Chemical proteomic profiling reveals prostaglandin termination enzyme PTGR2 as a key molecular target of natural coumarin fraxetin

Natural coumarins represent a diverse group of secondary metabolites with a wide range of biological activities. However, their specific molecular targets have remained largely unexplored. Employing chemical proteomics, a comprehensive analysis of the protein targets of the natural coumarin fraxetin has been conducted. Prostaglandin reductase 2 (PTGR2), a key enzyme involved in the final inactivation of prostaglandins, was identified as a primary target of fraxetin. Inhibition of PTGR2 can lead to the accumulation of 15-keto-PGE2, which subsequently activates the Nrf2 signaling pathway and suppresses NF-κB, resulting in notable anti-inflammatory effects. These findings provide novel insights into the molecular targets of fraxetin and other coumarins, which are crucial for fully exploring their therapeutic potential.

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Publication Details

Journal
Chemical Communications
Published
2025-01-01
DOI
https://doi.org/10.1039/d4cc05681g
Citations
1
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.94

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Chemical proteomic profiling reveals prostaglandin termination enzyme PTGR2 as a key molecular target of natural coumarin fraxetin

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Chemical proteomic profiling reveals prostaglandin termination enzyme PTGR2 as a key molecular target of natural coumarin fraxetin

Jie Lian, Weining Zhao, Shuo Song, Yangyang Bian, Fangrui Zhong, Yu Fu, Juan Shi, Songyao Kang, Zhiwei Cai, Yuqing Wang, Zhou Zhang, Yin Qing, Jianhua Liu, Fangyuan Zhao, Ang Dai
article en
1 citations

Abstract

Natural coumarins represent a diverse group of secondary metabolites with a wide range of biological activities. However, their specific molecular targets have remained largely unexplored. Employing chemical proteomics, a comprehensive analysis of the protein targets of the natural coumarin fraxetin has been conducted. Prostaglandin reductase 2 (PTGR2), a key enzyme involved in the final inactivation of prostaglandins, was identified as a primary target of fraxetin. Inhibition of PTGR2 can lead to the accumulation of 15-keto-PGE2, which subsequently activates the Nrf2 signaling pathway and suppresses NF-κB, resulting in notable anti-inflammatory effects. These findings provide novel insights into the molecular targets of fraxetin and other coumarins, which are crucial for fully exploring their therapeutic potential.

Chemical CommunicationsVol. 61(12)
South China Agricultural University (CN), China University of Mining and Technology (CN), Northwest University (CN), Ministry of Agriculture and Rural Affairs (CN), Shenzhen Technology University (CN), Shenzhen Genoimmune Medical Institute (CN), Huazhong University of Science and Technology (CN)
National Natural Science Foundation of China, Shuangchuang Program of Jiangsu Province, Guangdong Provincial Pearl River Talents Program
Openalex Percentile: Top 30%
Click Chemistry and Applications
0.94
DOISourceOpenAlex
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