肝脏X受体激动剂T0901317在人前列腺癌细胞中作为雄激素受体拮抗剂发挥作用。
The liver X receptor agonist T0901317 acts as androgen receptor antagonist in human prostate cancer cells.
作者信息
Chuu Chih-Pin, Chen Rou-Yu, Hiipakka Richard A, Kokontis John M, Warner Karen V, Xiang Jialing, Liao Shutsung
机构信息
The Ben May Department for Cancer Research, The University of Chicago, CIS W325F, 929 E. 57th Street, Chicago, IL 60637, USA.
出版信息
Biochem Biophys Res Commun. 2007 Jun 1;357(2):341-6. doi: 10.1016/j.bbrc.2007.03.116. Epub 2007 Mar 28.
Abstract
T0901317 is a potent non-steroidal synthetic liver X receptor (LXR) agonist. T0901317 blocked androgenic stimulation of the proliferation of androgen-dependent LNCaP 104-S cells and androgenic suppression of the proliferation of androgen-independent LNCaP 104-R2 cells, inhibited the transcriptional activation of an androgen-dependent reporter gene by androgen, and suppressed gene and protein expression of prostate specific antigen (PSA), a target gene of androgen receptor (AR) without affecting gene and protein expression of AR. T0901317 also inhibited binding of a radiolabeled androgen to AR, but inhibition was much weaker compared to the effect of the antiandrogens, bicalutamide and hydroxyflutamide. The LXR agonist T0901317, therefore, acts as an antiandrogen in human prostate cancer cells.
摘要
T0901317是一种强效非甾体类合成肝X受体（LXR）激动剂。T0901317可阻断雄激素对雄激素依赖性LNCaP 104-S细胞增殖的刺激作用以及雄激素对雄激素非依赖性LNCaP 104-R2细胞增殖的抑制作用，抑制雄激素对雄激素依赖性报告基因的转录激活，并抑制雄激素受体（AR）的靶基因前列腺特异性抗原（PSA）的基因和蛋白表达，而不影响AR的基因和蛋白表达。T0901317还可抑制放射性标记雄激素与AR的结合，但与抗雄激素药物比卡鲁胺和羟基氟他胺相比，其抑制作用要弱得多。因此，LXR激动剂T0901317在人前列腺癌细胞中可作为一种抗雄激素发挥作用。
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本文引用的文献
1
Liver X receptor agonist T0901317 inhibition of glucocorticoid receptor expression in hepatocytes may contribute to the amelioration of diabetic syndrome in db/db mice.肝脏X受体激动剂T0901317对肝细胞中糖皮质激素受体表达的抑制作用可能有助于改善db/db小鼠的糖尿病综合征。
Endocrinology. 2006 Nov;147(11):5061-8. doi: 10.1210/en.2006-0243. Epub 2006 Jul 27.
2
Inhibition of tumor growth and progression of LNCaP prostate cancer cells in athymic mice by androgen and liver X receptor agonist.雄激素和肝脏X受体激动剂对无胸腺小鼠LNCaP前列腺癌细胞肿瘤生长和进展的抑制作用
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LXR activation reduces proinflammatory cytokine expression in human CD4-positive lymphocytes.肝X受体激活可降低人CD4阳性淋巴细胞中促炎细胞因子的表达。
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Role of androgen receptor in the progression of human prostate tumor cells to androgen independence and insensitivity.雄激素受体在人类前列腺肿瘤细胞向雄激素非依赖性和不敏感性进展中的作用。
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The liver X receptor ligand T0901317 decreases amyloid beta production in vitro and in a mouse model of Alzheimer's disease.肝脏X受体配体T0901317在体外和阿尔茨海默病小鼠模型中可降低β-淀粉样蛋白的产生。
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