Journal of Biological Chemistry · 2001 · 136 citations · 34 references
Life SciencesCell BiologyMolecular BiologyChromatin StructureNuclear OrganizationTranscriptional RegulationChromatinEuchromatin OrganizationFluorescence ImagingFluorescence MicroscopyHeterochromatin OrganizationHormone ReceptorsAndrogen ReceptorsGreen Fluorescent Protein ReportersHeterochromatin DistributionHeterochromatin LocalizationNuclear Hormone ReceptorsPoint Mutation EffectsReceptor-ligand SpecificitySubnuclear Localization
To establish the novel approach in order to distinguish the transcriptionally active androgen receptor (AR) from the transcriptionally inactive AR, we performed the three-dimensional construction of confocal microscopic images of intranuclear AR. This method clearly distinguished the subnuclear localization of transcriptionally active AR tagged with green fluorescent protein (AR-GFP) from the transcriptionally inactive AR-GFP. Transcriptionally active AR-GFP mainly produced 250-400 fluorescence foci in the boundary region between euchromatin and heterochromatin. Although the AR-GFP bound to such antiandrogens as hydroxyflutamide or bicalutamide translocated to the nucleus, they homogeneously spread throughout the nucleus without producing any fluorescence foci. Antiandrogenic environmental disrupting chemicals, such as 1,1-dichloro-2,2-bis(p-chlorophenyl)ethylene, vinclozolin, or nitrofen, also disrupted the intranuclear fluorescence foci. A point mutation (T877A) resulted in the loss of ligand specificity in AR-GFP. Even in this mutant receptor, agonists, such as dihydrotestosterone, hydroxyflutamide, or progesterone, produced the fluorescence foci in the nucleus, whereas the transcriptionally inactive mutant binding bicalutamide was observed to be spread homogeneously in the nucleus. Taken together, our findings suggest that, after nuclear translocation, AR is possibly located in the specific region in the nucleus while demonstrating clustering tightly depending on the agonist-induced transactivation competence.
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LNCaP model of human prostatic carcinoma.
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Medicine, Cancer Biology, Oncology +15
Persistent DDT metabolite p,p'–DDE is a potent androgen receptor antagonist
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Jos Veldscholte, C. Ris-Stalpers, George G. J. M. Kuiper et al. · Biochemical and Biophysical Research Communications · 1990 · 945 citations · Full text
Several environmental oestrogens are also anti-androgens
Pamela Sohoni, J. P. Sumpter · Journal of Endocrinology · 1998 · 853 citations
Medicine, Endocrinology, Toxicology +11