Molecular determinants of tissue selectivity in estrogen receptor modulators

Timothy A. Grese; James P. Sluka; Henry U. Bryant

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Molecular determinants of tissue selectivity in estrogen receptor modulators

机译：雌激素受体调节剂中组织选择性的分子决定因素

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Interaction of the estrogen receptor/ligand complex with a DNA estrogen response element is known to regulate gene transcription. In turn, specific conformations of the receptor-ligand complex have been postulated to influence unique subsets of estrogen-responsive genes resulting in differ- ential modulation and, ultimately, tissue-selective outcomes. The estrogen receptor ligands raloxifene and tamoxifen have dem- onstrated such tissue-specific estrogen agonist/antagonist ef- fects. Both agents antagonize the effects of estrogen on mammary tissue while mimicking the actions of estrogen on bone. However, tamoxifen induces significant stimulation of uterine tissue whereas raloxifene does not.

机译：已知雌激素受体/配体复合物与DNA雌激素反应元件的相互作用调节基因转录。反过来，已经假定受体-配体复合物的特定构象会影响雌激素反应性基因的独特子集，从而导致差异调节，最终导致组织选择性结果。雌激素受体配体雷洛昔芬和他莫昔芬已经证明了这种组织特异性雌激素激动剂/拮抗剂的作用。两种药剂都拮抗雌激素对乳腺组织的作用，同时模仿雌激素对骨骼的作用。然而，他莫昔芬诱导对子宫组织的显着刺激，而雷洛昔芬则不。

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《Proceedings of the National Academy of Sciences of the United States of America》 |1997年第25期|p.14105-14110|共6页
作者
Timothy A. Grese; James P. Sluka; Henry U. Bryant;
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收录信息美国《科学引文索引》(SCI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
原文格式 PDF
正文语种 eng
中图分类自然科学总论;
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1. Molecular Structural Characteristics of Estrogen Receptor Modulators as Determinants of Estrogen Receptor Selectivity [J] . S. Agatonovic-Kustrin J. V. Turner Mini-Reviews in Medicinal Chemistry . 2008,第9期

机译：雌激素受体调节剂的分子结构特征决定雌激素受体选择性
2. Molecular structural characteristics of estrogen receptor modulators as determinants of estrogen receptor selectivity. [J] . Agatonovic-Kustrin S, Turner JV Mini reviews in medicinal chemistry . 2008,第9期

机译：雌激素受体调节剂的分子结构特征决定了雌激素受体选择性。
3. Tissue-selective agents: selective estrogen receptor modulators and the tissue-selective estrogen complex. [J] . Pickar JH, Mirkin S Menopause international . 2010,第3期

机译：组织选择剂：选择性雌激素受体调节剂和组织选择性雌激素复合物。
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. Molecular determinants of tissue selectivity in estrogen receptor modulators [O] . Timothy A. Grese, James P. Sluka, Henry U. Bryant, 1997

机译：雌激素受体调节剂中组织选择性的分子决定因素
7. Estrogens, selective estrogen receptor modulators, and a selective estrogen receptor down-regulator inhibit endothelial production of tissue factor pathway inhibitor 1 [O] . Ree Anne, Birkenes Baard, Iversen Nina, 2006

机译：雌激素，选择性雌激素受体调节剂和选择性雌激素受体下调剂抑制组织因子途径抑制剂1的内皮生成
8. Definition of the Molecular Mechanisms Which Distinguish Between Selective Estrogen Receptor Modulators (SERMs) and Full Antiestrogens. [R] . Huang, H. 2005

机译：区分选择性雌激素受体调节剂（sERms）和完全抗雌激素的分子机制的定义。

Molecular determinants of tissue selectivity in estrogen receptor modulators

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