Estrogen Receptor Subtypes

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... 

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. 

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

DeLisle RK, Yu SJ, Welsh WJ. Homology modeling of the estrogen receptor subtype (ER- ) and prediction of ligand binding affinities. J Mol Graphics Model 2001 20 155-67. 

Wolohan P, Reichert DE. CoMFA and docking study of novel estrogen receptor subtype selective ligands. J Comput Aided Mol Des 2003 17 313-28. 

The estrogen receptor-subtype ERa mediates the hepatotoxicity of 17a-ethinylestradiol (EE2). Upon EE2 treatment, ERa represses the expression of bile acid and cholesterol transporters (bile salt export pump, BSEP), Na /taurocholate cotransporting polypeptide (NTCP), OATPl, OATP2, ABCG5, and ABCG8 in the liver [101]. The genetic variability of some of these transporters is well known and could explain, at least in part, the interindividual differences for the tolerability of oral contraceptives. 

Xin, D., H. Wang, J. Yang, et al. 2010. Phytoestrogens from Psoralea corylifolia reveal estrogen receptor-subtype selectivity. Phytomedicine 17(2) 126-131. 

It is not surprising that the pyrazine products of the Gutknecht synthesis have been frequently used as intermediates in the synthesis of biologically active compounds, both pharmaceuticals and agrochemicals. For example, a series of pyrazine derivatives (23, Ri = methyl, ethyl, propyl, wo-propyl, and n-butyl) have recently been examined as heterocyclic nonsteroidal estrogens with selectivity for estrogen receptor subtype ERa over ERp. ... 

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. 

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. 

Shiau, A.K., Barstad, D., Radek, J.T., Meyers, M.J., Nettles, K.W., Katzenel-lenbogen, B.S., Katzenellenbogbn, J.A., Agard, D.A., Greene, G.L Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism. Nat. Struct. 

Merchenthaler I, Lane MV, Numan S, Dellovade TL (2004) Distribution of estrogen receptor alpha and beta in the mouse central nervous system in vivo autoradiographic tmd immunocytochemical analyses. J Comp Neurol 473 270-291 Mezey E, Toth ZE, Corthright DN, Arzubi MK, Krause JE, Elde R, Guo A, Blumbeig PM, SzaUasi A (2000) Distribution of mRNA for vanUloid receptor subtype 1 (VRl), tmd VRl-hke immunorectivity, in the central nervous system of the rat and human. Proc Natl Acad Sci USA 97 3655-3660... 

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