Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells
文献类型：期刊论文
| 作者 | Lin, Zhaohu1; Shen, Hong2; Huang, Jin1; Chen, Shuai2; Chen, Lili2 ; Chen, Jing2; Liu, Guixia1; Jiang, Hualiang1,2; Shen, Xu1,2
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| 刊名 | JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
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| 出版日期 | 2008-05 |
| 卷号 | 110期号:1-2页码:150-156 |
| 关键词 | estrogen receptor butyl 4-(butyryloxy)benzoate surface plasmon resonance selective agonist yeast two-hybrid system glucose transporter 4 (GLU74) |
| ISSN号 | 0960-0760 |
| DOI | 10.1016/j.jsbmb.2008.03.028 |
| 文献子类 | Article |
| 英文摘要 | Estrogen receptors (ERs) belong to nuclear hormone receptor superfamily and can be activated by estrogens and regulate many target genes. Two ER isoforms, ER alpha and ER beta have been discovered to date and ER beta was indicated to involve in anti-inflammatory and anti-diabetogenic effects. Recently, some studies also demonstrated an association between ER beta and GLUT4 expression. The development of selective ER beta ligand has facilitated probing its novel biological functions and clinical benefits. In this work, a new ER beta selective agonist, butyl 4-(butyryloxy)benzoate (DCW234), was discovered as investigated by surface plasmon resonance (SPR) technology, yeast two-hybrid and cell-based transcription-based assays. SPR results demonstrated that DCW234 has a higher binding affinity against ER beta over ER alpha and induces a strong and selective stimulation on ER beta/SRC1 interaction, which could be efficiently blocked by Tamoxifen. Meanwhile, the yeast two-hybrid technology-based assay indicated that DCW234 exhibits a higher agonistic activity (similar to 13-fold) in stimulating ER beta ligand-binding domain (LBD) interaction with SRC1 (EC50 = 2.5 mu M) than ER alpha-LBD/SRC1 interaction (EC50 = 32.7 mu M). The cell-based transcriptional assay further proved the potency and selectivity of DCW234. Moreover, DCW234 was found to be able to induce GLUT4 expression in CHO-K1 cell. The discovered DCW234 might be hopefully developed as a potential lead compound for further research. (c) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | BONE-MINERAL DENSITY ; POSTMENOPAUSAL WOMEN ; ER-BETA ; TRANSCRIPTIONAL ACTIVATION ; NUCLEAR RECEPTORS ; BREAST-CANCER ; HUMAN-DISEASE ; COACTIVATOR ; BINDING ; SUPERFAMILY |
| WOS研究方向 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000257409000018 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272932]  |
| 专题 | 药理学第三研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 生物技术药物研发中心（筹） 药物安全性评价中心 |
| 通讯作者 | Huang, Jin |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lin, Zhaohu,Shen, Hong,Huang, Jin,et al. Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,2008,110(1-2):150-156. |
| APA | Lin, Zhaohu.,Shen, Hong.,Huang, Jin.,Chen, Shuai.,Chen, Lili.,...&Shen, Xu.(2008).Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells.JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,110(1-2),150-156. |
| MLA | Lin, Zhaohu,et al."Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells".JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 110.1-2(2008):150-156. |
入库方式： OAI收割
来源：上海药物研究所
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