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The development of small-molecule inhibitors that target PRC2-related proteins
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Jing GU1, 2, Xiao-ke GUO1, 2, *, Qi-dong YOU1, 2, *
Acta Pharmaceutica Sinica | 2020, 55(8) : 1726 - 1734
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Acta Pharmaceutica Sinica | 2020, 55(8): 1726-1734
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The development of small-molecule inhibitors that target PRC2-related proteins
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Jing GU1, 2, Xiao-ke GUO1, 2, *, Qi-dong YOU1, 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: 2020-08-12 doi: 10.16438/j.0513-4870.2020-0049
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Abnormal expression of polycomb repressive complex 2 (PRC2) is related to the development of a variety of diseases. Inhibition of normal or overactive PRC2 can reduce cell survival and inhibit tumor growth in several cancers. Therefore, the identification and development of small molecule inhibitors has become an active field of current epigenetic-related anti-tumor strategies. A small molecule inhibitor targeting the S-adenosyl-L-methionine (SAM) binding site of enhancer of zeste homologue 2 (EZH2) has been approved by FDA. However, acquired drug resistance is of concern. Drugs targeting two different binding sites of embryonic ectoderm development (EED) are also being developed. The development of EZH2-EED proton pump inhibitor has attracted extensive attention due to its unique mechanism of action. In this paper, we review the research progress on various small molecule inhibitors that target PRC2-related proteins to provide a basis for further research and development of related drugs.

epigenetic  /  polycomb repressive complex 2  /  inhibitor  /  protein-protein interaction  /  anti-tumor
Jing GU, Xiao-ke GUO, Qi-dong YOU. The development of small-molecule inhibitors that target PRC2-related proteins[J]. Acta Pharmaceutica Sinica, 2020 , 55 (8) : 1726 -1734 . DOI: 10.16438/j.0513-4870.2020-0049
Year 2020 volume 55 Issue 8
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Article Info
doi: 10.16438/j.0513-4870.2020-0049
  • Receive Date:2020-01-15
  • Online Date:2026-01-21
  • Published:2020-08-12
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  • Received:2020-01-15
  • Accepted:2020-02-20
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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

Family
属数
Number of
genus
种数
Number of
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占总种数比例
Percentage of
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Genus
种数
Number of
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占总种数比例
Percentage of total
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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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