Test No. 493: Performance-Based Test Guideline for Human Recombinant Estrogen Receptor (hrER) In Vitro Assays to Detect Chemicals with ER Binding Affinity / Organisation for Economic Co-operation and Development.

Organisation for Economic Co-operation and Development.
Paris : OECD Publishing, 2015.
Government document
1 online resource (64 pages).
OECD Guidelines for the Testing of Chemicals Section 4 20745788.
OECD Guidelines for the Testing of Chemicals, Section 4 20745788.

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This Performance-Based Test Guideline (PBTG) describes in vitro assays, which provide the methodology for human recombinant in vitro assays to detect substances with estrogen receptor binding affinity (hrER binding assays). It comprises two mechanistically and functionally similar test methods for the identification of estrogen receptor (id est ERα) binders and should facilitate the development of new similar or modified test methods. The two reference test methods that provide the basis for this PBTG are: the Freyberger-Wilson (FW) In Vitro Estrogen Receptor (ER) Binding Assay Using a Full Length Human Recombinant ERα, and the Chemical Evaluation and Research Institute (CERI) In Vitro Estrogen Receptor Binding Assay Using a Human Recombinant Ligand Binding Domain Proteinches This assay measures the ability of a radiolabeled ligand ([3H]17β-estradiol) to bind with the ER in the presence of increasing concentrations of a test chemical (id est competitor).  Test chemicals that possess a high affinity for the ER compete with the radiolabeled ligand at a lower concentration as compared with those chemicals with lower affinity for the receptor. This assay consists of two major components: a saturation binding experiment to characterise receptor-ligand interaction parameters and document ER specificity, followed by a competitive binding experiment that characterises the competition between a test chemical and a radiolabeled ligand for binding to the ER. These test methods are being proposed for screening and prioritisation purposes, but also provide mechanistic information that can be used in a weight of evidence approach.
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SourceOECD (Online Service)
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