Structure–activity relationships of synthetic progestins in a yeast-based in vitro androgen bioassay

McRobb, Lucinda S.; Handelsman, David J.; Kazlauskas, Rymantas; Wilkinson, Shane M.; McLeod, Malcolm D.; Heather, Alison K.

doi:10.1016/j.jsbmb.2007.10.008

Cited by 43 publications

(54 citation statements)

References 47 publications

(61 reference statements)

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“…However, the MMTV promoter in a useful for modeling the steroid hormone response (Adom et al 1991, Truss et al 1992, McNally et al 2000, Nagaich et al 2004, Vicent et al 2010, Wiench et al 2011. Chinese hamster ovarian (CHO) cells are not the ideal vehicle to explore the bioactivation of progesterone receptors by potential agonists, although even yeast-based assays have been utilized successfully and extensively (McRobb et al 2008). Primary cell cultures of equine endometrial epithelium, myometrium or mammary glandular epithelium could provide a better physiological cell model if they retained responsiveness in vitro.…”

Section: Discussionmentioning

confidence: 99%

Progestin withdrawal at parturition in the mare

Legacki¹,

Corbin²,

Ball³

et al. 2016

Reproduction

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Mammalian pregnancies need progestogenic support and birth requires progestin withdrawal. The absence of progesterone in pregnant mares, and the progestogenic bioactivity of 5α-dihydroprogesterone (DHP), led us to reexamine progestin withdrawal at foaling. Systemic pregnane concentrations (DHP, allopregnanolone, pregnenolone, 5α-pregnane-3β, 20α-diol (3β,20αDHP), 20α-hydroxy-5α-dihydroprogesterone (20αDHP)) and progesterone) were monitored in mares for 10 days before foaling (n = 7) by liquid chromatography-mass spectrometry. The biopotency of dominant metabolites was assessed using luciferase reporter assays.

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Section: Discussionmentioning

confidence: 99%

Progestin withdrawal at parturition in the mare

Legacki¹,

Corbin²,

Ball³

et al. 2016

Reproduction

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“…A recent report on in vitro potency of progestins for the human PR and androgen receptor identified altrenogest as the most potent progestogen and the most potent androgen of all steroids tested. Altrenogest was actually five times more potent than testosterone itself in the human androgen receptor bioassay [105]. Anabolic steroids have been shown to impair the fertility of mares after treatment in the breeding season, exhibiting shortened estrous periods, abnormal behavior, and detrimental effects on the reproductive tract [106].…”

Section: The Luteo-placental Shiftmentioning

confidence: 99%

Review of the reproductive endocrinology of the pregnant and parturient mare

Conley

2016

Theriogenology

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“…Later, THG was detected in a human urine sample using a bioassay in combination with LC/TOFMS [38]. Structural modification of either the T or progesterone background could produce an almost limitless number of androgenic steroids with structures that are not on the WADA detection list [39]. Also in development for clinical use are non-steroidal androgenic molecules (SARMs) that too will pose a risk to sports doping because of their ability to activate the AR.…”

Section: Androgen Detection Methodsmentioning

confidence: 99%

In Vitro Androgen Bioassays as a Detection Method for Designer Androgens

Cooper

McGrath

Heather

2013

Sensors

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Androgens are the class of sex steroids responsible for male sexual characteristics, including increased muscle mass and decreased fat mass. Illicit use of androgen doping can be an attractive option for those looking to enhance sporting performance and/or physical appearance. The use of in vitro bioassays to detect androgens, especially designer or proandrogens, is becoming increasingly important in combating androgen doping associated with nutritional supplements. The nutritional sports supplement market has grown rapidly throughout the past decade. Many of these supplements contain androgens, designer androgens or proandrogens. Many designer or proandrogens cannot be detected by the standard highly-sensitive screening methods such as gas chromatography-mass spectrometry because their chemical structure is unknown. However, in vitro androgen bioassays can detect designer and proandrogens as these assays are not reliant on knowing the chemical structure but instead are based on androgen receptor activation. For these reasons, it may be advantageous to use routine androgen bioassay screening of nutraceutical samples to help curb the increasing problem of androgen doping.

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Structure–activity relationships of synthetic progestins in a yeast-based in vitro androgen bioassay

Cited by 43 publications

References 47 publications

Progestin withdrawal at parturition in the mare

Progestin withdrawal at parturition in the mare

Review of the reproductive endocrinology of the pregnant and parturient mare

In Vitro Androgen Bioassays as a Detection Method for Designer Androgens

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