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靶向突变型雌激素受体。

Targeting mutant estrogen receptors.

机构信息

Department of Pharmacology and Cancer Biology, Duke University School of Medicine, Durham, United States.

出版信息

Elife. 2019 Jan 16;8:e44181. doi: 10.7554/eLife.44181.

DOI:10.7554/eLife.44181
PMID:30648967
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6335051/
Abstract

A drug used in hormone replacement therapy can target estrogen receptors that have become resistant to breast cancer treatments.

摘要

一种用于激素替代疗法的药物可以针对已经对乳腺癌治疗产生抗药性的雌激素受体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d34/6335051/8458cb0a93b9/elife-44181-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d34/6335051/8458cb0a93b9/elife-44181-fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d34/6335051/8458cb0a93b9/elife-44181-fig1.jpg

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1
Targeting mutant estrogen receptors.靶向突变型雌激素受体。
Elife. 2019 Jan 16;8:e44181. doi: 10.7554/eLife.44181.
2
The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.基于 SERM/SERD 的巴多昔芬破坏 ESR1 螺旋 12，以克服乳腺癌细胞获得性激素耐药性。
Elife. 2018 Nov 29;7:e37161. doi: 10.7554/eLife.37161.
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Selective estrogen modulators as an anticancer tool: mechanisms of efficiency and resistance.选择性雌激素调节剂作为一种抗癌工具：作用机制及耐药性
Adv Exp Med Biol. 2008;630:206-19. doi: 10.1007/978-0-387-78818-0_13.
4
Selective estrogen receptor modulators and the combination therapy conjugated estrogens/bazedoxifene: A review of effects on the breast.选择性雌激素受体调节剂及结合雌激素/巴多昔芬联合疗法：对乳腺影响的综述
Post Reprod Health. 2015 Sep;21(3):112-21. doi: 10.1177/2053369115599090. Epub 2015 Aug 19.
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[Hormone therapy and breast cancer].[激素疗法与乳腺癌]
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Selective estrogen receptor modulators. An aid in unraveling the links between estrogen and breast cancer.选择性雌激素受体调节剂。有助于揭示雌激素与乳腺癌之间的联系。
Postgrad Med. 2001 Mar;Spec No:3-10.
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Endocrine therapy resistance in breast cancer: current status, possible mechanisms and overcoming strategies.乳腺癌内分泌治疗耐药：现状、可能机制及克服策略
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Advantages of multiple clinical tests for determining the optimum treatment strategy for ER-positive breast cancer.多项临床试验对于确定雌激素受体阳性乳腺癌最佳治疗策略的优势。
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Endocrine resistance in breast cancer.乳腺癌中的内分泌耐药性。
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Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment.选择性雌激素受体调节剂（SERMs）和选择性雌激素受体降解剂（SERDs）在癌症治疗中的应用。
Pharmacol Ther. 2018 Jun;186:1-24. doi: 10.1016/j.pharmthera.2017.12.012. Epub 2017 Dec 28.

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Kv11.1-dependent senescence activates a lethal immune response via tumor necrosis factor alpha.依赖Kv11.1的衰老通过肿瘤坏死因子α激活致死性免疫反应。
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本文引用的文献

1
The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.基于 SERM/SERD 的巴多昔芬破坏 ESR1 螺旋 12，以克服乳腺癌细胞获得性激素耐药性。
Elife. 2018 Nov 29;7:e37161. doi: 10.7554/eLife.37161.
2
Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.雌激素受体α体细胞突变Y537S和D538G通过稳定激活功能-2结合构象赋予乳腺癌内分泌抗性。
Elife. 2016 Feb 2;5:e12792. doi: 10.7554/eLife.12792.
3
Efficacy of SERD/SERM Hybrid-CDK4/6 Inhibitor Combinations in Models of Endocrine Therapy-Resistant Breast Cancer.
单细胞免疫印迹法解析乳腺癌中的雌激素受体-α亚型。
PLoS One. 2021 Jul 27;16(7):e0254783. doi: 10.1371/journal.pone.0254783. eCollection 2021.
4
Melatonin as an Oncostatic Molecule Based on Its Anti-Aromatase Role in Breast Cancer.褪黑素作为一种基于其在乳腺癌中抗芳香化酶作用的抑瘤分子。
Int J Mol Sci. 2021 Jan 4;22(1):438. doi: 10.3390/ijms22010438.
5
miR-452 Reverses Abnormal Glycosylation Modification of ERα and Estrogen Resistance in TNBC (Triple-Negative Breast Cancer) Through Targeting UGT1A1.微小RNA-452通过靶向尿苷二磷酸葡萄糖醛酸基转移酶1A1逆转三阴性乳腺癌中雌激素受体α的异常糖基化修饰及雌激素抵抗
Front Oncol. 2020 Aug 26;10:1509. doi: 10.3389/fonc.2020.01509. eCollection 2020.
6
Discovery of novel natural compound inhibitors targeting estrogen receptor α by an integrated virtual screening strategy.通过整合虚拟筛选策略发现针对雌激素受体 α 的新型天然化合物抑制剂。
J Mol Model. 2019 Aug 28;25(9):278. doi: 10.1007/s00894-019-4156-7.
SERD/SERM 杂交 CDK4/6 抑制剂组合在内分泌治疗抵抗性乳腺癌模型中的疗效
Clin Cancer Res. 2015 Nov 15;21(22):5121-5130. doi: 10.1158/1078-0432.CCR-15-0360. Epub 2015 May 19.
4
Development of conjugated estrogens/bazedoxifene, the first tissue selective estrogen complex (TSEC) for management of menopausal hot flashes and postmenopausal bone loss.共轭雌激素/巴多昔芬的研发，这是首个用于治疗更年期潮热和绝经后骨质流失的组织选择性雌激素复合物（TSEC）。
Steroids. 2014 Nov;90:71-81. doi: 10.1016/j.steroids.2014.06.004. Epub 2014 Jun 11.
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ESR1 ligand-binding domain mutations in hormone-resistant breast cancer.激素抵抗型乳腺癌中的 ESR1 配体结合域突变。
Nat Genet. 2013 Dec;45(12):1439-45. doi: 10.1038/ng.2822. Epub 2013 Nov 3.
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Bazedoxifene exhibits antiestrogenic activity in animal models of tamoxifen-resistant breast cancer: implications for treatment of advanced disease.比卡鲁胺在他莫昔芬耐药乳腺癌动物模型中表现出抗雌激素活性：对晚期疾病治疗的影响。
Clin Cancer Res. 2013 May 1;19(9):2420-31. doi: 10.1158/1078-0432.CCR-12-3771. Epub 2013 Mar 27.
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Efficacy and safety of bazedoxifene for postmenopausal osteoporosis.巴泽多昔芬治疗绝经后骨质疏松症的疗效和安全性。
Clin Interv Aging. 2011;6:151-60. doi: 10.2147/CIA.S15711. Epub 2011 Jun 21.
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Conformational dynamics of the estrogen receptor alpha: molecular dynamics simulations of the influence of binding site structure on protein dynamics.雌激素受体α的构象动力学：结合位点结构对蛋白质动力学影响的分子动力学模拟
Biochemistry. 2007 Feb 20;46(7):1743-58. doi: 10.1021/bi061656t. Epub 2007 Jan 24.