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Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates
Xiong, Yu; Zhao, Ming; Wang, Chao; Chang, Heng Wei; Peng, Shiqi
刊名JOURNAL OF MEDICINAL CHEMISTRY
2007-07-12
DOI10.1021/jm070242a
50期:14页:3340-3353
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]POSTMENOPAUSAL WOMEN ; LINKERS ; RISK ; OSTEOBLASTS ; OSTEOCLASTS ; ESTRADIOL ; BONE
英文摘要

To improve the specificity and potency of estrogen replacement therapy therapeutics while also minimizing the side effects such as bone resorption and thickening of the uterine wall, a series of novel estrogen-derived conjugates estradiol-3-RGD, estradiol-17-RGD, and estrone-3-RGD peptides have been prepared. In a mouse model, intraperitoneal (i.p.) administration of these estrogen-RGD peptide conjugates resulted in decreased serum concentrations of calcium and alkaline phosphatase, as well as increased levels of calcium, phosphorus, and minerals in the mouse femur. Furthermore, the anti-osteoporosis action of these conjugates followed a dose-dependent manner and was accompanied with no observable effects on endometrial cell hyperplasia. In addition to all of these compounds exhibiting biological activity when administered by the i.p. route, we were particularly pleased to note that the estradiol-3-RGD and estradiol-17-RGD conjugates were both orally active.

语种英语
WOS记录号WOS:000247760400021
引用统计
被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/61014
专题北京大学药学院
作者单位1.CS Bio Co, Menlo Pk, CA 94025 USA
2.Capitla Univ Med Sci, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
3.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
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GB/T 7714
Xiong, Yu,Zhao, Ming,Wang, Chao,et al. Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates[J]. JOURNAL OF MEDICINAL CHEMISTRY,2007,50(14):3340-3353.
APA Xiong, Yu,Zhao, Ming,Wang, Chao,Chang, Heng Wei,&Peng, Shiqi.(2007).Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates.JOURNAL OF MEDICINAL CHEMISTRY,50(14),3340-3353.
MLA Xiong, Yu,et al."Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates".JOURNAL OF MEDICINAL CHEMISTRY 50.14(2007):3340-3353.
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