title: Evaluating the interactions of vertebrate receptors with persistent pollutants and antifouling pesticides using recombinant yeast assays.
abstract: The development of in vitro methods for screening potentially harmful biological activities of new compounds is an extremely important way to increase not only their intrinsic environmental safety, but also the public perception of the safety standards associated with them. In this work we use two yeast systems to test the ability of different chemicals to bind and activate two vertebrate receptors which are intimately related to adverse biological effects of pollution in exposed fauna: the estrogen receptor (ER) and the aryl hydrocarbon receptor (AhR). The panel of compounds analysed here includes well-known pollutants, like PCBs, pp'-DDT and hexachlorobenzene, together with the less-known, emerging putative pollutants, such as Sea-Nine, Irgarol and diuron. Results show the ability of some of these compounds to interact with one or both receptors, provide hints about the relationship between structure and activity, and suggest mechanistic explanations for the biological activities already described in whole-animal experiments. In addition, we show that AhR may have an intrinsic ligand promiscuity comparable to that of ER, a feature not fully appreciated in the past due to the technical difficulties involved with testing highly lipophilic substances in yeast-based assays.
authors.affiliation: Department of Molecular Biology, Institut de Biologia Molecular de Barcelona, CSIC, Jordi Girona 18-26, 08034 Barcelona, Spain.
authors.forename: Tania-Noelia
authors.initials: TN
authors.lastname: Noguerol
authors.forename: Susanna
authors.initials: S
authors.lastname: Boronat
authors.forename: Marta
authors.initials: M
authors.lastname: Casado
authors.forename: Demetrio
authors.initials: D
authors.lastname: Raldúa
authors.forename: Damià
authors.initials: D
authors.lastname: Barceló
authors.forename: Benjamin
authors.initials: B
authors.lastname: Piña
mesh_terms: D000818:Animals; D001681:Biological Assay / Q000379:methods*; D003634:DDT; D004237:Diuron; D004785:Environmental Pollutants / Q000493:pharmacokinetics*; D006581:Hexachlorobenzene; D008024:Ligands; D010575:Pesticides / Q000493:pharmacokinetics*; D011078:Polychlorinated Biphenyls; D011485:Protein Binding; D018336:Receptors, Aryl Hydrocarbon / Q000378:metabolism*; D011960:Receptors, Estrogen / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013844:Thiazoles; D014227:Triazines; D020798:Two-Hybrid System Techniques; D014714:Vertebrates
chemical_list: D004785:Environmental Pollutants; D008024:Ligands; D010575:Pesticides; D018336:Receptors, Aryl Hydrocarbon; D011960:Receptors, Estrogen; D013844:Thiazoles; D014227:Triazines; C103341:irgarol 1051; D006581:Hexachlorobenzene; C080469:Kathon 930; D004237:Diuron; D003634:DDT; D011078:Polychlorinated Biphenyls