2ayr

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2ayr, resolution 1.900Å

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A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats

Contents

Overview

The design of a novel selective estrogen receptor modulator (SERM) for the, potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl), binds with high affinity to estrogen receptors alpha and beta (ERalpha and, ERbeta, respectively) and is a potent uterine antagonist with minimal, effects on the ovaries as determined by serum biomarkers and histologic, evaluation.

Disease

Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[133430], Breast cancer OMIM:[133430], Estrogen resistance OMIM:[133430], HDL response to hormone replacement, augmented OMIM:[133430], Migraine, susceptibility to OMIM:[133430], Myocardial infarction, susceptibility to OMIM:[133430]

About this Structure

2AYR is a Single protein structure of sequence from Homo sapiens with L4G as ligand. Full crystallographic information is available from OCA.

Reference

A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats., Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA, J Med Chem. 2005 Nov 3;48(22):6772-5. PMID:16250633

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