Protein Information

Name androgen receptor
Synonyms AIS; AR; Androgen receptor; DHTR; Dihydrotestosterone receptor; HUMARA; KD; NR3C4…

Compound Information

Name prochloraz
CAS

Reference List

PubMed Abstract RScore(About this table)
15901916 Ankley GT, Jensen KM, Durhan EJ, Makynen EA, Butterworth BC, Kahl MD, Villeneuve DL, Linnum A, Gray LE, Cardon M, Wilson VS: Effects of two fungicides with multiple modes of action on reproductive endocrine function in the fathead minnow (Pimephales promelas). Toxicol Sci. 2005 Aug;86(2):300-8. Epub 2005 May 18.

Notable in this regard are fungicides, such as prochloraz or fenarimol, which in mammals have the potential to impact endocrine function through inhibition of CYP enzymes involved in steroid metabolism, as well as through antagonism of the androgen receptor (s).
162(2,2,2,2) Details
17229592 Kinnberg K, Holbech H, Petersen GI, Bjerregaard P: Effects of the fungicide prochloraz on the sexual development of zebrafish (Danio rerio). Comp Biochem Physiol C Toxicol Pharmacol. 2007 Mar;145(2):165-70. Epub 2006 Nov 17.

Prochloraz is an imidazole fungicide that displays diverse mechanisms of action, including inhibition of aromatase activity, inhibition of androgen synthesis, and antagonism of the androgen receptor.
81(1,1,1,1) Details
17234647 Blystone CR, Furr J, Lambright CS, Howdeshell KL, Ryan BC, Wilson VS, Leblanc GA, Gray LE Jr: Prochloraz inhibits testosterone production at dosages below those that affect androgen-dependent organ weights or the onset of puberty in the male Sprague Dawley rat. Toxicol Sci. 2007 May;97(1):65-74. Epub 2007 Jan 18.

Prochloraz (PCZ) is an imidazole fungicide that inhibits gonadal steroidogenesis and antagonizes the androgen receptor (AR).
81(1,1,1,1) Details
20132345 Kjaerstad MB, Taxvig C, Andersen HR, Nellemann C: Mixture effects of endocrine disrupting compounds in vitro. Int J Androl. 2010 Jan 28.

It was found that additive effects on the same molecular target (the androgen receptor; AR) can be predicted for both mixtures of compounds with effect on the AR (flutamide, procymidone and vinclozolin) and of compounds with and without effects on the AR [finasteride, mono-(2-ethylhexyl) phthalate, prochloraz and vinclozolin].
31(0,1,1,1) 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 [dihydrotestosterone (DHT), androstenedione] ten test compounds with different affinities for the AR [levonorgestrel, progesterone, 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
16466539 Vinggaard AM, Hass U, Dalgaard M, Andersen HR, Bonefeld-Jorgensen E, Christiansen S, Laier P, Poulsen ME: Prochloraz: an imidazole fungicide with multiple mechanisms of action. Int J Androl. 2006 Feb;29(1):186-92.

Thus, a novel endocrine disruptor has been identified that is mechanistically interesting as it elicits dual mechanisms of action and acts as an antiandrogen both by blocking the androgen receptor and by inhibiting fetal steroidogenesis.
1(0,0,0,1) Details
15519604 Birkhoj M, Nellemann C, Jarfelt K, Jacobsen H, Andersen HR, Dalgaard M, Vinggaard AM: The combined antiandrogenic effects of five commonly used pesticides. Toxicol Appl Pharmacol. 2004 Nov 15;201(1):10-20.

Deltamethrin, methiocarb, prochloraz, simazine, and tribenuron-methyl are all commonly used for agricultural and horticultural purposes.
Concentration-response curves for the inhibition of R1881-induced transcriptional activity of the androgen receptor (AR) in vitro of each pesticide alone and in an equimolar mixture were obtained.
1(0,0,0,1) Details
15590119 Vinggaard AM, Jacobsen H, Metzdorff SB, Andersen HR, Nellemann C: Antiandrogenic effects in short-term in vivo studies of the fungicide fenarimol. Toxicology. 2005 Feb 1;207(1):21-34.

In an additional Hershberger test, the effects of fenarimol were compared to those of estradiol benzoate, prochloraz and the aromatase inhibitor fadrozole.
Thus, it is suggested that fenarimol mediates its antiandrogenic effects at least partly via antagonism of androgen receptors.
1(0,0,0,1) Details
15673607 Noriega NC, Ostby J, Lambright C, Wilson VS, Gray LE Jr: Late gestational exposure to the fungicide prochloraz delays the onset of parturition and causes reproductive malformations in male but not female rat offspring. Biol Reprod. 2005 Jun;72(6):1324-35. Epub 2005 Jan 26.

0(0,0,0,0) Details
11884232 Andersen HR, Vinggaard AM, Rasmussen TH, Gjermandsen IM, Bonefeld-Jorgensen EC: Effects of currently used pesticides in assays for estrogenicity, androgenicity, and aromatase activity in vitro. Toxicol Appl Pharmacol. 2002 Feb 15;179(1):1-12.

Twenty-four pesticides were tested for interactions with the estrogen receptor (ER) and the androgen receptor (AR) in transactivation assays.
Pesticides (endosulfan, methiocarb, methomyl, pirimicarb, propamocarb, deltamethrin, fenpropathrin, dimethoate, chlorpyriphos, dichlorvos, tolchlofos-methyl, vinclozolin, iprodion, fenarimol, prochloraz, fosetyl-aluminum, chlorothalonil, daminozid, paclobutrazol, chlormequat chlorid, and ethephon) were selected according to their frequent use in Danish greenhouses.
1(0,0,0,1) Details
12377983 Vinggaard AM, Nellemann C, Dalgaard M, Jorgensen EB, Andersen HR: Antiandrogenic effects in vitro and in vivo of the fungicide prochloraz. . Toxicol Sci. 2002 Oct;69(2):344-53.

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.


All other compounds were tested according to the generic protocol: Compounds screened for agonism were the reference androgen 17alpha-methyldihydrotestosterone (MDHT), levonorgestrel, norethynodrel, progesterone, o,p'-DDT, and dibutylphthalate (DBP), while compounds screened for antagonism were the reference anti-androgen flutamide, prochloraz, o,p'-DDT, progesterone, norethynodrel, and DBP.
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 phthalate, dibutyl phthalate and diethylhexyl phthalate 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