4-Hydroxyphenylretinamide (4HPR) derivatives regulate aromatase activity and expression in breast cancer cells
4-Hydroxyphenylretinamide (4HPR) derivatives regulate aromatase activity and expression in breast cancer cells
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DOI：
10.1016/j.jsbmb.2007.12.005
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发表时间：
2008-03
期刊：
影响因子：
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通讯作者：
Bin Su;S. M. Mershon;Laura A. Stonerock;R. Curley;R. Brueggemeier
中科院分区：
文献类型：
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作者：
Bin Su;S. M. Mershon;Laura A. Stonerock;R. Curley;R. Brueggemeier
最近的研究表明，4-羟基苯基维A酰胺 (4HPR) 会降低乳腺和胎盘细胞中的芳香酶活性。在三种乳腺癌细胞系中检查了合成 4HPR 类似物对芳香酶及其表达的影响。大多数衍生物不会降低细胞芳香酶活性。其中两种类似物甚至在转录水平上刺激了芳香酶活性。只有一种衍生物显着降低所有三种乳腺癌细胞系中的芳香酶，并且还抑制其中一种细胞系中的 CYP19 基因表达。胎盘微粒体芳香酶测定排除了该化合物直接抑制芳香酶的可能性。提出了该化合物抑制细胞芳香酶活性的非基因组机制。
Recent studies exhibit that 4-hydroxyphenylretinamide (4HPR) decreases aromatase activity in breast and placental cells. The effect of synthetic 4HPR analogs on aromatase and expression was examined in three breast cancer cell lines. Most derivatives did not decrease cellular aromatase activity. Two of the analogs even stimulated aromatase activity at the transcriptional level. Only one derivative significantly decreased aromatase in all three breast cancer cell lines and also suppressed CYP19 gene expression in one of the cell line. Placental microsomal aromatase assay rule out the possibility that this compound directly inhibits the aromatase enzyme. A non-genomic mechanism in suppression of cellular aromatase activity of this compound is proposed.