タキタ　モリチカ   Morichika Takita   瀧田　守親    所属   医学部 医学科    職種   助教
論文種別	原著
言語種別	英語
査読の有無	査読あり
表題	A novel carborane analog, BE360, with a carbon-containing polyhedral boron-cluster is a new selective estrogen receptor modulator for bone.
掲載誌名	正式名：Biochemical and Biophysical Research Commmunications 略　 称：Biochem. Biophys. Res. Commn. ISSNコード：0006291X
掲載区分	国外
出版社	Elsevier
巻・号・頁	380,pp.218-222
著者・共著者	Hirata Michiko†, Inada Masaki, Matsumoto Chiho, Takita Morichika, Ogawa Takumi, Endo Yasuyuki, Miyaura Chisato*
発行年月	2009/01
概要	Carboranes are a class of carbon-containing polyhedral boron-cluster compounds with globular geometry and hydrophobic surface that interact with hormone receptors. Estrogen deficiency results in marked bone loss due to increased osteoclastic bone resorption in females, but estrogen replacement therapy is not generally used for postmenopausal osteoporosis due to the risk of uterine cancer. We synthesized a novel carborane compound BE360 to clarify its anti-osteoporosis activity. BE360 showed a high binding affinity to estrogen receptors (ER), ERalpha and ERbeta. In ovariectomized (OVX) mice, femoral bone volume was markedly reduced and BE360 dose-dependently restored bone loss in OVX mice. However, BE360 did not exhibit any estrogenic activity in the uterus. BE360 also restored bone loss in orchidectomized mice without androgenic action in the sex organs. Therefore, BE360 is a novel selective estrogen receptor modulator (SERM) that may offer a new therapy option for osteoporosis.
DOI	10.1016/j.bbrc.2009.01.033
PMID	19159615