Matches in SemOpenAlex for { <https://semopenalex.org/work/W2991119006> ?p ?o ?g. }
- W2991119006 endingPage "370" @default.
- W2991119006 startingPage "365" @default.
- W2991119006 abstract "As regulators of steroidogenesis, development, and metabolism, the nuclear receptor 5A (NR5A) subfamily members steroidogenic factor 1 (SF-1) and liver receptor homologue 1 (LRH-1) are important pharmacological targets for cancers and metabolic diseases. Evaluation of small molecule modulators and candidate endogenous ligands for these orphan receptors has been hindered by the lack of accessible, robust direct-binding assays. Here, we leverage the potency of our new NR5A agonist (6N) to create a high-affinity probe for fluorescence polarization competition assays by conjugating 6N to fluorescein (FAM). The 6N-FAM probe tightly binds the NR5A receptors and detects direct binding of synthetic and phospholipid ligands. For 25 LRH-1 agonists, affinity predicts potency in cellular activation assays, demonstrating the potential for this assay in drug discovery. Moreover, phospholipids dilauroylphosphatidylcholine and phosphatidylinositol(4,5)phosphate bind with high affinity, demonstrating this assay is robust for evaluation of candidate endogenous ligands for human NR5A receptors." @default.
- W2991119006 created "2019-12-05" @default.
- W2991119006 creator A5010173597 @default.
- W2991119006 creator A5037444457 @default.
- W2991119006 creator A5038371942 @default.
- W2991119006 creator A5041989549 @default.
- W2991119006 creator A5042255159 @default.
- W2991119006 creator A5042492247 @default.
- W2991119006 creator A5048282260 @default.
- W2991119006 date "2019-11-21" @default.
- W2991119006 modified "2023-10-15" @default.
- W2991119006 title "Development of a Versatile and Sensitive Direct Ligand Binding Assay for Human NR5A Nuclear Receptors" @default.
- W2991119006 cites W1480848352 @default.
- W2991119006 cites W1804706871 @default.
- W2991119006 cites W1980102934 @default.
- W2991119006 cites W1982167352 @default.
- W2991119006 cites W1997876636 @default.
- W2991119006 cites W1998524704 @default.
- W2991119006 cites W2004490930 @default.
- W2991119006 cites W2009639026 @default.
- W2991119006 cites W2022560804 @default.
- W2991119006 cites W2024955650 @default.
- W2991119006 cites W2029335938 @default.
- W2991119006 cites W2033997896 @default.
- W2991119006 cites W2045519188 @default.
- W2991119006 cites W2068458442 @default.
- W2991119006 cites W2069221705 @default.
- W2991119006 cites W2082125652 @default.
- W2991119006 cites W2083234724 @default.
- W2991119006 cites W2096942972 @default.
- W2991119006 cites W2105603179 @default.
- W2991119006 cites W2108306880 @default.
- W2991119006 cites W2111684219 @default.
- W2991119006 cites W2111904970 @default.
- W2991119006 cites W2121435438 @default.
- W2991119006 cites W2121916956 @default.
- W2991119006 cites W2134218333 @default.
- W2991119006 cites W2152741970 @default.
- W2991119006 cites W2157309735 @default.
- W2991119006 cites W2166368797 @default.
- W2991119006 cites W2169480215 @default.
- W2991119006 cites W2169768051 @default.
- W2991119006 cites W2476309440 @default.
- W2991119006 cites W2557326422 @default.
- W2991119006 cites W2792582775 @default.
- W2991119006 cites W2811217496 @default.
- W2991119006 cites W2891588020 @default.
- W2991119006 cites W2967243590 @default.
- W2991119006 doi "https://doi.org/10.1021/acsmedchemlett.9b00442" @default.
- W2991119006 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7074214" @default.
- W2991119006 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32184971" @default.
- W2991119006 hasPublicationYear "2019" @default.
- W2991119006 type Work @default.
- W2991119006 sameAs 2991119006 @default.
- W2991119006 citedByCount "11" @default.
- W2991119006 countsByYear W29911190062020 @default.
- W2991119006 countsByYear W29911190062021 @default.
- W2991119006 countsByYear W29911190062022 @default.
- W2991119006 countsByYear W29911190062023 @default.
- W2991119006 crossrefType "journal-article" @default.
- W2991119006 hasAuthorship W2991119006A5010173597 @default.
- W2991119006 hasAuthorship W2991119006A5037444457 @default.
- W2991119006 hasAuthorship W2991119006A5038371942 @default.
- W2991119006 hasAuthorship W2991119006A5041989549 @default.
- W2991119006 hasAuthorship W2991119006A5042255159 @default.
- W2991119006 hasAuthorship W2991119006A5042492247 @default.
- W2991119006 hasAuthorship W2991119006A5048282260 @default.
- W2991119006 hasBestOaLocation W29911190062 @default.
- W2991119006 hasConcept C104317684 @default.
- W2991119006 hasConcept C107824862 @default.
- W2991119006 hasConcept C135285700 @default.
- W2991119006 hasConcept C170493617 @default.
- W2991119006 hasConcept C185592680 @default.
- W2991119006 hasConcept C2778938600 @default.
- W2991119006 hasConcept C55493867 @default.
- W2991119006 hasConcept C63932345 @default.
- W2991119006 hasConcept C74187038 @default.
- W2991119006 hasConcept C86339819 @default.
- W2991119006 hasConcept C86803240 @default.
- W2991119006 hasConcept C95444343 @default.
- W2991119006 hasConceptScore W2991119006C104317684 @default.
- W2991119006 hasConceptScore W2991119006C107824862 @default.
- W2991119006 hasConceptScore W2991119006C135285700 @default.
- W2991119006 hasConceptScore W2991119006C170493617 @default.
- W2991119006 hasConceptScore W2991119006C185592680 @default.
- W2991119006 hasConceptScore W2991119006C2778938600 @default.
- W2991119006 hasConceptScore W2991119006C55493867 @default.
- W2991119006 hasConceptScore W2991119006C63932345 @default.
- W2991119006 hasConceptScore W2991119006C74187038 @default.
- W2991119006 hasConceptScore W2991119006C86339819 @default.
- W2991119006 hasConceptScore W2991119006C86803240 @default.
- W2991119006 hasConceptScore W2991119006C95444343 @default.
- W2991119006 hasFunder F4320309381 @default.
- W2991119006 hasFunder F4320337357 @default.
- W2991119006 hasFunder F4320337368 @default.
- W2991119006 hasIssue "3" @default.
- W2991119006 hasLocation W29911190061 @default.
- W2991119006 hasLocation W29911190062 @default.