2ayr
From Proteopedia
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| , resolution 1.900Å | |||||||
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| Ligands: | |||||||
| Gene: | ESR1, ESR, NR3A1 (Homo sapiens) | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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
Page seeded by OCA on Thu Mar 20 15:55:31 2008
Categories: Homo sapiens | Single protein | Bryant, H U. | Cohen, I R. | Dally, R D. | Dodge, J A. | Fong, K C. | Frank, S A. | Geiser, A G. | Hinklin, R. | Hummel, C W. | Jones, S A. | Lewis, G. | McCann, D J. | Rudman, D G. | Shepherd, T A. | Tian, H. | Wallace, O B. | Wang, Y. | L4G | Ligand-binding | Receptor | Serm | Transcription | Transcription regulation
