A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats

Conrad W.Hummel; Andrew G.Geiser; Henry U.Bryant; Ilene R.Cohen; Robert D.Dally

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A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats

机译：一种选择性雌激素受体调节剂，设计用于治疗大鼠子宫和卵巢具有独特组织特异性的子宫平滑肌瘤

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The design of a novel selective estrogen receptor modulator(SERM)for the potential treatment of uterine leiomyoma is described.16(LY2066948-HCl)binds with high affinity to estrogen receptors a and beta(ERalpha and ERbeta,respectively)and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers and histologic evaluation.

机译：描述了一种潜在治疗子宫肌瘤的新型选择性雌激素受体调节剂（SERM）的设计。16（LY2066948-HCl）与雌激素受体α和β（分别为ERα和ERβ）具有高亲和力，是一种有效的子宫通过血清生物标志物和组织学评估确定，该拮抗剂对卵巢的影响最小。

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《Journal of Medicinal Chemistry》 |2005年第22期|共4页
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Conrad W.Hummel; Andrew G.Geiser; Henry U.Bryant; Ilene R.Cohen; Robert D.Dally;
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1. A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats [J] . Conrad W.Hummel, Andrew G.Geiser, Henry U.Bryant, Journal of Medicinal Chemistry . 2005,第22期

机译：一种选择性雌激素受体调节剂，设计用于治疗大鼠子宫和卵巢具有独特组织特异性的子宫平滑肌瘤
2. Estrogen-induced stromal cell-derived factor-1 (SDF-1/Cxcl12) expression is repressed by progesterone and by Selective Estrogen Receptor Modulators via estrogen receptor alpha in rat uterine cells and tissues. [J] . Glace L, Grygielko ET, Boyle Steroids: An International Journal . 2009,第13a14期

机译：雌激素诱导的基质细胞衍生因子-1（SDF-1 / Cxcl12）的表达被孕酮和选择性雌激素受体调节剂通过雌激素受体α抑制在大鼠子宫细胞和组织中的表达。
3. Concentration-dependent effects of a selective estrogen receptor modulator raloxifene on proliferation and apoptosis in human uterine leiomyoma cells cultured in vitro. [J] . Liu J, Matsuo H, Xu Q, Human Reproduction . 2007,第5期

机译：选择性雌激素受体调节剂雷洛昔芬对体外培养的人子宫平滑肌瘤细胞增殖和凋亡的浓度依赖性作用。
4. Estrogen Receptors and Selective Estrogen Receptor Modulators in Bladder Cancer [C] . Kristi Hoffman, Carolyn L. Smith ^dgt, Baylor College of Medicine, Genitourinary Cancers Symposium . 2012

机译：膀胱癌中雌激素受体和选择性雌激素受体调节剂
5. The effects of the selective estrogen receptor modulators MPP and raloxifene in normal and cancerous human and murine uterine tissue. [D] . Davis, Angela Marie. 2007

机译：选择性雌激素受体调节剂MPP和雷洛昔芬在正常和癌变的人和鼠子宫组织中的作用。
6. Effects of SERM (selective estrogen receptor modulator) treatment on growth and proliferation in the rat uterus [O] . Denis Stygar, Natalia Muravitskaya, Britt Eriksson, 2003

机译：SERM（选择性雌激素受体调节剂）对大鼠子宫生长和增殖的影响
7. A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats [O] . -1

机译：一种选择性雌激素受体调节剂，专门用于治疗子宫平滑肌瘤，对大鼠子宫和卵巢的独特组织特异性

A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats

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