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Design, synthesis and activity evaluation of protein arginine methyltransferase 5 inhibitor
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Kang-le ZHU1, 2, Ya-zhou WANG2, *, Qi-dong YOU1, *
Acta Pharmaceutica Sinica | 2020, 55(8) : 1859 - 1871
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Acta Pharmaceutica Sinica | 2020, 55(8): 1859-1871
Design, synthesis and activity evaluation of protein arginine methyltransferase 5 inhibitor
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Kang-le ZHU1, 2, Ya-zhou WANG2, *, Qi-dong YOU1, *
Affiliations
  • 1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
  • 2. Nanjing Sanhome Pharmaceutical Co., Ltd., Nanjing 210000, China
Published: 2020-08-12 doi: 10.16438/j.0513-4870.2020-0568
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Protein arginine methyltransferase 5 (PRMT5) is an important type Ⅱ human methyltransferase. It catalyzes the symmetrical double-methylation of many histones and non-histones, and it is highly expressed in many kinds of tumors. PRMT5 has been proven to be a potential new target for cancer treatment. Based on the reported crystal complex of EPZ015666 with PRMT5, a series of new compounds was designed using GSK3326595 (EPZ015938) as the lead compound and using the conformational restriction approach. We found that compounds B8 and the C series of derivatives displayed enzyme inhibitory activity comparable to that of GSK3326595. Compounds C3 and C4 showed poor permeability in Caco-2 cells, and that might be one of the reasons for their poor anti-proliferative activity against Z-138 cells. These data provide insights for further structural optimization.

PRMT5  /  structural optimization  /  cancer  /  GSK332659
Kang-le ZHU, Ya-zhou WANG, Qi-dong YOU. Design, synthesis and activity evaluation of protein arginine methyltransferase 5 inhibitor[J]. Acta Pharmaceutica Sinica, 2020 , 55 (8) : 1859 -1871 . DOI: 10.16438/j.0513-4870.2020-0568
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Article Info
doi: 10.16438/j.0513-4870.2020-0568
  • Receive Date：2020-04-17
  • Online Date：2026-01-21
  • Published：2020-08-12
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  • Received：2020-04-17
  • Revised：2020-05-14
Funding
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    1. Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
    2. Nanjing Sanhome Pharmaceutical Co., Ltd., Nanjing 210000, 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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