Discovery of the salicylaldehyde-based compound DDO-02267 as a lysine-targeting covalent inhibitor of ALKBH5 - Fei, Wen-Long; Wang, Ying-Zhe; Feng, Qing-Lan; Li, Cui-Ting; Jiang, Rui-Xin; Zhang, Shi-Di; Pan, Yun; Ni, Peng-Fei; Huang, Fei-Ran; Huangfu, Yi-Bing; Zhang, Shi-Da; You, Qi-Dong; et al. (European journal of medicinal chemistry, 2025)
Keywords: Aldehydes - chemistry; Aldehydes - pharmacology; AlkB Homolog 5, RNA Demethylase - antagonists & inhibitors; AlkB Homolog 5, RNA Demethylase - metabolism; ALKBH5; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Cell Proliferation - drug effects; Chemistry, Medicinal; Covalent inhibitor; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Humans; Life Sciences & Biomedicine; Lysine - chemistry; Lysine - metabolism; M6A; Molecular Structure; Pharmacology & Pharmacy; Salicylaldehyde warhead; Science & Technology; Structure-Activity Relationship; Salicylaldehyde warhead; M6A; ALKBH5; Covalent inhibitor; DEMETHYLASE; CELLS; KINASE INHIBITORS; MA