title: Profiling of Multiple Targets of Artemisinin Activated by Hemin in Cancer Cell Proteome.
abstract: The antimalarial drug artemisinin is found to have diverse biological activities ranging from anti-inflammatory to anticancer properties; however, as of today, the cellular targets and mechanism of action of this important compound have remained elusive. Here, we report the global protein target profiling of artemisinin in the HeLa cancer cell proteome using a chemical proteomics approach. In the presence of hemin, multiple proteins were targeted by artemisinin probe through covalent modification. Further studies revealed that reducing of hemin to heme by protein thiols was essential for endoperoxide activation and subsequent protein alkylation. Artemisinin may exert its synergistic therapeutic anticancer effects via modulation of a variety of cellular pathways through acting on multiple targets.
authors: CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences , Shanghai 200032, China.
authors: Yiqing
authors: Y
authors: Zhou
authors: CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences , Shanghai 200032, China.|University of Chinese Academy of Sciences , Beijing 100039, China.
authors: Weichao
authors: W
authors: Li
authors: CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences , Shanghai 200032, China.
authors: Youli
authors: Y
authors: Xiao
mesh_terms: D037621:Artemisinins / Q000494:pharmacology*; D006427:Hemin / Q000378:metabolism*; D006801:Humans; D020543:Proteome
chemical_list: D037621:Artemisinins; D020543:Proteome; D006427:Hemin; C031327:artemisinin