Drew Brian G, Hamidi Habib, Zhou Zhenqi, Villanueva Claudio J, Krum Susan A, Calkin Anna C, Parks Brian W, Ribas Vicent, Kalajian Nareg Y, Phun Jennifer, Daraei Pedram, Christofk Heather R, Hewitt Sylvia C, Korach Kenneth S, Tontonoz Peter, Lusis Aldons J, Slamon Dennis J, Hurvitz Sara A, Hevener Andrea L
From the David Geffen School of Medicine, Department of Medicine, Division of Endocrinology, Diabetes and Hypertension.
Division of Hematology-Oncology, and Jonsson Comprehensive Cancer Center, UCLA, Los Angeles, California 90095.
J Biol Chem. 2015 Feb 27;290(9):5566-81. doi: 10.1074/jbc.M114.606459. Epub 2014 Dec 2.
Obesity is associated with increased breast cancer (BrCA) incidence. Considering that inactivation of estrogen receptor (ER)α promotes obesity and metabolic dysfunction in women and female mice, understanding the mechanisms and tissue-specific sites of ERα action to combat metabolic-related disease, including BrCA, is of clinical importance. To study the role of ERα in adipose tissue we generated fat-specific ERα knock-out (FERKO) mice. Herein we show that ERα deletion increased adipocyte size, fat pad weight, and tissue expression and circulating levels of the secreted glycoprotein, lipocalin 2 (Lcn2), an adipokine previously associated with BrCA development. Chromatin immunoprecipitation and luciferase reporter studies showed that ERα binds the Lcn2 promoter to repress its expression. Because adipocytes constitute an important cell type of the breast microenvironment, we examined the impact of adipocyte ERα deletion on cancer cell behavior. Conditioned medium from ERα-null adipocytes and medium containing pure Lcn2 increased proliferation and migration of a subset of BrCA cells in culture. The proliferative and promigratory effects of ERα-deficient adipocyte-conditioned medium on BrCA cells was reversed by Lcn2 deletion. BrCA cell responsiveness to exogenous Lcn2 was heightened in cell types where endogenous Lcn2 expression was minimal, but components of the Lcn2 signaling pathway were enriched, i.e. SLC22A17 and 3-hydroxybutyrate dehydrogenase (BDH2). In breast tumor biopsies from women diagnosed with BrCA we found that BDH2 expression was positively associated with adiposity and circulating Lcn2 levels. Collectively these data suggest that reduction of ERα expression in adipose tissue promotes adiposity and is linked with the progression and severity of BrCA via increased adipocyte-specific Lcn2 production and enhanced tumor cell Lcn2 sensitivity.
肥胖与乳腺癌(BrCA)发病率增加有关。鉴于雌激素受体(ER)α失活会促进女性和雌性小鼠肥胖及代谢功能障碍,了解ERα对抗包括BrCA在内的代谢相关疾病的作用机制和组织特异性位点具有临床重要性。为研究ERα在脂肪组织中的作用,我们构建了脂肪特异性ERα敲除(FERKO)小鼠。在此我们表明,ERα缺失会增加脂肪细胞大小、脂肪垫重量以及分泌性糖蛋白lipocalin 2(Lcn2)的组织表达和循环水平,Lcn2是一种先前与BrCA发展相关的脂肪因子。染色质免疫沉淀和荧光素酶报告基因研究表明,ERα结合Lcn2启动子以抑制其表达。由于脂肪细胞是乳腺微环境的重要细胞类型,我们研究了脂肪细胞ERα缺失对癌细胞行为的影响。来自ERα缺失脂肪细胞的条件培养基以及含有纯Lcn2的培养基可增加培养的部分BrCA细胞的增殖和迁移。Lcn2缺失可逆转ERα缺陷脂肪细胞条件培养基对BrCA细胞的增殖和促迁移作用。在细胞内源性Lcn2表达极少但Lcn2信号通路成分丰富的细胞类型中,即溶质载体家族22成员17(SLC22A17)和3 - 羟基丁酸脱氢酶(BDH2),BrCA细胞对外源性Lcn2的反应性增强。在被诊断为BrCA的女性乳腺肿瘤活检中,我们发现BDH2表达与肥胖及循环Lcn2水平呈正相关。这些数据共同表明,脂肪组织中ERα表达降低会促进肥胖,并通过增加脂肪细胞特异性Lcn2产生和增强肿瘤细胞对Lcn2的敏感性与BrCA的进展和严重程度相关。