Cellular target identification of Withangulatin A using fluorescent analogues and subsequent chemical proteomics
| Autor: | Tianyu Zhu, Jian-Guang Luo, Yi Zhang, Ling-Nan Li, Chen Chen, Sisi Wang, Dong-Rong Zhu, Ling-Yi Kong |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Proteomics
SERCA 010402 general chemistry 01 natural sciences Catalysis Sarcoplasmic Reticulum Calcium-Transporting ATPases chemistry.chemical_compound Coumarins Cell Line Tumor Materials Chemistry Humans Withangulatin A Fluorescent Dyes 010405 organic chemistry Chemistry Endoplasmic reticulum Metals and Alloys Pregnenes General Chemistry Subcellular localization Coumarin Fluorescence 0104 chemical sciences Surfaces Coatings and Films Electronic Optical and Magnetic Materials Microscopy Fluorescence Biochemistry Cell culture cardiovascular system Ceramics and Composites |
| Zdroj: | Chemical Communications. 55:8231-8234 |
| ISSN: | 1364-548X 1359-7345 |
| DOI: | 10.1039/c9cc03653a |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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