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Advances in antitumor research of bifunctional small molecule inhibitors targeting heat shock protein 90
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Hong-ping ZHU1, Xin XIE1, Rui QIN1, Wei HUANG1, Yan-qing LIU1, Cheng PENG1, Gu HE2, *, Bo HAN1, *
Acta Pharmaceutica Sinica | 2024, 59(1) : 1 - 16
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Acta Pharmaceutica Sinica | 2024, 59(1): 1-16
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Advances in antitumor research of bifunctional small molecule inhibitors targeting heat shock protein 90
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Hong-ping ZHU1, Xin XIE1, Rui QIN1, Wei HUANG1, Yan-qing LIU1, Cheng PENG1, Gu HE2, *, Bo HAN1, *
Affiliations
  • 1. State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
  • 2. West China Hospital, Sichuan University, Chengdu 610041, China
Published: 2024-01-12 doi: 10.16438/j.0513-4870.2023-0388
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The heat shock protein 90 (Hsp90) protein family is a cluster of highly conserved molecules that play an important role in maintaining cellular homeostasis. Hsp90 and its co-chaperones regulate a variety of pathways and cellular functions, such as cell growth, cell cycle control and apoptosis. Hsp90 is closely associated with the occurrence and development of tumors and other diseases, making it an attractive target for cancer therapeutics. Inhibition of Hsp90 expression can affect multiple oncogenic pathways simultaneously. Most Hsp90 small molecule inhibitors are in clinical trials due to their low efficacy, toxicity or drug resistance, but they have obvious synergistic anti-tumor effect when used with histone deacetylase (HDAC) inhibitors, tubulin inhibitors or topoisomerase II (Topo II) inhibitors. To address this issue, the design of Hsp90 dual-target inhibitors can improve efficacy and reduce drug resistance, making it an effective tumor treatment strategy. In this paper, the domain and biological function of Hsp90 are briefly introduced, and the design, discovery and structure-activity relationship of Hsp90 dual inhibitors are discussed, in order to provide reference for the discovery of novel Hsp90 dual inhibitors and clinical drug research from the perspective of medicinal chemistry.

Hsp90  /  domain  /  biological function  /  dual inhibitor  /  antitumor activity
Hong-ping ZHU, Xin XIE, Rui QIN, Wei HUANG, Yan-qing LIU, Cheng PENG, Gu HE, Bo HAN. Advances in antitumor research of bifunctional small molecule inhibitors targeting heat shock protein 90[J]. Acta Pharmaceutica Sinica, 2024 , 59 (1) : 1 -16 . DOI: 10.16438/j.0513-4870.2023-0388
Year 2024 volume 59 Issue 1
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Article Info
doi: 10.16438/j.0513-4870.2023-0388
  • Receive Date:2023-03-30
  • Online Date:2025-11-28
  • Published:2024-01-12
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  • Received:2023-03-30
  • Revised:2023-04-05
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    1. State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
    2. West China Hospital, Sichuan University, Chengdu 610041, 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
species
占总种数比例
Percentage of
total species (%)

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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