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The Alginate Immobilization of Metabolic Enzymes (AIME) Platform Retrofits an Estrogen Receptor Transactivation Assay with Metabolic Competence
The objective of this study was to develop an approach to retrofit existing HTS assays with hepatic metabolism. The Alginate Immobilization of Metabolic Enzymes (AIME) platform encapsulates hepatic S9 fractions in alginate microspheres attached to 96-well peg lids. Functional characterization across a panel of reference substrates for phase I cytochrome P450 enzymes revealed substrate depletion with expected metabolite accumulation. Performance of the AIME method in the VM7Luc estrogen receptor (ER) transactivation assay was evaluated across 15 reference chemicals and 48 test chemicals that yield metabolites previously identified as ER active or inactive.
This dataset is associated with the following publication:
Deisenroth, C., D. DeGroot, T. Zurlinden, A. Eicher, J. McCord, M. Lee, P. Carmichael, and R. Thomas. The Alginate Immobilization of Metabolic Enzymes Platform Retrofits an Estrogen Receptor Transactivation Assay with Metabolic Competence. TOXICOLOGICAL SCIENCES. Society of Toxicology, RESTON, VA, 178(2): 281-301, (2020).
Complete Metadata
| accessLevel | public |
|---|---|
| bureauCode |
[
"020:00"
]
|
| contactPoint |
{
"fn": "Chad Deisenroth",
"hasEmail": "mailto:deisenroth.chad@epa.gov"
}
|
| description | The objective of this study was to develop an approach to retrofit existing HTS assays with hepatic metabolism. The Alginate Immobilization of Metabolic Enzymes (AIME) platform encapsulates hepatic S9 fractions in alginate microspheres attached to 96-well peg lids. Functional characterization across a panel of reference substrates for phase I cytochrome P450 enzymes revealed substrate depletion with expected metabolite accumulation. Performance of the AIME method in the VM7Luc estrogen receptor (ER) transactivation assay was evaluated across 15 reference chemicals and 48 test chemicals that yield metabolites previously identified as ER active or inactive. This dataset is associated with the following publication: Deisenroth, C., D. DeGroot, T. Zurlinden, A. Eicher, J. McCord, M. Lee, P. Carmichael, and R. Thomas. The Alginate Immobilization of Metabolic Enzymes Platform Retrofits an Estrogen Receptor Transactivation Assay with Metabolic Competence. TOXICOLOGICAL SCIENCES. Society of Toxicology, RESTON, VA, 178(2): 281-301, (2020). |
| distribution |
[
{
"title": "https://doi.org/10.5061/dryad.r2280gbb7",
"accessURL": "https://doi.org/10.5061/dryad.r2280gbb7"
}
]
|
| identifier | https://doi.org/10.23719/1518903 |
| keyword |
[
"endocrine toxicology",
"estrogen receptor",
"high-throughput screening",
"xenobiotic metabolism"
]
|
| license | https://pasteur.epa.gov/license/sciencehub-license.html |
| modified | 2020-08-24 |
| programCode |
[
"020:095"
]
|
| publisher |
{
"name": "U.S. EPA Office of Research and Development (ORD)",
"subOrganizationOf": {
"name": "U.S. Environmental Protection Agency",
"subOrganizationOf": {
"name": "U.S. Government"
}
}
}
|
| references |
[
"https://doi.org/10.1093/toxsci/kfaa147"
]
|
| rights |
null
|
| title | The Alginate Immobilization of Metabolic Enzymes (AIME) Platform Retrofits an Estrogen Receptor Transactivation Assay with Metabolic Competence |
