Rooney, John published the artcileA Gene Expression Biomarker Identifies Chemical Modulators of Estrogen Receptor α in an MCF-7 Microarray Compendium, Related Products of chlorides-buliding-blocks, the publication is Chemical Research in Toxicology (2021), 34(2), 313-329, database is CAplus and MEDLINE.
Identification of chems. that affect hormone-regulated systems will help to predict endocrine disruption. In our previous study, a 46 gene biomarker was found to be an accurate predictor of estrogen receptor (ER) α modulation in chem. treated MCF-7 cells. Here, potential ERα modulators were identified using the biomarker by screening a microarray compendium consisting of ∼1600 gene expression comparisons representing exposure to ∼1200 chems. A total of ∼170 chems. were identified as potential ERα modulators. In the Connectivity Map 2.0 collection, 75 and 39 chems. were predicted to activate or suppress ERα, and they included 12 and 6 known ERα agonists and antagonists/selective ERα modulators, resp. Nineteen and 8 of the total number were also identified as active in an ERα trans-activation assay carried out in a MCF-7-derived cell line used to screen the Tox21 10K chem. library in agonist or antagonist modes, resp. Chems. predicted to modulate ERα in MCF-7 cells were examined further using global and targeted gene expression in wild-type and ERα-null cells, trans-activation assays, and cell-free ERα coregulator interaction assays. Environmental chems. classified as weak and very weak agonists were confirmed to activate ERα including apigenin, kaempferol, and oxybenzone. Novel activators included digoxin, nabumetone, ivermectin, and six progestins. Novel suppressors included emetine, mifepristone, niclosamide, and proscillaridin. Our strategy will be useful to identify environmentally relevant ERα modulators in future high-throughput transcriptomic screens.
Chemical Research in Toxicology published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Related Products of chlorides-buliding-blocks.
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