Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonists
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Acknowledgments
We thank Grégoire Mouis and Michèle Aurelly for analytical support.
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2020, Journal of Biological ChemistryCitation Excerpt :Whereas other amino acids that delineate the allosteric pocket can be replaced for those with other side chains, modifications to these two elements are detrimental. Thus, the results of this study strongly bring forward that the allosteric pocket, as present in RORγt and receptive to MRL-871 and other ligands (16, 27–30, 37), is highly unique to RORγt within the NR superfamily. This implies that RORγt is the only NR capable of forming this specific type of allosteric pocket, which is also supported by a commercially available panel of cell-based NR reporter assays against which an MRL-871 analog was tested (16).
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