High-throughput screening assays for the identification of chemical probes.
- James Inglese, Ronald L. Johnson, D. Auld
- BiologyNature Chemical Biology
- 1 August 2007
High-throughput screening (HTS) assays enable the testing of large numbers of chemical substances for activity in diverse areas of biology. The biological responses measured in HTS assays span…
Integrated Model of Chemical Perturbations of a Biological Pathway Using 18 In Vitro High-Throughput Screening Assays for the Estrogen Receptor.
- R. Judson, F. Magpantay, Russell S. Thomas
- BiologyToxicological Sciences
- 1 November 2015
A computational network model is demonstrated that integrates 18 in vitro, high-throughput screening assays measuring estrogen receptor (ER) binding, dimerization, chromatin binding, transcriptional activation, and ER-dependent cell proliferation and is generalizable to any molecular pathway for which there are multiple upstream and downstream assays available.
Analysis of eight oil spill dispersants using rapid, in vitro tests for endocrine and other biological activity.
- R. Judson, Matt T. Martin, D. Dix
- Biology, ChemistryEnvironmental Science and Technology
- 1 August 2010
A series of in vitro high-throughput assays on eight commercial dispersants focused on the estrogen and androgen receptors (ER and AR), but also included a larger battery of assays probing other biological pathways.
Small Molecule Inhibitor of NRF2 Selectively Intervenes Therapeutic Resistance in KEAP1-Deficient NSCLC Tumors.
- Anju Singh, Sreedhar Venkannagari, S. Biswal
- Chemistry, BiologyACS Chemical Biology
- 17 October 2016
It is concluded that targeting NRF2 may represent a promising strategy for the treatment of advanced NSCLC because of its high specificity and selectivity and its ability to bind to and inhibit its downstream target gene expression.
Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen
- Miao Xu, Emily M. Lee, Hengli Tang
- Biology, MedicineNature Network Boston
- 29 August 2016
A pan-caspase inhibitor, emricasan, inhibited ZIKV-induced increases in caspase-3 activity and protected human cortical neural progenitors in both monolayer and three-dimensional organoid cultures, and combination treatments using one compound from each category (neuroprotective and antiviral) further increased protection of human neural progensitors and astrocytes from ZIKv-induced cell death.
Identification of known drugs that act as inhibitors of NF-kappaB signaling and their mechanism of action.
- S. Miller, Ruili Huang, M. Xia
- Biology, ChemistryBiochemical Pharmacology
- 1 May 2010
Compound Cytotoxicity Profiling Using Quantitative High-Throughput Screening
- M. Xia, Ruili Huang, C. Austin
- Biology, MedicineEnvironmental Health Perspectives
- 22 November 2007
The generation of high-quality cytotoxicity data on this large library of known compounds using qHTS demonstrates the potential of this methodology to profile a much broader array of assays and compounds, which, in aggregate, may be valuable for prioritizing compounds for further toxicologic evaluation, identifying compounds with particular mechanisms of action, and potentially predicting in vivo biological response.
Tox21Challenge to Build Predictive Models of Nuclear Receptor and Stress Response Pathways as Mediated by Exposure to Environmental Chemicals and Drugs
- Ruili Huang, M. Xia, A. Simeonov
- BiologyFrontiers in Environmental Science
- 14 January 2016
The competition attracted participants from 18 different countries to develop computational models aimed at better predicting chemical toxicity, and several models exceeded 90% accuracy, which was measured by area under the receiver operating characteristic curve (AUC-ROC).
Using in Vitro High Throughput Screening Assays to Identify Potential Endocrine-Disrupting Chemicals
- D. Rotroff, D. Dix, R. Judson
- Medicine, BiologyEnvironmental Health Perspectives
- 28 September 2012
Overall, results suggest that current ToxCast assays can accurately identify chemicals with potential to interact with the estrogenic and androgenic pathways, and could help prioritize chemicals for EDSP T1S assays.
Chemical Genomics Profiling of Environmental Chemical Modulation of Human Nuclear Receptors
- Ruili Huang, M. Xia, C. Austin
- BiologyEnvironmental Health Perspectives
- 4 May 2011
Background: The large and increasing number of chemicals released into the environment demands more efficient and cost-effective approaches for assessing environmental chemical toxicity. The U.S.…