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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.

Bromodomain-containing protein 9 (BRD9) has emerged as an epigenetic target in hematologic malignancies. However, previous studies on BRD9 PROTACs reported MYC upregulation following chronic administration. Here, we describe bifunctional BRD9 PROTAC/immunomodulatory drug (IMiD) degraders engineered to simultaneously el...

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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