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HTRF-based method for determination of HSP90-HOP inhibition activity and its application
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Hui-jie WANG1, Zi-han ZHOU3, Jia-chen XU1, Fen JIANG1, Qi-dong YOU1, 2, *, Xiao-li XU1, 2
Acta Pharmaceutica Sinica | 2017, 52(4) : 592 - 597
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Acta Pharmaceutica Sinica | 2017, 52(4): 592-597
• ORIGINAL ARTICLES Medicinal Chemistry •
HTRF-based method for determination of HSP90-HOP inhibition activity and its application
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Hui-jie WANG1, Zi-han ZHOU3, Jia-chen XU1, Fen JIANG1, Qi-dong YOU1, 2, *, Xiao-li XU1, 2
Affiliations
  • 1. Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
  • 2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
  • 3. Nanjing Foreign Language School, Nanjing 210008, China
Published: 2017-04-12 doi: 10.16438/j.0513-4870.2016-1177
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HSP90 is widely expressed in cells with the main function in assisting the maturation of other proteins that are called clients. Many clients play critical roles in the occurrence and development of cancer. Inhibition of HSP90 can lead to degradation of the oncogenic proteins, and result in potent anti-cancer effects. HSP90-HOP interaction is critical for the chaperone function of HSP90, thereby disruption of the HSP90-HOP interaction is a novel strategy in the inhibition of HSP90. Based on the technology of homogeneous time-resolved fluorescence (HTRF), we developed a new assay for the identification of new inhibitors of HSP90-HOP interaction. This method was evaluated in the study of the HSP90-HOP inhibition activity of the pentapeptide MEEVD from HSP90 C-terminal and its derivatives. This study can provide a basis for the screening and discovery of novel HSP90-HOP disruptors.

heat shock protein 90  /  HSP-organizing protein  /  homogeneous time-resolved fluorescence  /  protein-protein interaction
Hui-jie WANG, Zi-han ZHOU, Jia-chen XU, Fen JIANG, Qi-dong YOU, Xiao-li XU. HTRF-based method for determination of HSP90-HOP inhibition activity and its application[J]. Acta Pharmaceutica Sinica, 2017 , 52 (4) : 592 -597 . DOI: 10.16438/j.0513-4870.2016-1177
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Article Info
doi: 10.16438/j.0513-4870.2016-1177
  • Receive Date：2016-12-09
  • Online Date：2026-01-14
  • Published：2017-04-12
Article Data
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History
  • Received：2016-12-09
  • Revised：2017-01-04
Funding
Affiliations
    1. Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China
    2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China
    3. Nanjing Foreign Language School, Nanjing 210008, China
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表12种不同金属材料的力学参数
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Number 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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