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Int. J. Environ. Res. Public Health 2014, 11(9), 8709-8742; doi:10.3390/ijerph110908709

Versatility or Promiscuity: The Estrogen Receptors, Control of Ligand Selectivity and an Update on Subtype Selective Ligands

Division of Bioinformatics and Biostatistics, National Center for Toxicological Research, US Food and Drug Administration, 3900 NCTR Road, Jefferson, AR 72079, USA
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Received: 18 June 2014 / Revised: 13 August 2014 / Accepted: 14 August 2014 / Published: 26 August 2014
(This article belongs to the Special Issue Endocrine Disruptors and Human Health)
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Abstract

The estrogen receptors (ERs) are a group of versatile receptors. They regulate an enormity of processes starting in early life and continuing through sexual reproduction, development, and end of life. This review provides a background and structural perspective for the ERs as part of the nuclear receptor superfamily and discusses the ER versatility and promiscuity. The wide repertoire of ER actions is mediated mostly through ligand-activated transcription factors and many DNA response elements in most tissues and organs. Their versatility, however, comes with the drawback of promiscuous interactions with structurally diverse exogenous chemicals with potential for a wide range of adverse health outcomes. Even when interacting with endogenous hormones, ER actions can have adverse effects in disease progression. Finally, how nature controls ER specificity and how the subtle differences in receptor subtypes are exploited in pharmaceutical design to achieve binding specificity and subtype selectivity for desired biological response are discussed. The intent of this review is to complement the large body of literature with emphasis on most recent developments in selective ER ligands. View Full-Text
Keywords: estrogen receptors (ERs) ; estrogen receptor alpha (ERα); estrogen receptor beta (ERβ); promiscuity; ligand selectivity; subtype selective ligands estrogen receptors (ERs) ; estrogen receptor alpha (ERα); estrogen receptor beta (ERβ); promiscuity; ligand selectivity; subtype selective ligands
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Ng, H.W.; Perkins, R.; Tong, W.; Hong, H. Versatility or Promiscuity: The Estrogen Receptors, Control of Ligand Selectivity and an Update on Subtype Selective Ligands. Int. J. Environ. Res. Public Health 2014, 11, 8709-8742.

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