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- W4319066095 abstract "Heat shock protein 110 (HSP110) is an emerging biological target for development of drug to treat colorectal cancer. In the present study, we designed and synthesized a series of novel small-molecule inhibitors of HSP110 based on previously reported HSP110 modulator (hit 1). Among the novel compounds, molecule 7 exhibited the most improved biological activity in vitro and anticancer efficacy in vivo. It exerted greater anti-proliferative potency against several colorectal cancer cells including HCT116 and SW480 with IC50 values of 11.59 μM and 6.05 μM, respectively. Molecular docking experiment of 7 with HSP110 protein revealed it bound well with the target in the similar way as compound 1. Mechanistic studies revealed that 7 effectively inhibited STAT3 activity and the expression of STAT3 downstream genes, VEGF, MMP7, MMP9. Moreover, 7 significantly abolished IL-6-induced epithelial-mesenchymal transition (EMT) in HCT116 and SW480 cells. Finally, 7 exhibited stronger tumor growth inhibition than lead compound 1 at the dose of 5 mg/kg (i.p.) in an in vivo HCT116 cells xenografted nude mice model. Taken together, we identified 7 as 2nd generation of HSP110 inhibitor which exerts remarkable anti-colorectal cancer activities. This compound might serve as a new lead for developing anti-cancer drugs to treat colorectal cancer." @default.
- W4319066095 created "2023-02-04" @default.
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- W4319066095 date "2023-04-01" @default.
- W4319066095 modified "2023-09-30" @default.
- W4319066095 title "Discovery of second generation heat shock protein 110 (HSP110) inhibitors for potential treatment of colorectal cancer" @default.
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- W4319066095 doi "https://doi.org/10.1016/j.ejmcr.2023.100103" @default.
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