi-Qing Zhao, Yang-Qing Liu et al. · 0 citations
Open access Aug 2026

Discovery of a Potent and Selective KRAS G12D Degrader based on PROTAC Degradation.

This work designed and synthesized 20 novel KRAS G12D PROTACs based on the MRTX1133 derivative and found that compound VI-1 exhibited significant KRAS G12D degradation activity in PANC-0203 cells, achieving 69% effective degradation at 10 μM.

Lili Jiang, Wenyan Yang, Yanqing Liu et al. · 0 citations

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