Estrogen subtypes

Kuiper, G. G. J. M., Shughrue, P. J., Merchenthaler, I. and Gustafsson, J.-A. The estrogen receptor (3 subtype a novel mediator of estrogen action in neuroendocrine systems. Frontiers Neuroendocrinol. 19 253-286,1998. 

Mclnerney EM, Weis KE, Sun J, Mosselman S, Katzenellenbogen BS (1998) Transcription activation by the human estrogen receptor subtype beta (ERb) studied with ERa and ERb receptor chimeras. Endocrinology 139 4513... 

In rats and mice both ER transcripts and proteins have been identified in 60-70% of anterior pituitary cells (Kuiper et al. 1997 Wilson et al. 1998 Wilson et al. 1998 Nishihara et al. 2000 Pelletier et al. 2000). While ERa is the predominant subtype in adult rats, in anterior pituitaries from fetal and prepubertal animals ER/i appears to be expressed in greater abundance (Nishihara et al. 2000). In addition, differential developmental and estrogen-dependent expression of pituitary ERs has been reported (Pasqualini et al. 1999). Approximately... 

Vaillant C, Chesnel F, Schausi D, Tiffoche C, Thieulant M-L (2002) Expression of estrogen receptor subtypes in rat pituitary gland during pregnancy and lactation. Endocrinology 143 4249-4258... 

For the sake of comparison, the 3-character code for the human estrogen receptor subtype a is 3.A.1, whereas the NC-IUPHAR RC would be 4.1.3 EST 1 ERA HUMAN 00. 

The physiological functions of the ER subtypes have been characterised in mice lacking the ERa, the ER/1, or both receptors [11]. Disruption of the ERo resulted in infertility of both male and female mice and inhibited the outgrowth of the mammary duct during puberty, whereas disruption of the ER/1 had no effect on fertihty and mammary gland development [ 17]. A number of ERo and ER/1 isoforms have also been described, many of which alter estrogen-mediated gene expression [18]. 

Wolohan, P., Reichert, D.E. CoMFAand Docking Study of Novel Estrogen Receptor Subtype Selective Ligands. J. Comput.-Aided Mol Des. 2003, 27, 313-328. 

Estrogen receptors constitute the only known members of the family of steroid receptors that have multiple subtypes. This diversity of ERs offers unique possibilities for the modulation of estrogen-responsive genes. 

Tong, W.D., Perkins, R., Xing, L., Welsh, W.J., and Sheehan, D.M., QSAR models for binding of estrogenic compounds to estrogen receptor alpha and beta subtypes, Endocrinology, 138, 4022-4025, 1997b. 

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