Steroid androgen receptor

A high-affinity non-steroidal androgen receptor ligand 1470 has been designed, of which a fragment, 2-iodo-4-nitrobenzonitrile, has been synthesized from its carboxamide 1468 by dehydration with thionyl chloride in 80% yield [1116]. 

The mechanism by which TBT causes these effects has been extensively stiidied. The androgenic effects of TBT appear to be caused by interference with steroid biosynthesis rather than by mimicking the action of testosterone at the androgen receptor. Exposure of female molluscs to TBT leads to an elevation in testosterone in the haemolymph. " Much of the experimental evidence... 

Sex Steroid Receptors Androgen Receptor, Estrogen Receptors, Progesterone Receptor... 

Sex steroid receptors are members of the steroid hormone receptor (SHR) family that ligand-dependently regulate functions of the sexual organs. Sex steroid receptors are the androgen receptor [1] (AR), the estrogen receptor a [2] and (3 [3] (ERa, ER 3), and the progesterone receptor [4] (PR). 

Sex Steroid Receptors Androgen Receptor, Estrogen Receptors, Progesterone Receptor. Figure 1 Schematic structures of AR, ERa, ER(3, and PR. 

Carilla E, Briley M, Fauran F, et al. Binding of Permixon, a new treatment for prostatic benign hyperplasia, to the cytosolic androgen receptor in the rat prostate. J Steroid Biochem 20 521-523, 1984. 

Both aromatization and 5a-reductase are regulated by gonadal steroids. In mammals such as the rat, it is principally the neural aromatase activity that is upregulated by androgens acting via neural androgen receptors [1],... 

The binding domain for the hormone, or LBD, is situated in the carboxyl half of the receptor, the final portion of which is critical. For example, the deletion of 12 amino acids in the carboxyl end of the androgen receptor suppresses its capacity to bind hormone (O Malley et al. 1974). The LBD has an amino acid composition that confers upon it a net hydrophobic character, suitable for interacting with organic molecules of low molecular weight, such as steroids. 

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