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Screening of small molecule inhibitors for PLK1 PBD and evaluation of antitumor activities
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Yu-huan JIANG1, Jing ZHANG2, Yun-yu CHEN2, Yan-hong WANG1, *, Shu-yi SI2, *
Acta Pharmaceutica Sinica | 2017, 52(3) : 409 - 415
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Acta Pharmaceutica Sinica | 2017, 52(3): 409-415
• ORIGINAL ARTICLES •
Screening of small molecule inhibitors for PLK1 PBD and evaluation of antitumor activities
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Yu-huan JIANG1, Jing ZHANG2, Yun-yu CHEN2, Yan-hong WANG1, *, Shu-yi SI2, *
Affiliations
  • 1. Heilongjiang University of Chinese Medicine, Haerbin 150000, China
  • 2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2017-03-12 doi: 10.16438/j.0513-4870.2017-0028
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With the method of fluorescence polarization (FP), we screened small molecule inhibitors for PLK1 PBD to identify the lead compounds for antitumor drugs. FP led to the identification of a potent hit, F083-0063, whose inhibition rate was (99.7±0.4)% at 10 μg·mL-1. The IC50 was calculated to be 1.9±0.1 μmol·L-1 using Graphpad Prism 5. The effect of the compound on cells' multiplication was measured by MTT assay which showed that F083-0063 inhibited the proliferation of many tumor cell lines. Flow cytometry analysis indicated that the F083-0063 promoted cell apoptosis and induced cell G2/M arrest. Migration abilities of cells, evaluated using scratch test, increased significantly in the presence of F083-0063 with the mi-gration rate as low as (37.6±0.7)% at 20 μmol·L-1. Molecular linkage technique found F083-0063 had good affinity with PLK1 PBD. The results of Western blotting showed that the expression of cyclin-dependent proteins was increased after treatment with F083-0063. In summary, F083-0063 has an antitumor activity and is expected to be an antitumor lead compound targeting PLK1 PBD.

antitumor drug  /  fluorescence polarization method  /  PLK1 PBD inhibitor  /  serine/threonine protein kinase  /  polo-like kinase inhibitor
Yu-huan JIANG, Jing ZHANG, Yun-yu CHEN, Yan-hong WANG, Shu-yi SI. Screening of small molecule inhibitors for PLK1 PBD and evaluation of antitumor activities[J]. Acta Pharmaceutica Sinica, 2017 , 52 (3) : 409 -415 . DOI: 10.16438/j.0513-4870.2017-0028
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Article Info
doi: 10.16438/j.0513-4870.2017-0028
  • Receive Date：2017-01-05
  • Online Date：2026-01-14
  • Published：2017-03-12
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  • Received：2017-01-05
  • Revised：2017-02-04
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    1. Heilongjiang University of Chinese Medicine, Haerbin 150000, China
    2. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
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Family		 属数
Number of
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Number of
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Percentage of
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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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