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Celastrol inhibits PAK1 kinase and inhibits the proliferation of pancreatic cancer cells
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Ling-xia ZHU1, 2, Xiao-yan SUN1, 2, Jiao CHEN1, 2, Xue-ting CAI1, 2, Peng CAO1, 2, *
Acta Pharmaceutica Sinica | 2020, 55(1) : 60 - 66
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Acta Pharmaceutica Sinica | 2020, 55(1): 60-66
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Celastrol inhibits PAK1 kinase and inhibits the proliferation of pancreatic cancer cells
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Ling-xia ZHU1, 2, Xiao-yan SUN1, 2, Jiao CHEN1, 2, Xue-ting CAI1, 2, Peng CAO1, 2, *
Affiliations
  • 1. Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing 210028, China, Nanjing University of Chinese Medicine, Nanjing 210023, China
  • 2. School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China
Published: 2020-01-12 doi: 10.16438/j.0513-4870.2019-0580
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The p21-activated kinase 1 (PAK1) is a member of the P21-activated protein kinase family that plays an important role in the proliferation and on cogenesis of pancreatic cancer. PAK1 is an important target for the treatment of pancreatic cancer. At present, akinase inhibitor targeting PAK1 is still in the preclinical research stage. Therefore, screening for new PAK1 kinase inhibitors is of great significance. In this study the natural compound celastrol was found to have a significant inhibitory effect on PAK1, with an IC50 value of 3.614 μmol·L-1. Molecular docking results showed that celastrol had good binding to PAK1. An MTT assay indicated that celastrol inhibited the proliferation of pancreatic cancer cells BxPC-3 and PANC-1. Mechanistic studies revealed that the inhibition of pancreatic cancer cells by celastrol was reversed by PAK1 siRNA. Celastrol inhibited PAK1 and the subsequent activation of downstream signaling pathways, thereby activating apoptosis signaling pathways and triggering apoptosis in pancreatic cancer cells. These findings suggested that celastrol induced apoptosis in pancreatic cancer cells by suppressing the PAK1 kinase signaling pathway and has potential value for the treatment of pancreatic cancer.

p21-activated kinase 1  /  pancreatic neoplasms  /  tripterine  /  proliferation  /  apoptosis
Ling-xia ZHU, Xiao-yan SUN, Jiao CHEN, Xue-ting CAI, Peng CAO. Celastrol inhibits PAK1 kinase and inhibits the proliferation of pancreatic cancer cells[J]. Acta Pharmaceutica Sinica, 2020 , 55 (1) : 60 -66 . DOI: 10.16438/j.0513-4870.2019-0580
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Article Info
doi: 10.16438/j.0513-4870.2019-0580
  • Receive Date：2019-07-19
  • Online Date：2026-01-20
  • Published：2020-01-12
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History
  • Received：2019-07-19
  • Revised：2019-09-05
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Affiliations
    1. Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing 210028, China, Nanjing University of Chinese Medicine, Nanjing 210023, China
    2. 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
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
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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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