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Anna Wawruszak Jarogniew Luszczki Marta Halasa Estera Okon Sebastian Landor Cecilia Sahlgren Adolfo Rivero-Muller Andrzej Stepulak 《International journal of molecular sciences》2021,22(10)
Histone deacetylase inhibitors (HDIs) are promising anti-cancer agents that inhibit proliferation of many types of cancer cells including breast carcinoma (BC) cells. In the present study, we investigated the influence of the Notch1 activity level on the pharmacological interaction between cisplatin (CDDP) and two HDIs, valproic acid (VPA) and suberoylanilide hydroxamic acid (SAHA, vorinostat), in luminal-like BC cells. The type of drug–drug interaction between CDDP and HDIs was determined by isobolographic analysis. MCF7 cells were genetically modified to express differential levels of Notch1 activity. The cytotoxic effect of SAHA or VPA was higher on cells with decreased Notch1 activity and lower for cells with increased Notch1 activity than native BC cells. The isobolographic analysis demonstrated that combinations of CDDP with SAHA or VPA at a fixed ratio of 1:1 exerted additive or additive with tendency toward synergism interactions. Therefore, treatment of CDDP with HDIs could be used to optimize a combined therapy based on CDDP against Notch1-altered luminal BC. In conclusion, the combined therapy of HDIs and CDDP may be a promising therapeutic tool in the treatment of luminal-type BC with altered Notch1 activity. 相似文献
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Poya Kavianpour Madeleine C. M. Gemmell Dr. Jan U. Kahlert Prof. Louis M. Rendina 《Chembiochem : a European journal of chemical biology》2020,21(19):2786-2791
Histone deacetylase enzymes (HDACs) are responsible for the global silencing of tumour-suppressor genes. Treatment with a histone deacetylase inhibitor (HDACi) can reverse this process and restore normal cell function. Herein, we report a small series of boron-based (boronic acid, boronate ester and closo-1,2-carborane) HDAC2 inhibitors with IC50 values in the nanomolar range. The boronate ester 4 b was the most potent compound assessed in this study (IC50=40.6±1.5 nM), followed closely by the 1,2-closo-carborane (IC50=42.9±1.5 nM). Compound 4 b exceeds the potency of the related gold-standard HDAC pan-inhibitor vorinostat ( 1 ) toward this particular HDAC isoform. 相似文献
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目的研究伏立诺他的4种杂质制备工艺。方法制备伏立诺他中的4种工艺、降解杂质,进行了1H-NMR,,13C-NMR结构确证。结果 4种工艺、降解杂质的结构确证数据证明其结构与数据相符。结论伏立诺他4种工艺、降解杂质的合成工艺稳定、成熟。 相似文献
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