| Name | androgen receptor |
|---|---|
| Synonyms | AIS; AR; Androgen receptor; DHTR; Dihydrotestosterone receptor; HUMARA; KD; NR3C4… |
| Name | methoxychlor |
|---|---|
| CAS | 1,1′-(2,2,2-trichloroethylidene)bis[4-methoxybenzene] |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15589981 | Charles GD, Kan HL, Schisler MR, Bhaskar Gollapudi B, Sue Marty M: A comparison of in vitro and in vivo EDSTAC test battery results for detecting antiandrogenic activity. Toxicol Appl Pharmacol. 2005 Jan 1;202(1):108-20. The androgen receptor (AR) transactivation, binding, and Hershberger assays are being developed for large-scale screening of chemicals for endocrine activity. The goal of this study was to evaluate the correlation between in vitro and in vivo antiandrogenicity assays using a variety of compounds (p,p'-DDE, flutamide (FLUT), spironolactone, procymidone, RU486, methoxychlor (MXC), benzo (a) pyrene (BAP), and selected metabolites). |
1(0,0,0,1) | Details |
| 15253041 | Okubo T, Yokoyama Y, Kano K, Soya Y, Kano I: Estimation of estrogenic and antiestrogenic activities of selected pesticides by MCF-7 cell proliferation assay. Arch Environ Contam Toxicol. 2004 May;46(4):445-53. Among them, chlordecone, dicofol, methoxychlor, gamma-HCH, fenarimol, EPN, triadimefon, and triadimenol had estrogenic activities, all of which were suppressed by the addition of pure antiestrogen ICI 182,780. Affinities of the compounds for ERalpha and/or androgen receptor (AR) were lower than those of synthetic (diethylstilbestrol) and (mibolerone), respectively. |
1(0,0,0,1) | Details |
| 16199348 | Murono EP, Derk RC: The reported active metabolite of methoxychlor, 2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane, inhibits formation by cultured Leydig cells from neonatal rats. Reprod Toxicol. 2005 Nov-Dec;20(4):503-13. However, both MC and HPTE have been reported to have weak estrogenic and antiandrogenic activities, and they are thought to exert their potential adverse (endocrine disruptive) effects through the and androgen receptors, respectively. |
1(0,0,0,1) | Details |
| 12052007 | Kunimatsu T, Yamada T, Ose K, Sunami O, Kamita Y, Okuno Y, Seki T, Nakatsuka I: Lack of (anti-) androgenic or estrogenic effects of three pyrethroids (esfenvalerate, fenvalerate, and permethrin) in the Hershberger and uterotrophic assays. Regul Toxicol Pharmacol. 2002 Apr;35(2 Pt 1):227-37. Reference controls consisting of ethynyl (0.03 mg/kg/day) and methoxychlor (125 mg/kg/day) both showed a significant effect in this assay protocol. In the present study, we evaluated the interaction of three pyrethroids (esfenvalerate, fenvalerate, and permethrin) with androgen receptor (AR)- and estrogen receptor (ER)-mediated mechanisms using in vivo short-term assays. |
1(0,0,0,1) | Details |
| 10999957 | Gaido KW, Maness SC, McDonnell DP, Dehal SS, Kupfer D, Safe S: Interaction of methoxychlor and related compounds with estrogen receptor alpha and beta, and androgen receptor: structure-activity studies. Mol Pharmacol. 2000 Oct;58(4):852-8. We previously demonstrated differential interactions of the methoxychlor metabolite 2,2-bis (p-hydroxyphenyl)-1,1, 1-trichloroethane (HPTE) with estrogen receptor alpha (ERalpha), ERbeta, and the androgen receptor (AR). |
112(1,2,2,2) | Details |
| 18065196 | Akgul Y, Derk RC, Meighan T, Rao KM, Murono EP: The methoxychlor metabolite, HPTE, directly inhibits the catalytic activity of side-chain cleavage (P450scc) in cultured rat ovarian cells. Reprod Toxicol. 2008 Jan;25(1):67-75. Epub 2007 Oct 25. Both methoxychlor and HPTE have weak estrogenic and antiandrogenic activities, and these effects are thought to be mediated through the and androgen receptors, respectively. |
82(1,1,1,2) | Details |
| 11861976 | You L, Casanova M, Bartolucci EJ, Fryczynski MW, Dorman DC, Everitt JI, Gaido KW, Ross SM, Heck Hd H: Combined effects of dietary phytoestrogen and synthetic endocrine-active compound on reproductive development in Sprague-Dawley rats: and methoxychlor. Toxicol Sci. 2002 Mar;66(1):91-104. To explore possible mechanisms for interaction between the two compounds on development, we performed estrogen receptor (ER)- and androgen receptor (AR)-based in vitro transcriptional activation assays using and the primary methoxychlor metabolite 2,2-bis-(p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE). |
81(1,1,1,1) | Details |
| 9705896 | Maness SC, McDonnell DP, Gaido KW: Inhibition of androgen receptor-dependent transcriptional activity by DDT isomers and methoxychlor in HepG2 human hepatoma cells. Toxicol Appl Pharmacol. 1998 Jul;151(1):135-42. |
67(0,2,2,7) | Details |
| 11390175 | Cupp AS, Skinner MK: Actions of the endocrine disruptor methoxychlor and its estrogenic metabolite on in vitro embryonic rat seminiferous cord formation and perinatal testis growth. Reprod Toxicol. 2001 May-Jun;15(3):317-26. Androgen receptor (AR) expression was present from E14 through P5 of testis development, but at apparently reduced levels at E14 and E16. |
2(0,0,0,2) | Details |
| 11861975 | Hartig PC, Bobseine KL, Britt BH, Cardon MC, Lambright CR, Wilson VS, Gray LE Jr: Development of two androgen receptor assays using adenoviral transduction of MMTV-luc reporter and/or hAR for endocrine screening. Toxicol Sci. 2002 Mar;66(1):82-90. Luc gene expression was induced in a dose-dependent manner by DHT, and dexamethasone (MDA only) and inhibited by AR antagonist hydroxyflutamide (OHF), -DDE, HPTE (2,2-bis (p-hydroxyphenyl)-1,1, 1-trichloroethane), a methoxychlor metabolite, and M1 and M2 (vinclozolin metabolites). |
2(0,0,0,2) | Details |
| 15483189 | Sonneveld E, Jansen HJ, Riteco JA, Brouwer A, van der Burg B: Development of androgen- and -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. We have established highly sensitive and specific androgen and reporter cell lines which we have named AR (androgen receptor) and ERalpha (estrogen receptor alpha) CALUX (Chemically Activated LUciferase eXpression), respectively. 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. |
2(0,0,0,2) | Details |
| 9171990 | Danzo BJ: Environmental xenobiotics may disrupt normal endocrine function by interfering with the binding of physiological ligands to steroid receptors and binding proteins. Environ Health Perspect. 1997 Mar;105(3):294-301. The gamma- and delta-isomers of hexachlorocyclohexane, congeners of dichlorodiphenyl-trichloroethane (DDT; p,p'-DDT; p,p'-DDE; o,p'-DDT), dieldrin, atrazine, and pentachlorophenol, caused a statistically significant inhibition of specific binding of [3H] 5 alpha-DHT to the androgen receptor that ranged from 100% (p,p'-DDE) to 25% (dieldrin). Methoxychlor, o,p'-DDT1, pentachlorophenol, and nonylphenol significantly reduced [3H] 17 beta- binding to the estrogen receptor by 10, 60, 20, and 75%, respectively. |
1(0,0,0,1) | Details |
| 11509743 | Waters KM, Safe S, Gaido KW: Differential gene expression in response to methoxychlor and through ERalpha, ERbeta, and AR in reproductive tissues of female mice. Toxicol Sci. 2001 Sep;63(1):47-56. The MXC metabolite 2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane (HPTE) was previously shown to have selective agonist activity through estrogen receptor alpha (ERalpha) and antagonist activity through ERbeta and androgen receptor (AR). |
1(0,0,0,1) | Details |
| 15336722 | Murono EP, Derk RC: The effects of the reported active metabolite of methoxychlor, 2,2-bis (p-hydroxyphenyl)-1,1,1-trichloroethane, on formation by cultured Leydig cells from young adult rats. Reprod Toxicol. 2004 Nov;19(1):135-46. Both MC and HPTE have been demonstrated to exhibit weak estrogenic and antiandrogenic activities, and they are thought to exert their effects through or androgen receptors, respectively. |
2(0,0,0,2) | Details |
| 9073609 | Gaido KW, Leonard LS, Lovell S, Gould JC, Babai D, Portier CJ, McDonnell DP: Evaluation of chemicals with endocrine modulating activity in a yeast-based steroid hormone receptor gene transcription assay. Toxicol Appl Pharmacol. 1997 Mar;143(1):205-12. Methoxychlor, DDT and its metabolites, o,p'-DDD, and o,p'-DDE ranged in potency from 5 to 24 X 10 (6) less potent than and were most potent in the androgen receptor assay, followed by and p,p'-DDE was approximately 10 (6)-fold less potent than |
1(0,0,0,1) | Details |
| 16226009 | Murono EP, Derk RC, Akgul Y: In vivo exposure of young adult male rats to methoxychlor reduces serum levels and ex vivo Leydig cell formation and side-chain cleavage activity. Reprod Toxicol. 2006 Feb;21(2):148-53. Epub 2005 Oct 12. Both MC and HPTE have been shown to exhibit weak estrogenic and antiandrogenic activities, and they are thought to exert their effects through and androgen receptors, respectively. |
1(0,0,0,1) | Details |
| 16111029 | Zhao HT, Zhu JB, Zhu YF, Wang Z, Ma X, Zhang T: [Establishment of reporter gene-based assays for the identification of (anti) androgenic effects of chemicals in CHO cells]. Wei Sheng Yan Jiu. 2005 May;34(3):281-4. OBJECTIVE: Develop reporter gene-based assays for the identification of (anti) androgenic effects of chemicals in CHO cells, explore the antiandrogenic effects of 2,4-DDT and methoxychlor. METHODS: Chinese Ovary cells were cotransfected with the human androgen receptor expression vector, mouse mammary tumour virus MMTV-luciferase vector and phRL-SV40 using the transfection reagent test the luciferase activity. |
1(0,0,0,1) | Details |