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Author

Tie-Gen Chen

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Jul 2026

Discovery of a Highly Subtype-Selective AURKA PROTAC Degrader (CT3) with Superior Activity to the Inhibitor for Hematological Malignancies.

Aurora kinases, especially AURKA, are critical for mitotic regulation, and their dysregulation is linked to tumorigenesis, making AURKA a promising anticancer target. Conventional ATP-competitive AURKA inhibitors suffer from low subtype selectivity and failure to disrupt noncatalytic functions, resulting in limited the...

Yuanna Ye, Yalan Feng, Hao Wang et al. · 0 citations
Open access Aug 2026

Discovery of novel dual-target CDK12/PARP1 inhibitors for the treatment of triple-negative breast cancer.

The dual-target CDK12/PARP1 inhibitor 20b developed herein represents a novel lead molecule for TNBC drug development and exhibited markedly superior antiproliferative effects compared with single-target inhibitors and effectively reduced pSer2-CTD and PAR levels in TNBC cells.

Zhi-Jian Zhong, Miao Sun, Zhi-Wen Luo et al. · 0 citations

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