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Synthesis, evaluation and proteomic analysis of PROTAC based on parthenolide
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Tong GAO1, Wen-tao ZHANG2, Shan-shan SONG3, Di ZHOU1, Tong-chao LIU3, *, Ze-hong MIAO3, Bing XIONG3, *
Acta Pharmaceutica Sinica | 2023, 58(9) : 2715 - 2726
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Acta Pharmaceutica Sinica | 2023, 58(9): 2715-2726
Synthesis, evaluation and proteomic analysis of PROTAC based on parthenolide
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Tong GAO1, Wen-tao ZHANG2, Shan-shan SONG3, Di ZHOU1, Tong-chao LIU3, *, Ze-hong MIAO3, Bing XIONG3, *
Affiliations
  • 1. Anhui University of Chinese Medicine, Hefei 230031, China
  • 2. Shenyang Pharmaceutical University, Shenyang 110016, China
  • 3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Published: 2023-09-12 doi: 10.16438/j.0513-4870.2023-0228
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As a natural product with a long history of medicinal use, parthenolide has aroused great interest of chemists and biologists. Existing studies have shown that it has anti-inflammatory, antitumor and other pharmacological activities, and also revealed its action on NF-κB signaling pathway, DNMT1 enzyme and Wnt/β-catenin signaling pathway. But its biological targets remain to be elucidated systematically. Proteolysis Targeting Chimeras (PROTAC) provides a new strategy for target discovery of natural products, which can be used to explore the panorama of protein changes in cells through proteomic investigation, so as to analyze their potential targets. Based on this idea, current study designed and synthesized 20 parthenolide-derived degraders. After measured their antitumor activity in vitro, selected compounds were carried out the proteomic experiment. Finally, 139 down-regulated differentially expressed proteins were identified and the discovery of parthenolide interacting protein was preliminarily explored.

parthenolide  /  PROTAC  /  target  /  antitumor  /  proteomics
Tong GAO, Wen-tao ZHANG, Shan-shan SONG, Di ZHOU, Tong-chao LIU, Ze-hong MIAO, Bing XIONG. Synthesis, evaluation and proteomic analysis of PROTAC based on parthenolide[J]. Acta Pharmaceutica Sinica, 2023 , 58 (9) : 2715 -2726 . DOI: 10.16438/j.0513-4870.2023-0228
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Article Info
doi: 10.16438/j.0513-4870.2023-0228
  • Receive Date：2023-02-27
  • Online Date：2025-11-21
  • Published：2023-09-12
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History
  • Received：2023-02-27
  • Revised：2023-03-28
Affiliations
    1. Anhui University of Chinese Medicine, Hefei 230031, China
    2. Shenyang Pharmaceutical University, Shenyang 110016, China
    3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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