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Article

Rational Design of Potent and Orally Efficacious PI3Kα/δ Degrader for PIK3CA Mutant Breast Cancer without Hyperglycemic Liability.

Journal of medicinal chemistry - 9 Apr 2026

Hou Yi, Zheng Xinqing, Zhang Yiwen, Shen Hao, Kang Chenxun, Qin Han, Cao Shuyang, Zhu Yasheng, Wang Xiao, Sun Chengliang, Ding Jiayu, Shi Zhongrui, Wang Liping, Yuan Kai, Min Wenjian, Yang Peng

Abstract excerpt

Although PROTAC technology has been reported for targeted PI3K degradation in cancer therapy, the rational design of isoform-selective PI3K PROTACs and their safety profiles compared to their cognate small-molecule inhibitors remain unexplored. We have reported a structure-guided PROTAC development strategy for selective PI3Kα/δ degradation. This approach enabled the rational design of copanlisib-based PROTACs,...

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PMID: 41796700
DOI: 10.1021/acs.jmedchem.5c03368

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PIK3CA

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 8 Sept 2026.

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