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

Author

Yu-Bo Zhou

h-index 29 View on Semantic Scholar

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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
Aug 2026

Discovery of BRD9 PROTAC/IMiD Bifunctional Molecules as Potent Therapeutics for Hematologic Malignancies.

Bifunctional BRD9 PROTAC/immunomodulatory drug (IMiD) degraders engineered to simultaneously eliminate BRD9 and IKZF1 validate this dual-targeting PROTAC/IMiD strategy as an effective approach to overcoming the limitations of selective BRD9 degraders, underscores its therapeutic potential in hematologic malignancies.

Hai-Ting Duan, Ruo-Xin Chen, Jing-Yu Zhang 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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