2AYR
A SERM Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats
Summary for 2AYR
| Entry DOI | 10.2210/pdb2ayr/pdb |
| Descriptor | Estrogen receptor, 6-(4-METHYLSULFONYL-PHENYL)-5-[4-(2-PIPERIDIN-1-YLETHOXY)PHENOXY]NAPHTHALEN-2-OL (3 entities in total) |
| Functional Keywords | receptor, transcription, transcription regulation, ligand-binding, serm |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 1 |
| Total formula weight | 28814.81 |
| Authors | 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. (deposition date: 2005-09-07, release date: 2005-11-22, Last modification date: 2023-08-23) |
| Primary citation | 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 Cited by 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: 16250633DOI: 10.1021/jm050723z PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.9 Å) |
Structure validation
Download full validation report
