Design of antiandrogens and their mechanisms of action: a case study (anandron).

@article{Raynaud1987DesignOA,
  title={Design of antiandrogens and their mechanisms of action: a case study (anandron).},
  author={Jean Pierre Raynaud and Jean Fiet and J.-M. Le Goff and P. M. Martin and Martine Moguilewsky and Tiiu Ojasoo},
  journal={Hormone research},
  year={1987},
  volume={28 2-4},
  pages={
          230-41
        }
}
The design of a new drug is conditioned by knowledge of the biochemical mechanisms involved in the etiology of the disease to be treated. With regard to endocrine pathologies, such knowledge can be obtained in the clinic from systematic assays of urinary and plasma hormones, enzyme activities and target tissue receptor concentrations. The present paper describes the results of our assays of plasma 3 alpha-androstanediol glucuronide, 5 alpha-reductase and androgen receptor in prostate cancer… Expand
Chapter 21. New Horizons in the Treatment of Proliferative Prostatic Disease
TLDR
The discovery and development of potent and selective inhibitors of 5α-reductase and “pure” AR antagonists that do not uncouple negative-feedback at the hypothalamic/pituitary demonstrates continuing interest in this therapeutic arena. Expand
Ockham's razor and selective androgen receptor modulators (SARMs): are we overlooking the role of 5alpha-reductase?
TLDR
The tissue-specific expression of 5alpha-reductase might provide a simple explanation for this puzzle of the SARM story, and lead compounds with much improved specificity for AR, in vivo pharmacokinetic profiles, and higher degree of tissue selectivity have entered clinical development. Expand
Nilutamide: An Antiandrogen for the Treatment of Prostate Cancer
TLDR
Nilutamide does not appear to represent a major advance in the treatment of advanced prostate cancer and appears to be somewhat inferior to both flutamide and bicalutamide with regard to adverse effects. Expand
Non-michaelian behavior of 5α-reductase in human prostate
TLDR
It is postulate that regulation of 5α-reductase activity in the prostate depends on the molecular flexibility of the enzyme and on changes in the cooperativity of different enzyme forms over time, as previously described for other key metabolic enzymes. Expand
Inhibition of the activity of ‘basic’ 5α-reductase (type 1) detected in DU 145 cells and expressed in insect cells
TLDR
Two studies suggest that LSESr might exert a regulatory inhibitory activity due to its specific lipid/sterol composition and, when expressed in terms of recommended therapeutic doses, was 3-fold greater for LSESR than for finasteride. Expand
Ensayo de actividad antimutagénica de un nuevo neuroesteroide sintético (3α-acetoxi-5,6-epoxi-16-pregnen-20-ona)
Synthetic progestins are used in different types of cancer and hormonal replacement therapy, and in recent studies they have been linked to DNA adduct formation in steroid therapies. The purpose ofExpand
Effects of two new steroids and cyproterone on some biomarkers of oxidative stress and serotonergic system on rat prostate and brain
TLDR
It is concluded that CPA and the homologues B and C steroids induce changes in the levels of GSH and serotonin in rat prostate and brain. Expand
Pathological and morphometric assessment of testicular parameters in patients with metastatic prostate cancer following treatment with either the antiandrogen Casodex (ZM176,334) or bilateral orchidectomy
TLDR
No evidence for induction of Leydig cell hypertrophy or hyperplasia as a result of chronic oral administration of 50 mg Casodex daily was obtained in this study. Expand
Multivariate analysis of plasma hormones in patients with metastatic prostate cancer receiving combined LHRH‐analog and antiandrogen therapy
TLDR
Multivariate analysis of the treatment values by two complementary methods, correspondence factorial analysis (CFA) and the minimum spanning tree (MST) method, identified those variables within the pathways of androgen metabolism that were correlated over time and, in a comparison of the two treatment groups, identified the enzyme targets of nilutamide action in humans. Expand
Anti‐androgenic effects of Win 49,596 on development of the neonatal mouse bulbourethral gland in culture
TLDR
In summary, Win 49,596 produced a dose‐dependent suppression of BUG development in vitro, and was not androgenic. Expand