title: Nuclear receptor profiling of bisphenol-A and its halogenated analogues.
abstract: Bisphenol-A (BPA) is one of the highest-volume chemicals produced worldwide and the widespread exposure of individuals to BPA is suspected to affect a variety of physiological functions, including reproduction, development, and metabolism. Its estrogenic activity has been well documented in the last 15 years. In addition to estrogen receptors, BPA has been also shown to bind to and activate the estrogen-related receptor γ and pregnane X receptor and inhibit the androgen receptor. Halogenated BPAs were also shown to activate the peroxisome proliferator-activated receptor γ and inhibit thyroid hormone receptors. In this chapter, we review recent studies shedding light on the structural and molecular mechanisms by which BPA and its halogenated derivatives interfere with nuclear hormone receptor signaling. These data provide guidelines for the development of safer substitutes devoid of hormonal activity and may help environmental risk assessment.
authors.affiliation: Centre de Biochimie Structurale, Institut National de la Santé et de la Recherche Médicale U1054, Montpellier, France; Centre National de la Recherche Scientifique, Unité Mixte de Recherche 5048; Universités Montpellier 1 and 2, Montpellier, France.
authors.forename: Vanessa
authors.initials: V
authors.lastname: Delfosse
authors.affiliation: Institut de Recherche en Cancérologie de Montpellier, Montpellier, France; Institut National de la Santé et de la Recherche Médicale U896, Montpellier, France; Institut régional du Cancer de Montpellier, Montpellier, France; Universités Montpellier 1, Montpellier, France.
authors.forename: Marina
authors.initials: M
authors.lastname: Grimaldi
authors.affiliation: Centre de Biochimie Structurale, Institut National de la Santé et de la Recherche Médicale U1054, Montpellier, France; Centre National de la Recherche Scientifique, Unité Mixte de Recherche 5048; Universités Montpellier 1 and 2, Montpellier, France.
authors.forename: Albane
authors.initials: A
authors.lastname: le Maire
authors.affiliation: Centre de Biochimie Structurale, Institut National de la Santé et de la Recherche Médicale U1054, Montpellier, France; Centre National de la Recherche Scientifique, Unité Mixte de Recherche 5048; Universités Montpellier 1 and 2, Montpellier, France. Electronic address: bourguet@cbs.cnrs.fr.
authors.forename: William
authors.initials: W
authors.lastname: Bourguet
authors.affiliation: Institut de Recherche en Cancérologie de Montpellier, Montpellier, France; Institut National de la Santé et de la Recherche Médicale U896, Montpellier, France; Institut régional du Cancer de Montpellier, Montpellier, France; Universités Montpellier 1, Montpellier, France. Electronic address: patrick.balaguer@icm.unicancer.fr.
authors.forename: Patrick
authors.initials: P
authors.lastname: Balaguer
mesh_terms: D000726:Androgen Antagonists / Q000737:chemistry / Q000633:toxicity*; D000818:Animals; D001559:Benzhydryl Compounds / Q000737:chemistry / Q000633:toxicity*; D052244:Endocrine Disruptors / Q000737:chemistry / Q000633:toxicity; D004785:Environmental Pollutants / Q000737:chemistry / Q000633:toxicity*; D004968:Estrogens, Non-Steroidal / Q000737:chemistry / Q000633:toxicity*; D054879:Halogenation; D006801:Humans; D047495:PPAR gamma / Q000819:agonists* / Q000378:metabolism; D010636:Phenols / Q000737:chemistry / Q000633:toxicity*; D000077297:Pregnane X Receptor; D011944:Receptors, Androgen / Q000737:chemistry / Q000378:metabolism; D011960:Receptors, Estrogen / Q000819:agonists / Q000378:metabolism; D011987:Receptors, Steroid / Q000819:agonists* / Q000378:metabolism; D011988:Receptors, Thyroid Hormone / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000098826:Bisphenol A Compounds
chemical_list: D000726:Androgen Antagonists; D001559:Benzhydryl Compounds; D052244:Endocrine Disruptors; D004785:Environmental Pollutants; D004968:Estrogens, Non-Steroidal; D047495:PPAR gamma; D010636:Phenols; D000077297:Pregnane X Receptor; D011944:Receptors, Androgen; D011960:Receptors, Estrogen; D011987:Receptors, Steroid; D011988:Receptors, Thyroid Hormone; C006780:bisphenol A; D000098826:Bisphenol A Compounds
keywords: Bisphenol-A; Endocrine disruptor; Halogenated bisphenol-A; Nuclear hormone receptor