Histone lysine demethylase 4 (KDM4) enzymes are frequently overexpressed in cancer and are considered to be promising therapeutic targets. QC6352, which is widely used as a best-in-class KDM4 chemical probe, shows potent antitumor activity across cancer models. Using comprehensive chemical biology approaches in gliobla...
Jayden Sterling, Jacinda R. Holtsmark, George L. Joun et al.· Nature Chemical Biology· 1 citation
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.· bioRxiv· 1 citation
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.· Journal of Medicinal Chemist...· 0 citations
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.· Journal of Medicinal Chemist...· 0 citations
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