Evaluating the interactions of vertebrate receptors with persistent pollutants and antifouling pesticides using recombinant yeast assays.

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Noguerol TN, Boronat S, Casado M, Raldua D, Barcelo D, Pina B

Evaluating the interactions of vertebrate receptors with persistent pollutants and antifouling pesticides using recombinant yeast assays.

Anal Bioanal Chem. 2006 Jul;385(6):1012-9. Epub 2006 May 17.

PubMed ID

16705413 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
1-[(4S)-4-amino-5-(1,3-benzothiazol-2-yl)-5-oxopentyl]guanidine	Aryl hydrocarbon receptor	Protein	Humans	Unknown	Not Available	Details