pone.0248034.s002.tif (7.47 MB)
IC50 values for inhibition of human and murine RORγt.
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posted on 2021-11-09, 18:32 authored by Steven A. Saenz, Andrea Local, Tiffany Carr, Arvind Shakya, Shivsmriti Koul, Haiqing Hu, Lisa Chourb, Justin Stedman, Jenna Malley, Laura Akullian D’Agostino, Veerabahu Shanmugasundaram, John Malona, C. Eric Schwartz, Lisa Beebe, Meghan Clements, Ganesh Rajaraman, John Cho, Lan Jiang, Alex Dubrovskiy, Matt Kreilein, Roman Shimanovich, Lawrence G. Hamann, Laure Escoubet, J. Michael EllisConcentrations of the RORγt inhibitors, Compound 1, Compound 2 or Compound 3, in which 50% (IC50) relative light units (RLUs) was inhibited. Assays utilized reporter cells (HEK293) harboring a receptor hybrid in which the native N-terminal DNA binding domain (DBD) has been replaced with that of the yeast Gal4 DBD, with a firefly luciferase reporter gene functionally linked to a Gal4 upstream activation sequence.
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retinoic acid receptorpancreatic ductal adenocarcinomadiv >< pattractive therapeutic targetassociated gene expressionnumerous autoimmune diseasesdelay tumor volumeinhibit th17 differentiationinhibit tumor formationrorγt block th17tumor formationautoimmune disorderstumor growthtumor effectsth17 cellsvivo vitro transcription factorsrorγt inhibitorsrorγt functionsprimary functionpreclinical modelsimmune responsesdependent mannercritical regulator17a production
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