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Advances in histone epigenetic enzyme inhibitors based on proteomics
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Quan LIU1, 2, Lu-lu WANG1, 3, Jun-yu XU1, Min-jia TAN1, 2, 3, *
Acta Pharmaceutica Sinica | 2023, 58(9) : 2541 - 2550
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Acta Pharmaceutica Sinica | 2023, 58(9): 2541-2550
Advances in histone epigenetic enzyme inhibitors based on proteomics
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Quan LIU1, 2, Lu-lu WANG1, 3, Jun-yu XU1, Min-jia TAN1, 2, 3, *
Affiliations
  • 1. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 100049, China
  • 3. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
Published: 2023-09-12 doi: 10.16438/j.0513-4870.2022-0937
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As an important component of nucleosomes on the chromatin of eukaryotic cells, histones play an important role in the development and progression of tumour diseases by regulating epigenetic post-translational modifications such as acetylation and methylation. In addition, development of inhibitors targeting methyltransferase and deacetylase provides novel therapeutic strategies for cancer treatment. Mass spectrometry-based proteomics can reveal the global changes of histone modifications under the action of drugs during disease progression, which in turn provides important support for revealing drug action mechanism, drug resistance mechanism, and investigating novel drug combination strategies. This article focuses on the progress and status of proteomic research on a variety of histone modifying enzyme inhibitors, including methyltransferase inhibitors and histone deacetylase inhibitors, which will help to understand the current and further utilization of proteomics in studying histone modifications.

proteomics  /  histone modification  /  histone methyltransferase  /  histone deacetylase  /  epigenetic inhibitor
Quan LIU, Lu-lu WANG, Jun-yu XU, Min-jia TAN. Advances in histone epigenetic enzyme inhibitors based on proteomics[J]. Acta Pharmaceutica Sinica, 2023 , 58 (9) : 2541 -2550 . DOI: 10.16438/j.0513-4870.2022-0937
Year 2023 volume 58 Issue 9
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Article Info
doi: 10.16438/j.0513-4870.2022-0937
  • Receive Date:2022-07-29
  • Online Date:2025-11-21
  • Published:2023-09-12
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  • Received:2022-07-29
  • Revised:2022-09-13
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Affiliations
    1. State Key Laboratory of New Drug Research, Shanghai Institute of Materia Medica, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 100049, China
    3. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
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表12种不同金属材料的力学参数

Family
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Number of
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Number of
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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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