Bulun Serdar E, Utsunomiya Hiroki, Lin Zhihong, Yin Ping, Cheng You-Hong, Pavone Mary E, Tokunaga Hideki, Trukhacheva Elena, Attar Erkut, Gurates Bilgin, Milad Magdy P, Confino Edmond, Su Emily, Reierstad Scott, Xue Qing
Division of Reproductive Biology Research, Department of Obstetrics and Gynecology, Northwestern University Feinberg School of Medicine, 333 E. Superior Street, Suite 484, Chicago, IL 60611, United States.
Mol Cell Endocrinol. 2009 Mar 5;300(1-2):104-8. doi: 10.1016/j.mce.2008.12.012. Epub 2008 Dec 25.
Endometriosis is a common and chronic disease characterized by persistent pelvic pain and infertility. Estradiol is essential for growth and inflammation in endometriotic tissue. The complete cascade of steroidogenic proteins/enzymes including aromatase is present in endometriosis leading to de novo estradiol synthesis. PGE(2) induces the expression of the genes that encode these enzymes. Upon PGE(2) treatment, coordinate recruitment of the nuclear receptor SF-1 to the promoters of these steroidogenic genes is the key event for estradiol synthesis. SF-1 is the key factor determining that an endometriotic cell will respond to PGE(2) by increased estradiol formation. The presence of SF-1 in endometriosis and its absence in endometrium is determined primarily by the methylation of its promoter. The key steroidogenic enzyme in endometriosis is aromatase encoded by a single gene because its inhibition blocks all estradiol biosynthesis. Aromatase inhibitors diminish endometriotic implants and associated pain refractory to existing treatments in affected women.
子宫内膜异位症是一种常见的慢性疾病,其特征为持续性盆腔疼痛和不孕。雌二醇对于子宫内膜异位组织的生长和炎症至关重要。包括芳香化酶在内的完整类固醇生成蛋白/酶级联反应存在于子宫内膜异位症中,导致雌二醇的从头合成。前列腺素E2(PGE2)诱导编码这些酶的基因表达。在PGE2处理后,核受体SF-1协同募集到这些类固醇生成基因的启动子上是雌二醇合成的关键事件。SF-1是决定子宫内膜异位细胞是否会通过增加雌二醇生成来响应PGE2的关键因素。子宫内膜异位症中SF-1的存在及其在子宫内膜中的缺失主要由其启动子的甲基化决定。子宫内膜异位症中的关键类固醇生成酶是由单个基因编码芳烃酶,因为其抑制作用会阻断所有雌二醇的生物合成。芳香化酶抑制剂可减少受影响女性体内对现有治疗产生耐药性的子宫内膜异位植入物及相关疼痛。