2AYR

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

2AYR の概要

• エントリーDOI: 10.2210/pdb2ayr/pdb
• 分子名称: Estrogen receptor, 6-(4-METHYLSULFONYL-PHENYL)-5-[4-(2-PIPERIDIN-1-YLETHOXY)PHENOXY]NAPHTHALEN-2-OL (3 entities in total)
• 機能のキーワード: receptor, transcription, transcription regulation, ligand-binding, serm
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 28814.81

構造登録者

Hummel, C.W.,Geiser, A.G.,Bryant, H.U.,Cohen, I.R.,Dally, R.D.,Fong, K.C.,Frank, S.A.,Hinklin, R.,Jones, S.A.,Lewis, G.,McCann, D.J.,Shepherd, T.A.,Tian, H.,Rudman, D.G.,Wallace, O.B.,Wang, Y.,Dodge, J.A. (登録日: 2005-09-07, 公開日: 2005-11-22, 最終更新日: 2023-08-23)

主引用文献

Hummel, C.W.,Geiser, A.G.,Bryant, H.U.,Cohen, I.R.,Dally, R.D.,Fong, K.C.,Frank, S.A.,Hinklin, R.,Jones, S.A.,Lewis, G.,McCann, D.J.,Rudman, D.G.,Shepherd, T.A.,Tian, H.,Wallace, O.B.,Wang, Y.,Dodge, J.A.
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats
J.Med.Chem., 48:6772-6775, 2005

PubMed Abstract: 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.

PubMed: 16250633
DOI: 10.1021/jm050723z

実験手法

X-RAY DIFFRACTION (1.9 Å)