Protein Information

Name progesterone receptor
Synonyms NR3C3; PGR; PR; Progesterone receptor; Progesterone receptors

Compound Information

Name endosulfan
CAS 6,7,8,9,10,10-hexachloro-1,5,5a,6,9,9a-hexahydro-6,9-methano-2,4,3-benzodioxathiepin 3-oxide

Reference List

PubMed Abstract RScore(About this table)
10397250 Hunter DS, Hodges LC, Vonier PM, Fuchs-Young R, Gottardis MM, Walker CL: Estrogen receptor activation via activation function 2 predicts agonism of xenoestrogens in normal and neoplastic cells of the uterine myometrium. Cancer Res. 1999 Jul 1;59(13):3090-9.

Diethylstilbestrol, coumestrol, genistein, naringenin, and endosulfan were able to activate the AF2 function of the ER in vitro and demonstrated agonist activity in estrogen-responsive myometrial cells, as determined by induction of proliferation and increased message levels of progesterone receptor.
81(1,1,1,1) Details
9118873 Vonier PM, Crain DA, McLachlan JA, Guillette LJ Jr, Arnold SF: Interaction of environmental chemicals with the estrogen and progesterone receptors from the oviduct of the American alligator. Environ Health Perspect. 1996 Dec;104(12):1318-22.

Modern-use chemicals such as alachlor, trans-nonachlor, endosulfan, and atrazine also competed with [3H] 17 beta-estradiol for binding to the aER.
2(0,0,0,2) Details
14579009 Scippo ML, Argiris C, Van De Weerdt C, Muller M, Willemsen P, Martial J, Maghuin-Rogister G: Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors. Anal Bioanal Chem. 2004 Feb;378(3):664-9. Epub 2003 Oct 25.

Except for phytoestrogens, most of the tested chemicals (DDT and its metabolites, aldrin, alpha- and beta-endosulfan, toxaphen, trans-nonachlor) show higher affinities for hPR than for hERalpha, indicating that the interaction with the progesterone receptor could contribute to the endocrine-disrupting effects imputed to these chemicals.
82(1,1,1,2) Details
9144411 Jin L, Tran DQ, Ide CF, McLachlan JA, Arnold SF: Several synthetic chemicals inhibit progesterone receptor-mediated transactivation in yeast. Biochem Biophys Res Commun. 1997 Apr 7;233(1):139-46.

The other chemicals which decreased progesterone activity were endosulfan II, endosulfan sulfate, and lindane.
2(0,0,0,2) Details
18262749 Chatterjee S, Kumar V, Majumder CB, Roy P: Screening of some anti-progestin endocrine disruptors using a recombinant yeast based in vitro bioassay. Toxicol In Vitro. 2008 Apr;22(3):788-98. Epub 2007 Dec 25.

The present study was aimed to develop a sensitive, fast and user friendly progesterone receptor transactivation assay using recombinant yeast cells, Saccharomyces cerevisiae, modified to express human progesterone receptor (PR) and progesterone response element (PRE) driving the expression of green fluorescent protein.
About 7 different chemicals (mostly pesticides or their metabolites) like DDT and its metabolites, nonylphenol, endosulfan were screened in this assay system for their role in transactivation and they were all found to be anti-progestative and IC50 values within the range of 3-20 microM.
1(0,0,0,1) Details
8593856 Soto AM, Sonnenschein C, Chung KL, Fernandez MF, Olea N, Serrano FO: The E-SCREEN assay as a tool to identify estrogens: an update on estrogenic environmental pollutants. Environ Health Perspect. 1995 Oct;103 Suppl 7:113-22.

Among the compounds tested, several "new" estrogens were found; alkylphenols, phthalates, some PCB congeners and hydroxylated PCBs, and the insecticides dieldrin, endosulfan, and toxaphene were estrogenic by the E-SCREEN assay.
In addition, these compounds competed with estradiol for binding to the estrogen receptor and increased the levels of progesterone receptor and pS2 in MCF-7 cells, as expected from estrogen mimics.
1(0,0,0,1) Details
16242299 Wong PS, Matsumura F: Serum free BG-1 cell proliferation assay: a sensitive method for determining organochlorine pesticide estrogen receptor activation at the nanomolar range. Toxicol In Vitro. 2006 Apr;20(3):382-94. Epub 2005 Oct 19.

We observed concentration dependent ER mediated cell proliferation in BG-1 cells using heptachlor epoxide (HE), beta-hexachlorohexane (beta-HCH), and endosulfan (Endo).
In addition, we observed upregulation of the ERE-dependent proteins progesterone receptor and PS2.
1(0,0,0,1) Details
9075711 Ramamoorthy K, Wang F, Chen IC, Norris JD, McDonnell DP, Leonard LS, Gaido KW, Bocchinfuso WP, Korach KS, Safe S: Estrogenic activity of a dieldrin/toxaphene mixture in the mouse uterus, MCF-7 human breast cancer cells, and yeast-based estrogen receptor assays: no apparent synergism. Endocrinology. 1997 Apr;138(4):1520-7.

Treatment with 10 (-6)-10 (-4) M chlordane, dieldrin, toxaphene, or an equimolar mixture of dieldrin/toxaphene did not induce activity, whereas 10 (-4) M endosulfan caused a 2000-fold increase in beta-gal activity.
Treatment of the animals with 17beta-estradiol (E2) (0.0053 kg/day x3) resulted in a 3.1-, 4.8-, and 7.8-fold increase in uterine wet weight, peroxidase activity, and progesterone receptor binding, respectively.
1(0,0,0,1) Details
10774817 Hodges LC, Bergerson JS, Hunter DS, Walker CL: Estrogenic effects of organochlorine pesticides on uterine leiomyoma cells in vitro. Toxicol Sci. 2000 Apr;54(2):355-64.

In Eker rat leiomyoma-derived cells, HPTE, kepone, and the alpha isomer of endosulfan stimulated proliferation, an effect dampened by the antiestrogen ICI 182,780.
In addition, these compounds stimulated transcription of the vitellogenin estrogen-response element via the ER in a transcriptional reporter gene assay and induced the expression of an endogenous estrogen-responsive gene, the progesterone receptor (PR).
1(0,0,0,1) Details
18790044 Varayoud J, Monje L, Bernhardt T, Munoz-de-Toro M, Luque EH, Ramos JG: Endosulfan modulates estrogen-dependent genes like a non-uterotrophic dose of 17beta-estradiol. Reprod Toxicol. 2008 Oct;26(2):138-45. Epub 2008 Aug 23.

After 24h of treatment, the uteri were weighed (uterotrophic assay) and the luminal epithelial cell height (LECH) and progesterone receptor (PR), and estrogen receptor alpha (ERalpha) protein levels were measured.
1(0,0,0,1) Details