Medvedev, Alexander published the artcileComprehensive assessment of NR ligand polypharmacology by a multiplex reporter NR assay, Computed Properties of 6217-54-5, the publication is Scientific Reports (2022), 12(1), 3115, database is CAplus and MEDLINE.
Nuclear receptors (NR) are ligand-modulated transcription factors that regulate multiple cell functions and thus represent excellent drug targets. However, due to a considerable NR structural homol., NR ligands often interact with multiple receptors. Here, we describe a multiplex reporter assay (the FACTORIAL NR) that enables parallel assessment of NR ligand activity across all 48 human NRs. The assay comprises one-hybrid GAL4-NR reporter modules transiently transfected into test cells. To evaluate the reporter activity, we assessed their RNA transcripts. We used a homogeneous RNA detection approach that afforded equal detection efficacy and permitted the multiplex detection in a single-well format. For validation, we examined a panel of selective NR ligands and polypharmacol. agonists and antagonists of the progestin, estrogen, PPAR, ERR, and ROR receptors. The assay produced highly reproducible NR activity profiles (r > 0.96) permitting quant. assessment of individual NR responses. The inferred EC50 values agreed with the published data. The assay showed excellent quality (<Z> = 0.73) and low variability (<CV> = 7.2%). Furthermore, the assay permitted distinguishing direct and non-direct NR responses to ligands. Therefore, the FACTORIAL NR enables comprehensive evaluation of NR ligand polypharmacol.
Scientific Reports published new progress about 6217-54-5. 6217-54-5 belongs to catalysis-chemistry, auxiliary class Alkenyl,Carboxylic acid,Aliphatic hydrocarbon chain,Metabolic Enzyme,RAR/RXR,Natural product, name is Docosahexaenoic Acid, and the molecular formula is C22H32O2, Computed Properties of 6217-54-5.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia