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Advances in nucleoside analogues as methyltransferase inhibitors
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Jun-jie ZHANG1, 2, Tong-chao LIU1, *, Bing XIONG1, 2, *
Acta Pharmaceutica Sinica | 2024, 59(5) : 1126 - 1150
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Acta Pharmaceutica Sinica | 2024, 59(5): 1126-1150
• Reviews •
Advances in nucleoside analogues as methyltransferase inhibitors
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Jun-jie ZHANG1, 2, Tong-chao LIU1, *, Bing XIONG1, 2, *
Affiliations
  • 1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 100049, China
Published: 2024-05-12 doi: 10.16438/j.0513-4870.2023-1406
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As the second largest cofactor after ATP in body, S-adenosyl-L-methionine (SAM) is responsible for methyl donor in SAM-dependent methyltransferases (MTases). The methylation of essential ingredients (e.g., DNA, RNA, protein) plays a critical role in epigenetic regulation, cellular signal transduction and metabolic cycles, which is closely related to different kinds of diseases. Therefore, SAM-dependent methyltransferases are considered as promising drug targets. Currently, a growing number of nucleoside analogues have been developed as SAM-competitive inhibitors, blocking the downstream signaling pathways to cure diseases. In the review, we outline the design strategy and optimization process of methyltransferase inhibitors, analyze the shortcomings and solutions of developing nucleoside derivatives as MTase inhibitors, to provide guidance and broad direction to the development of nucleoside MTase inhibitors.

epigenetics  /  S-adenosyl-L-methionine  /  methyltransferase  /  nucleoside analogue
Jun-jie ZHANG, Tong-chao LIU, Bing XIONG. Advances in nucleoside analogues as methyltransferase inhibitors[J]. Acta Pharmaceutica Sinica, 2024 , 59 (5) : 1126 -1150 . DOI: 10.16438/j.0513-4870.2023-1406
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Year 2024 volume 59 Issue 5
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Article Info
doi: 10.16438/j.0513-4870.2023-1406
  • Receive Date：2023-12-17
  • Online Date：2025-11-27
  • Published：2024-05-12
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History
  • Received：2023-12-17
  • Revised：2024-03-06
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Affiliations
    1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 100049, China
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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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