Androgen receptor binding

Androgen receptor binding/Reporter gene assay. 

Cyproterone acetate is a progestational antiandrogen that blocks androgen receptor binding and suppresses androgen-sensitive tissues. It is available in a topical form in Europe for the treatment of hirsutism. 

L15. Luke, M. C., and Coffey, D. S., Human androgen receptor binding to the androgen response element of prostate specific antigen. J. Androl. 15,41—51 (1994). 

Androgen receptor binding affinities were determined using competitive binding assays described by Kirkovsky (1) and summarized in Table 1. 

Serafimova R, Walker J, Mekenyan O. Androgen receptor binding affinity of pesticide active formulation ingredients QSAR evaluation by COREPA method. SAR QSAR Environ Res 2002 13 127-34. 

Rasmusson, G.H., G.F. Reynolds, N.G. Sieinberg, E. Walton, G.F. Patel, T. Liang, M.A. Cascieri, A.H. Cheung, J.R. Brooks, and C. Berman (1986). Azasteroids Structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding. J. Med. Chem. 29, 2298. 

Shaffer PL, Jivan Arif, Dollins DE, et al. Structural basis of androgen receptor binding to selective androgen response elements. Proc Natl Acad Sci U S A 2004 101 4758-4763. 

Rasmusson GH, Reynolds GF, Steinberg NG, et al. Azasteroids structure-activity relationships for inhibition of 5a-reductase and of androgen receptor binding. J Med Chem 1986 29 2298. 

In many but not all types of responsive cells, testosterone is extensively and irreversibly reduced to DHT by NADPH-specific 5a-steroid reductases located on the endoplasmic reticulum and the nuclear membrane. The cytoplasmic form of the androgen receptor binds DHT... 

First, the growth inhibitory effect of LNCaP-P cells was around 17% for 9-cis retinoic acid (30), arormd 21-24% for aW-trans retinoic acid (29) treatnent, and aroimd 19-22% for the treatment with mibolerone (MB. 48) of androgenic receptor binding repressor, respeetively. 

Endocrine active Androgen receptor binding assay (rat prostate cytosol) Ex vivo... 

RA and its isomers inhibit prostate epithelial cell growth [54]. Inhibition of RA metabolism raises plasma RA and inhibits relapse in the rat Dunning prostate cancer model [55]. RA decreases the concentrations of dihydrotestosterone, 3a-adiol and androsterone in serum, seems to cause a metabolic deviation away from the 5a-reductase path in liver [56], and causes a three-fold decrease in androgen receptor binding capacity [57]. Conversely, androgens affect the actions of retinoids by decreasing the mRNA of RARa approximately five-fold in prostate epithelia and 15 to 20-fold in seminal vesicles, while increasing it two-fold in kidney [58]. 

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