Protein Information

Name glucocorticoid receptors
Synonyms GCCR; GCR; GR; GRL; Glucocorticoid receptor; NR3C1; Glucocorticoid receptors

Compound Information

Name vinclozolin
CAS 3-(3,5-dichlorophenyl)-5-ethenyl-5-methyl-2,4-oxazolidinedione

Reference List

PubMed Abstract RScore(About this table)
15483189 Sonneveld E, Jansen HJ, Riteco JA, Brouwer A, van der Burg B: Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. Toxicol Sci. 2005 Jan;83(1):136-48. Epub 2004 Oct 13.

Both bioassays are member of a panel of CALUX reporter cell lines derived from the human U2-OS osteosarcoma cell line, all using highly selective reporter constructs based with a basal promoter element linked to multimerized response elements, allowing efficient and specific measurement of compounds interfering with androgen, estrogen, progesterone, and glucocorticoid receptors.
Flutamide, cyproterone acetate, and the environmental contaminants vinclozolin, DDT, methoxychlor, its metabolite HPTE, and penta-BFR showed clear antagonistic activity in the AR CALUX bioassay, competitively inhibiting DHT-mediated transactivation.
1(0,0,0,1) Details
16621434 Kim HJ, Park YI, Dong MS: Comparison of prostate cancer cell lines for androgen receptor-mediated reporter gene assays. Toxicol In Vitro. 2006 Oct;20(7):1159-67. Epub 2006 Mar 8.

Both the mRNA and the proteins of AR and glucocorticoid receptor (GR) were expressed in all three cell lines.
The transcriptional activity induced with 10 (-8) M DHT was inhibited about 50-75% in the PC3/AR (+) and 22Rv1, and 98% in the LNCaP, by vinclozolin.
1(0,0,0,1) Details
12730620 Ma R, Cotton B, Lichtensteiger W, Schlumpf M: UV filters with antagonistic action at androgen receptors in the MDA-kb2 cell transcriptional-activation assay. Toxicol Sci. 2003 Jul;74(1):43-50. Epub 2003 May 2.

The fact that certain ultraviolet (UV) filters used in cosmetics display estrogenic activity prompted us to study potential actions on androgen receptors (AR) in the human breast carcinoma cell line MDA-kb2, which expresses functional endogenous AR and glucocorticoid receptors (GR) and is stably transfected with a luciferase reporter plasmid.
DHT-induced luciferase gene expression was inhibited by nonsteroidal antiandrogens, hydroxyflutamide, flutamide, bicalutamide, and vinclozolin.
1(0,0,0,1) Details