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Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity
Liu, Jiangyuan2; Zhang, Xiaoyi1; Zhao, Ming1; Peng, Shiqi1,2
关键词Estradiol Rgd Octapeptide Conjugate Anti-osteoporosis 3d Qsar
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2009-04-01
DOI10.1016/j.ejmech.2008.09.036
44期:4页:1689-1704
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
资助者National Natural Scientific Foundation of China ; Beijing Municipal Commission of Education ; National Natural Scientific Foundation of China ; Beijing Municipal Commission of Education
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]HORMONE REPLACEMENT THERAPY ; BONE LOSS ; LINKERS ; OSTEOCLASTS ; ADHESION ; DISEASE
英文摘要

To enhance the potency, reduce the side effects and improve oral property of estradiol in estrogen replacement therapy (ERT), 6 novel estradiol-RGD octapeptide conjugates have been prepared. In an ovariectomized mouse osteoporotic model, at an oral dosage of 110.3 nmol/kg per day, their anti-osteoporosis activity was significantly higher than that of estradiol and estradiol-RCD tetrapeptide conjugates, and their risks of thrombogenesis and endometrial hyperplasia were significantly lower than that of estradiol and estradiol-RGD tetrapeptide conjugates. Using QSAR module of Cerius2, the 3D QSAR was performed for both femur weights and femur ash weights of estradiol-RGD peptide conjugates receiving mice. The r(2) of the 3D QSAR equations up to 0.995 and 0.988 indicates that they are capable of predicting a comparatively exact anti-osteoporosis activity for a conjugate. (c) 2008 Elsevier Masson SAS. All rights reserved.

语种英语
所属项目编号30572235 ; KZ 200810025010
资助者National Natural Scientific Foundation of China ; Beijing Municipal Commission of Education ; National Natural Scientific Foundation of China ; Beijing Municipal Commission of Education
WOS记录号WOS:000264920000035
Citation statistics
Cited Times:5[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/55134
Collection北京大学药学院
作者单位1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
2.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
Recommended Citation
GB/T 7714
Liu, Jiangyuan,Zhang, Xiaoyi,Zhao, Ming,et al. Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2009,44(4):1689-1704.
APA Liu, Jiangyuan,Zhang, Xiaoyi,Zhao, Ming,&Peng, Shiqi.(2009).Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,44(4),1689-1704.
MLA Liu, Jiangyuan,et al."Synthesis, evaluation and 3D QSAR analysis of novel estradiol-RGD octapeptide conjugates with oral anti-osteoporosis activity".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 44.4(2009):1689-1704.
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