C-7 Progesterone Analogues and MDR1 in Breast Cancer

机译：C-7孕酮类似物和mDR1在乳腺癌中的应用

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We have generated novel analogs of progesterone (PgA) as potent inhibitors of the MDR1 multidrug resistant phenotype in breast cancer. The objectives of this Research Project include the optimization of the PgA's MDR1- reversing activity through the generation of additional compounds, using an analog design approach, the definition of these compounds' in vivo efficacy, and of their mechanism of action. In the course of the fourth year of the Project, we have: (1) tested the in vivo MDR-reversing activity of PgA4, the most potent among our initial progesterone analogs; (2) designed and synthesized additional progesterone analogs and evaluated their structure-activity relationships; (3) related the in vitro activity of some of the analogs to their in vitro toxicity.

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Clarke, R. R.;
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年度 2001
页码 1-151
总页数 151
原文格式 PDF
正文语种 eng
中图分类工业技术;
关键词
Inhibitors; Drugs; In vivo analysis; Progesterone; Breast cancer; Optimization; Toxicity; Glycoproteins; In vitro analysis; Chemical bonds; Analogs; Accumulation; Assaying; Potency; Chromatography; Mammary glands; Resistance(Biology);

机译：抑制剂;药物;体内分析;孕酮;乳腺癌;优化;毒性;糖蛋白;体外分析;化学键;类似物;积累;测定;效力;色谱;乳腺;抗性（生物学）;

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1. C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. [J] . Leonessa Fabio, Kim JiHyun, Ghiorghis Alem, Journal of Medicinal Chemistry . 2002,第2期

机译：孕酮的C-7类似物作为P-糖蛋白外排泵的有效抑制剂。
2. NANOLIPOPARTICLES-MEDIATED MDR1 SIRNA DELIVERY REDUCES DOXORUBICIN RESISTANCE IN BREAST CANCER CELLS AND SILENCES MDR1 EXPRESSION IN XENOGRAFT MODEL OF HUMAN BREAST CANCER [J] . NOURBAKHSH MAHNAZ, JAAFARI MAHMOUD REZA, LAGE HERMANN, Iranian Journal of Basic Medical Sciences . 2015,第4期

机译：纳米寡核苷酸介导的MDR1 SIRNA递减降低阿霉素在乳腺癌细胞中的耐药性，并使MDR1在人乳腺癌异种移植模型中的表达沉默
3. Prognostic Significance of Single Progesterone Receptor Positivity A Comparison Study of Estrogen Receptor Negative/Progesterone Receptor Positive/Her2 Negative Primary Breast Cancer With Triple Negative Breast Cancer [J] . Fan Ying, Ding Xiaoyan, Xu Binghe, Medicine. . 2015,第46期

机译：单孕酮受体积极性的预后意义对雌激素受体负/黄体酮受体阳性/ HER2阴性原发性乳腺癌的比较研究，三重阴性乳腺癌
4. Stilbene analogues as inhibitors of breast cancer Stem cells through P-glycoprotein efflux; A 3D quantitative structure-activity relationship study (Inhibitory activity of stilbenes analogues on breast cancer stem cells) [C] . Anushree Tripathi, Krishna Misra 2016 International Conference on Bioinformatics and Systems Biology . 2016

机译：Stilbene类似物通过P-糖蛋白外排作为乳腺癌干细胞的抑制剂； 3D定量结构-活性关系研究（Stilbenes类似物对乳腺癌干细胞的抑制活性）
5. Progesterone-only oral contraceptive pill, breast cancer, heart disease, and stroke. [D] . Samson, Marsha Ema. 2016

机译：仅黄体酮口服避孕药，乳腺癌，心脏病和中风。
6. Nanolipoparticles-mediated MDR1 siRNA delivery reduces doxorubicin resistance in breast cancer cells and silences MDR1 expression in xenograft model of human breast cancer [O] . Mahnaz Nourbakhsh, Mahmoud Reza Jaafari, Hermann Lage, 2015

机译：纳米脂质体介导的MDR1 siRNA传递降低乳腺癌细胞对阿霉素的抗性并沉默人乳腺癌异种移植模型中MDR1的表达
7. The role of oestrogen and progesterone receptors in breast cancer – immunohistochemical evaluation of oestrogen and progesterone receptor expression in invasive breast cancer in women [O] . Anna M. Badowska-Kozakiewicz, Janusz Patera, Maria Sobol, 2015

机译：雌激素和孕酮受体在乳腺癌中的作用 - 雌激素和孕酮受体表达在女性侵袭性乳腺癌中的免疫组化评价

C-7 Progesterone Analogues and MDR1 in Breast Cancer

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