Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent

JR Neale, NB Richter, KE Merten, KG Taylor…

Index: Neale, Jason R.; Richter, Natali B.; Merten, Kevyn E.; Grant Taylor; Singh, Sujan; Waite, Leonard C.; Emery, Nicole K.; Smith, Ned B.; Cai, Jian; Pierce Jr., William M. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 680 - 683

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Citation Number: 30

Abstract

In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the ...