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Cellular target identification of Withangulatin A using fluorescent analogues and subsequent chemical proteomics
Tianyu Zhu1, Chen Chen1, Sisi Wang1
1State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. luojg@cpu.edu.cn lykong@cpu.edu.cn.
Abstract:
Withangulatin A (WA) has been reported to exhibit potent antitumor activity. However, its possible mechanism and direct proteomic targets remain unknown. Herein we report the subcellular localization of WA by designing and synthesizing its fluorescent analogues with coumarin moieties. Furthermore, sarco/endoplasmic reticulum calcium-ATPase (SERCA)2 was identified as the potential target of WA for its antitumor activity by chemical proteomics.
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