EMAIL THIS PAGE TO A FRIEND

Bioorganic & medicinal chemistry letters

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


PMID 19117754

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.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

D109606
2,6-Dihydroxybenzoic acid, 98%
C7H6O4