Chalcone-templated Hsp90 inhibitors and their effects on gefitinib resistance in non-small cell lung cancer (NSCLC)

Authors
Ju Hui JeongYong Jin OhTaeg Kyu KwonYoung Ho Seo
Department
Dept. of Immunology (면역학)
Issue Date
2017
Citation
Archives of Pharmacal Research, Vol.40(1) : 96-105, 2017
ISSN
0253-6269
Abstract
The molecular chaperone Hsp90 has emerged as an attractive cancer therapeutic target due to its role in cellular homeostasis by modulating the stabilization and maturation of many oncogenic proteins. In this study, we designed and synthesized a series of Hsp90 inhibitors that hybridized NVP-AUY992 (2) and PU3 (3) in the chalcone scaffold using a structure-based approach. Our results indicate that compound 1g inhibited the proliferation of gefitinib-resistant non-small cell lung cancer (H1975) cells, downregulated the expression of client proteins of Hsp90 including EGFR, MET, Her2 and Akt, and up-regulated the expression of Hsp70. The compound 1g represents a new class of Hsp90 inhibitors with a chalcone structure. The design, synthesis, and evaluation of 1g are described herein.
Keywords
Heat shock protein 90ChalconeCancerResistanceGefitinib
URI
http://kumel.medlib.dsmc.or.kr/handle/2015.oak/32725
Appears in Collections:
1. Journal Papers (연구논문) > 1. School of Medicine (의과대학) > Dept. of Immunology (면역학)
Keimyung Author(s)
권택규
Full Text
https://link.springer.com/article/10.1007%2Fs12272-016-0848-z
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