Structural Optimization of Pyrazole Compounds as Hsp90 Regulators with Enhanced Antitumor Activity

Structural Optimization of Pyrazole Compounds as Hsp90 Regulators with Enhanced Antitumor Activity

Targeting Hsp90 is an effective strategy for cancer therapy. TAS-116 has been approved for the treatment of gastrointestinal stromal tumors. Our previous studies identified a series of pyrazole derivatives as covalent Hsp90 inhibitors that allosterically disrupt the Hsp90-Cdc37 interaction. Here, th...

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Main Author: Zi-Wen Feng (14608411) (author)
Other Authors: Li Li (14993) (author), Shi-Duo Zhang (14608414) (author), Ying-Ji Wang (21228156) (author), Jia-Yue Pei (21228159) (author), Nan-Nan Chen (15198729) (author), Bei-Duo Wu (15198735) (author), Qiu-Ling Zheng (13119805) (author), Qi-Dong You (294415) (author), Xiao-Ke Guo (459015) (author), Xiao-Li Xu (404540) (author)
Published: 2025
Subjects:
Biochemistry
Medicine
Cell Biology
Pharmacology
Biotechnology
Sociology
Cancer
Chemical Sciences not elsewhere classified
Information Systems not elsewhere classified
previous studies identified
novel mechanistic approach
gastrointestinal stromal tumors
collective findings underscore
new covalent warhead
39 </ b
covalent hsp90 inhibitors
50 </ sub
covalent hsp90
50 μm
therapeutic promise
targeted disruption
pyrazole derivatives
pyrazole compounds
knockout counterparts
hsp90 regulators
effective strategy
cancer therapy
allosterically disrupt
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