Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, 524 Burrill Hall, 407 South Goodwin Avenue, Urbana, Illinois 61801-3704, USA.
Endocrinology. 2012 Aug;153(8):3982-94. doi: 10.1210/en.2012-1044. Epub 2012 May 14.
Although the effectiveness of nuclear hormone-receptor complexes is known to depend on coregulator partner proteins, relatively little is known about the roles of coregulators in uterine development and early stages of pregnancy and implantation. Because conventional genetic deletion of the coregulator, repressor of estrogen receptor activity (REA), was embryonic lethal, we here study REA conditional knockout mice generated by cre-loxP recombination, in which REA function was abrogated only in progesterone receptor-expressing tissues, to define the roles of REA in postembryonic stages and in a tissue-specific manner. We find that REA has gene dose-dependent activity impacting uterine development and fertility. Conditional homozygous mutant (REA(d/d)) mice developed to adulthood and showed normal ovarian function, but females were infertile with severely compromised uterine development and function characterized by cell cycle arrest, apoptosis, and altered adenogenesis (endometrial gland morphogenesis), resulting in failure of implantation and decidualization. By contrast, mice heterozygous for REA (REA(f/d)) had a very different phenotype, with estradiol treatment resulting in hyperstimulated, large uteri showing increased proliferation of luminal epithelial cells, and enhanced fluid imbibition associated with altered regulation of aquaporins. These REA(f/d) female mice showed a subfertility phenotype with reduced numbers and sizes of litters. These findings highlight that uterine development and regulation of estrogen receptor activities show a bimodal dependence on the gene dosage of REA. Optimal uterine development and functional activities require the normal gene dosage of REA, with partial or complete deletion resulting in hyperresponsiveness or underresponsiveness to hormone and subfertility or infertility, respectively.
尽管核激素受体复合物的有效性已知取决于共激活因子伴侣蛋白,但对于共激活因子在子宫发育和妊娠早期及着床阶段的作用,人们了解甚少。由于共激活因子抑制物,即雌激素受体活性抑制剂(REA)的常规基因缺失具有胚胎致死性,因此我们在此使用 CRE-loxP 重组技术生成的 REA 条件性敲除小鼠进行研究,在此技术中,REA 功能仅在孕激素受体表达组织中被阻断,以确定 REA 在胚胎后期及组织特异性条件下的作用。我们发现,REA 具有剂量依赖性的基因活性,可影响子宫发育和生育能力。条件性纯合突变(REA(d/d))小鼠发育至成年期,表现出正常的卵巢功能,但雌性小鼠不育,子宫发育和功能严重受损,表现为细胞周期停滞、细胞凋亡和腺发生改变(子宫内膜腺形态发生),导致着床和蜕膜化失败。相比之下,REA 杂合子(REA(f/d))小鼠具有非常不同的表型,雌二醇处理导致子宫过度刺激,形成大子宫,表现为腔上皮细胞增殖增加,以及与水通道蛋白调节改变相关的增强的液体吸收。这些 REA(f/d)雌性小鼠表现出亚生育表型,产仔数量和大小减少。这些发现强调了子宫发育和雌激素受体活性的调节对 REA 基因剂量具有双峰依赖性。最佳的子宫发育和功能活动需要 REA 的正常基因剂量,部分或完全缺失分别导致对激素的超敏反应或低反应,以及生育力降低或不育。