| Literature DB >> 19117754 |
Jason R Neale1, Natali B Richter, Kevyn E Merten, K Grant Taylor, Sujan Singh, Leonard C Waite, Nicole K Emery, Ned B Smith, Jian Cai, William M Pierce.
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 (BTE(2)-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE(2)-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety profile of estradiol in the treatment of osteoporosis.Entities:
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Year: 2008 PMID： 19117754 DOI： 10.1016/j.bmcl.2008.12.051
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823