| Name | androgen receptor |
|---|---|
| Synonyms | AIS; AR; Androgen receptor; DHTR; Dihydrotestosterone receptor; HUMARA; KD; NR3C4… |
| Name | linuron |
|---|---|
| CAS |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 8480329 | Cook JC, Mullin LS, Frame SR, Biegel LB: Investigation of a mechanism for Leydig cell tumorigenesis by linuron in rats. Toxicol Appl Pharmacol. 1993 Apr;119(2):195-204. In addition, competitive receptor binding studies were conducted to evaluate the ability of linuron to bind to the androgen receptor. |
168(2,2,3,3) | Details |
| 10435283 | Bauer ER, Meyer HH, Stahlschmidt-Allner P, Sauerwein H: Application of an androgen receptor assay for the characterisation of the androgenic or antiandrogenic activity of various phenylurea herbicides and their derivatives. Analyst. 1998 Dec;123(12):2485-7. The phenylurea herbicide linuron and its derivative 3,4-dichloroaniline (3,4-DCA), which are found in sediments and surface waters, are known to displace bound from the rat androgen receptor. |
85(1,1,1,5) | Details |
| 10964759 | McIntyre BS, Barlow NJ, Wallace DG, Maness SC, Gaido KW, Foster PM: Effects of in utero exposure to linuron on androgen-dependent reproductive development in the male Crl:CD (SD) BR rat. Toxicol Appl Pharmacol. 2000 Sep 1;167(2):87-99. Studies were undertaken to characterize the ability of linuron to activate transcription through the human androgen receptor (AR) in vitro and to determine whether in utero linuron exposure induces dose-responsive alterations in androgen-dependent reproductive development in the male rat. |
81(1,1,1,1) | Details |
| 17512650 | Dent MP: Strengths and limitations of using repeat-dose toxicity studies to predict effects on fertility. Regul Toxicol Pharmacol. 2007 Aug;48(3):241-58. Epub 2007 Apr 12. Three showed evidence of direct interaction with oestrogen or androgen receptors (linuron, nonylphenol, and fenarimol). |
81(1,1,1,1) | Details |
| 12730624 | Turner KJ, McIntyre BS, Phillips SL, Barlow NJ, Bowman CJ, Foster PM: Altered gene expression during rat Wolffian duct development in response to in utero exposure to the antiandrogen linuron. Toxicol Sci. 2003 Jul;74(1):114-28. Epub 2003 May 2. Linuron is an herbicide with weak androgen receptor (AR) antagonist activity. |
31(0,1,1,1) | Details |
| 11752686 | McIntyre BS, Barlow NJ, Foster PM: Male rats exposed to linuron in utero exhibit permanent changes in anogenital distance, nipple retention, and epididymal malformations that result in subsequent testicular atrophy. Toxicol Sci. 2002 Jan;65(1):62-70. Prenatal exposure to the herbicide linuron, a weak androgen receptor antagonist, has been shown to perturb androgen-dependent male rat reproductive development as evidenced by slight decreases in anogenital distance (AGD), increased retention of areolae/nipples, and induction of epididymal malformations in combination with testicular atrophy in the adult rat over dose levels ranging from 12.5 to 100 mg/kg/day. |
31(0,1,1,1) | Details |
| 15286035 | Hotchkiss AK, Parks-Saldutti LG, Ostby JS, Lambright C, Furr J, Vandenbergh JG, Gray LE Jr: A mixture of the "antiandrogens" linuron and butyl benzyl alters sexual differentiation of the male rat in a cumulative fashion. Biol Reprod. 2004 Dec;71(6):1852-61. Epub 2004 Jul 30. The objectives of this study were to 1) determine whether a documented antiandrogen butyl benzyl (BBP) and/or linuron (an androgen receptor antagonist) would decrease fetal (T) production, 2) describe reproductive developmental effects of linuron and BBP in the male, 3) examine the potential cumulative effects of linuron and BBP, and 4) investigate whether treatment-induced changes to neonatal anogenital distance (AGD) and juvenile areola number were predictive of adult reproductive alterations. |
31(0,1,1,1) | Details |
| 11955944 | McIntyre BS, Barlow NJ, Sar M, Wallace DG, Foster PM: Effects of in utero linuron exposure on rat Wolffian duct development. Reprod Toxicol. 2002 Mar-Apr;16(2):131-9. Linuron is an herbicide that displays weak androgen receptor antagonist activity. |
31(0,1,1,1) | Details |
| 12075120 | Turner KJ, Barlow NJ, Struve MF, Wallace DG, Gaido KW, Dorman DC, Foster PM: Effects of in utero exposure to the organophosphate insecticide fenitrothion on androgen-dependent reproductive development in the Crl:CD (SD) BR rat. Toxicol Sci. 2002 Jul;68(1):174-83. At the dose levels evaluated in this study, fenitrothion was only weakly antiandrogenic in vivo compared with other androgen receptor antagonists such as flutamide, linuron, and vinclozolin. |
31(0,1,1,1) | Details |
| 11222873 | Tamura H, Maness SC, Reischmann K, Dorman DC, Gray LE, Gaido KW: Androgen receptor antagonism by the organophosphate insecticide fenitrothion. Toxicol Sci. 2001 Mar;60(1):56-62. Our results demonstrate that fenitrothion is a competitive AR antagonist, comparable in potency to the pharmaceutical antiandrogen flutamide and more potent, based on in vitro assays, than the known environmental antiandrogens linuron and p,p'-, 2,2-bis (p-hydroxyphenyl)-1,1-dichloroethylene ( p,p'-DDE). |
2(0,0,0,2) | Details |
| 15597887 | Wilson VS, Cardon MC, Thornton J, Korte JJ, Ankley GT, Welch J, Gray LE Jr, Hartig PC: Cloning and in vitro expression and characterization of the androgen receptor and isolation of estrogen receptor alpha from the fathead Minnow (Pimephales promelas). Environ Sci Technol. 2004 Dec 1;38(23):6314-21. We also report affinity of the receptor for a number of environmental contaminants including the AR agonists and 17a- and 17beta-trenbolone;AR antagonists such as p,p'-DDE, linuron, and vinclozolin; and the ER agonist 17beta- |
2(0,0,0,2) | Details |
| 16498641 | Mu X, Liu K, Kleymenova E, Sar M, Young SS, Gaido KW: Gene expression profiling of androgen receptor antagonists in the rat fetal testis reveals few common gene targets. J Biochem Mol Toxicol. 2006;20(1):7-17. Pregnant Sprague-Dawley rats were treated with flutamide (50 mg/kg/day), linuron (50 mg/kg/day), vinclozolin (200 mg/kg/day), p,p'-DDE (100 mg/kg/day) or corn oil vehicle by gavage daily from gestation day (GD) 12-19. |
2(0,0,0,2) | Details |
| 19833195 | Freyberger A, Weimer M, Tran HS, Ahr HJ: Assessment of a recombinant androgen receptor binding assay: Initial steps towards validation. Reprod Toxicol. 2009 Oct 13. Besides two reference compounds (DHT), ten test compounds with different affinities for the AR [levonorgestrel, prochloraz, 17alpha-methyltestosterone, flutamide, norethynodrel, o,p'-DDT, dibutylphthalate, vinclozolin, linuron] were used to explore the performance of the assay. |
1(0,0,0,1) | Details |
| 11861974 | Wilson VS, Bobseine K, Lambright CR, Gray LE Jr: A novel cell line, MDA-kb2, that stably expresses an androgen- and glucocorticoid-responsive reporter for the detection of hormone receptor agonists and antagonists. Toxicol Sci. 2002 Mar;66(1):69-81. In addition, known AR antagonists, including hydroxyflutamide, vinclozolin, vinclozolin metabolites M1 and M2, p,p'-DDE, and linuron inhibited DHT-induced luciferase gene expression at appropriate concentrations in this system. Environmental Protection Agency has proposed that in vitro assays for estrogen receptor (ER)- and androgen receptor (AR)-mediated actions be included in a Tier-I screening battery to detect hormonally active chemicals. |
1(0,0,0,1) | Details |
| 11403899 | Sultan C, Balaguer P, Terouanne B, Georget V, Paris F, Jeandel C, Lumbroso S, Nicolas J: Environmental xenoestrogens, antiandrogens and disorders of male sexual differentiation. Mol Cell Endocrinol. 2001 Jun 10;178(1-2):99-105. We also developed a model based on a fusion protein between the androgen receptor (AR) and the green fluorescent protein (GFP) to study the intracellular dynamics of AR. Environmental xenoestrogens (such as herbicides, pesticides, PCBs, plasticizers, and polystyrenes) that mimic estrogens or environmental antiandrogens (such as polyaromatic hydrocarbons, linuron, vinclozolin, and pp'DDE) that disturb endocrine balance, cause demasculinizing effects in the male foetus. |
1(0,0,0,1) | Details |
| 10188194 | Gray LE Jr, Wolf C, Lambright C, Mann P, Price M, Cooper RL, Ostby J: Administration of potentially antiandrogenic pesticides (procymidone, linuron, iprodione, chlozolinate, p,p'-DDE, and ketoconazole) and toxic substances (dibutyl- and diethylhexyl PCB 169, and ethane dimethane sulphonate) during sexual differentiation produces diverse profiles of reproductive malformations in the male rat. Toxicol Ind Health. 1999 Jan-Mar;15(1-2):94-118. For example, in utero treatment with the androgen receptor (AR) antagonist, flutamide, produces ventral prostate agenesis and testicular nondescent, while in contrast, finasteride, an inhibitor of 5 alpha- (DHT) synthesis, rarely, if ever, induces such malformations. |
1(0,0,0,1) | Details |
| 10910998 | Lambright C, Ostby J, Bobseine K, Wilson V, Hotchkiss AK, Mann PC, Gray LE Jr: Cellular and molecular mechanisms of action of linuron: an antiandrogenic herbicide that produces reproductive malformations in male rats. Toxicol Sci. 2000 Aug;56(2):389-99. Some, like flutamide, procymidone, or vinclozolin compete with androgens for the androgen receptor (AR), inhibit AR-DNA binding, and alter androgen-dependent gene expression in vivo and in vitro. |
1(0,0,0,1) | Details |
| 15147789 | Kang IH, Kim HS, Shin JH, Kim TS, Moon HJ, Kim IY, Choi KS, Kil KS, Park YI, Dong MS, Han SY: Comparison of anti-androgenic activity of flutamide, vinclozolin, procymidone, linuron, and p, p'-DDE in rodent 10-day Hershberger assay. Toxicology. 2004 Jul 1;199(2-3):145-59. Our results indicate that procymidone may act as a stronger androgen receptor (AR) antagonist than vinclozolin, linuron, or p,p'-DDE. |
1(0,0,0,1) | Details |
| 11392371 | Gray LE, Ostby J, Furr J, Wolf CJ, Lambright C, Parks L, Veeramachaneni DN, Wilson V, Price M, Hotchkiss A, Orlando E, Guillette L: Effects of environmental antiandrogens on reproductive development in experimental animals. Hum Reprod Update. 2001 May-Jun;7(3):248-64. Chemicals that act as androgen receptor (AR) agonists and antagonists or inhibit fetal steroidogenesis can induce reproductive malformations in humans and laboratory animals. The pesticides vinclozolin, procymidone, linuron and DDT are AR antagonists. |
1(0,0,0,1) | Details |
| 12215663 | O'Connor JC, Frame SR, Ladics GS: Evaluation of a 15-day screening assay using intact male rats for identifying antiandrogens. Toxicol Sci. 2002 Sep;69(1):92-108. The test compounds included cyproterone acetate (CPA), flutamide (FLUT), p,p'-DDE (DDE), di-n-butyl (DBP), linuron (LIN), and vinclozolin (VCZ). |
0(0,0,0,0) | Details |
| 18205796 | Rider CV, Furr J, Wilson VS, Gray LE Jr: A mixture of seven antiandrogens induces reproductive malformations in rats. Int J Androl. 2008 Apr;31(2):249-62. Epub 2008 Jan 16. In this study, pregnant rats were exposed to four dilutions of a mixture containing vinclozolin, procymidone, linuron, prochloraz, benzyl butyl dibutyl and diethylhexyl during the period of sexual differentiation and male offspring were assessed for effects on hormone sensitive endpoints including: anogenital distance, infant areolae retention and reproductive tract tissue weights and malformations. |
0(0,0,0,0) | Details |
| 18315717 | Wilson VS, Blystone CR, Hotchkiss AK, Rider CV, Gray LE Jr: Diverse mechanisms of anti-androgen action: impact on male rat reproductive tract development. Int J Androl. 2008 Apr;31(2):178-87. Classes of chemicals currently known to interfere with the androgen signalling pathway include dicarboximide fungicides (e.g. vinclozolin), organochlorine-based insecticides (e.g. p,p'-DDT and -DDE), conazole fungicides (e.g. prochloraz), plasticizers (phthalates) and urea-based herbicides (linuron). |
0(0,0,0,0) | Details |
| 19836445 | Freyberger A, Witters H, Weimer M, Lofink W, Berckmans P, Ahr HJ: Screening for (anti) androgenic properties using a standard operation protocol based on the human stably transfected androgen sensitive PALM cell line. Reprod Toxicol. 2009 Oct 27. A few compounds, 17alpha-methyltestosterone (17alpha-MT), vinclozolin and linuron, were studied using a real world scenario, i.e., assuming that their interaction with the AR was not known: A prescreening for agonism and true, competitive antagonism was used to select conditions such as the appropriate mode of action, and the working range excluding cytotoxicity for the final screening. |
0(0,0,0,0) | Details |