Chemical proteomic profiling with photoaffinity labeling strategy identifies antimalarial targets of artemisinin

• Published in: Chinese chemical letters Vol. 34; no. 12; pp. 108296 - 465
• Main Authors: Gao, Peng, Chen, Jiayun, Sun, Peng, Wang, Jianyou, Tang, Huan, Xia, Fei, Gu, Liwei, Zhang, Huimin, Wang, Chen, Wong, Yin Kwan, Zhu, Yinhua, Xu, Chengchao, Wang, Jigang
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.12.2023; Artemisinin Research Center,and Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China%Pharmaceutical College,Henan University,Kaifeng 475004,China%Shandong Academy of Chinese Medicine,Ji'nan 250014,China%Artemisinin Research Center,and Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700,China; Shandong Academy of Chinese Medicine,Ji'nan 250014,China; Department of Nephrology,Shenzhen Key Laboratory of Kidney Diseases,Shenzhen Clinical Research Centre for Geriatrics,Shenzhen People's Hospital,The First Affiliated Hospital,Southern University of Science and Technology,Shenzhen 518020,China
• Subjects: Artemisinin Antimalarial Chemical proteomic Target identification Photoaffinity probe; Artemisinin Antimalarial Chemical proteomic Target identification Photoaffinity probe; Antimalarial; Chemical proteomic; Target identification; Artemisinin; Photoaffinity probe
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2023.108296

Present research on the antimalarial mechanisms of artemisinin (ART) is mainly focused on covalent drug binding targets alkylated by free radicals, while non-covalent binding targets have rarely been reported. Here, we developed a novel photoaffinity probe of ART to globally capture and identify the antimalarial target proteins of ART through chemical proteomics. The results demonstrated that ART can bind to parasite proteins by both covalent and non-covalent modification, and these may jointly contribute to the antimalarial effects. Our work enriches the research on the antimalarial targets of ART, and provides a new perspective for further exploring the antimalarial mechanism of ART. Here, we developed a novel photoaffinity probe of artemisinin (ART) to capture and identify globally the antimalarial target proteins of ART through chemical proteomics. [Display omitted]