In Vitro and in Vivo Molecular Imaging of Estrogen Receptor α and β Homo- and Heterodimerization: Exploration of New Modes of Receptor Regulation

• Published in: Molecular endocrinology (Baltimore, Md.) Vol. 25; no. 12; pp. 2029 - 2040
• Main Authors: Paulmurugan, Ramasamy, Tamrazi, Anobel, Massoud, Tarik F., Katzenellenbogen, John A., Gambhir, Sanjiv S.
• Format: Journal Article
• Language: English
• Published: United States Oxford University Press 01.12.2011; Endocrine Society
• Subjects: Animals; Estrogen Receptor alpha - agonists; Estrogen Receptor alpha - metabolism; Estrogen Receptor beta - agonists; Estrogen Receptor beta - metabolism; Female; Gene Expression Regulation; Genes, Reporter; HEK293 Cells; Humans; Luciferases, Firefly - biosynthesis; Luciferases, Firefly - genetics; Luciferases, Renilla - biosynthesis; Luciferases, Renilla - genetics; Mice; Mice, Nude; Molecular Imaging; Original Research; Piperidines - pharmacology; Protein Multimerization; Protein Stability; Protein Structure, Tertiary; Pyrazoles - pharmacology; Raloxifene Hydrochloride - pharmacology; Recombinant Fusion Proteins - metabolism; Selective Estrogen Receptor Modulators - pharmacology; Tamoxifen - analogs & derivatives; Tamoxifen - pharmacology; Transplantation, Heterologous; 17β-estradiol | Genistein | 4-Hydroxytamoxifen | Raloxifene | Estriol | Estrone | Diarylpropionitrile | Diethylstilbestrol; ER-α | ER-β

Abstract Estrogen receptor (ER) biology reflects the actions of estrogens through the two receptors, ERα and ERβ, although little is known regarding the preference for formation of ER homo- vs. heterodimers, and how this is affected by the level of ligand occupancy and preferential ligand affinity f...