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The development of small-molecule inhibitors targeting MYC
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Jun-jie XU1, 2, Qi-dong YOU1, 2, *, Xiao-ke GUO1, 2, *
Acta Pharmaceutica Sinica | 2022, 57(6) : 1689 - 1701
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Acta Pharmaceutica Sinica | 2022, 57(6): 1689-1701
• Reviews •
The development of small-molecule inhibitors targeting MYC
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Jun-jie XU1, 2, Qi-dong YOU1, 2, *, Xiao-ke GUO1, 2, *
Affiliations
  • 1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 211198, China
  • 2. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
Published: 2022-06-12 doi: 10.16438/j.0513-4870.2021-1794
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The MYC gene, one of the most common dysregulated driver genes in human cancers, is composed of three paralogous genes C-MYC, N-MYC and L-MYC. It is abnormally activated in more than half of cancer types. Since MYC plays an important role in the formation, maintenance and progression of cancer, targeting MYC is an effective strategy for cancer treatment. As a potential anti-cancer target, MYC is considered "undruggable" because it lacks a suitable pocket for accommodating small molecule inhibitors. Recently, under the guidance of protein structure information and many computational tools, many indirect strategies to inhibit MYC have emerged and shown favorable anti-cancer effects in tumor models. In this paper, the recent small molecules that indirectly target MYC are divided into inhibitors acting on the protein-protein interaction (PPI) among MYC and other proteins, and targeting inhibitors regulating MYC action. Additionally, the introduction and assessment towards compounds with different mechanisms are summarized to provide reference for the further research of MYC inhibitors.

MYC  /  inhibitor  /  MYC associated factor X  /  guanine quadruplex  /  WD40 repeat protein 5
Jun-jie XU, Qi-dong YOU, Xiao-ke GUO. The development of small-molecule inhibitors targeting MYC[J]. Acta Pharmaceutica Sinica, 2022 , 57 (6) : 1689 -1701 . DOI: 10.16438/j.0513-4870.2021-1794
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Article Info
doi: 10.16438/j.0513-4870.2021-1794
  • Receive Date：2021-12-15
  • Online Date：2025-12-23
  • Published：2022-06-12
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  • Received：2021-12-15
  • Revised：2022-01-07
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Affiliations
    1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 211198, China
    2. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, 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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