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Author

Lewis Elson

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Open access Apr 2026

Macrocyclization of Broad-Spectrum Kinase Inhibitor Bosutinib Leads to Potent and Selective Quinoline-Based HIPK4 Inhibitor AZ137

A rational design strategy utilizing macrocyclization of a bosutinib-based scaffold provides a foundational framework for the validating HIPK4 as a therapeutic target and a high-quality resource to elucidate its roles in normal physiology and disease.

Athina Zerva, Nicolai D. Raig, Zai-Le Zhuang et al. · 1 citation
Open access Aug 2026

Selective Macrocyclic WEE1 Kinase Inhibitors with Strong Efficacy against Patient-Derived Colorectal Cancer Organoids

Significantly enhanced WEE1 inhibitory selectivity over PLK1 was determined for leading macrocycle 2, which also demonstrated broader kinome-wide selectivity and the X-ray cocrystal structure of 2 bound to WEE1 validated its computationally predicted bioactive binding mode.

Joel L Syphers, Josephine A. Wright, Adarsh Kumar et al. · 0 citations
Open access Aug 2026

Macrocyclization of Broad-Spectrum Kinase Inhibitor Bosutinib Leads to Potent and Selective Quinoline-Based HIPK4 Inhibitor AZ137

Homeodomain-interacting protein kinase 4 (HIPK4) remains an understudied member of the dark kinome. While genetic knockout studies suggest its involvement in spermiogenesis and cutaneous squamous cell carcinoma, whether these cellular functions can be recapitulated by pharmacological inhibition remains to be determin...

Athina Zerva, Nicolai D. Raig, Zaile Zhuang et al. · 0 citations

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