Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells

doi:10.1016/j.jsbmb.2008.03.028

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	Butyl 4-(butyryloxy)benzoate functions as a new selective estrogen receptor beta agonist and induces GLUT4 expression in CHO-K1 cells
	Lin, Zhaohu 1; Shen, Hong 2; Huang, Jin 1; Chen, Shuai 2; Chen, Lili2 ; Chen, Jing2 ; Liu, Guixia 1; Jiang, Hualiang1,2 ; Shen, Xu1,2
刊名	JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
	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
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000257409000018
内容类型	期刊论文
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.