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We reported that a nonsteroidal compound, CpdX, selectively activates the tethered transrepression function of the glucocorticoid receptor (GR), which contributes to the glucocorticoid beneficial antiinflammatory properties, while not inducing the GR-mediated direct transactivation nor the direct transrepression to which GC undesirable side effects are attributed. We now demonstrate that both CpdX and its deuterated form CpdX-D3 selectively trigger GR-mediated tethered transrepression, and are as efficient as the synthetic glucocorticoid Dexamethasone at curing several major inflammatory diseases in the mouse, indicating that they could be of great interest as antiinflammatory drugs.<\/jats:p>","DOI":"10.1073\/pnas.1908258116","type":"journal-article","created":{"date-parts":[[2019,6,21]],"date-time":"2019-06-21T20:06:31Z","timestamp":1561147591000},"page":"14191-14199","update-policy":"https:\/\/doi.org\/10.1073\/pnas.cm10313","source":"Crossref","is-referenced-by-count":12,"title":["Glucocorticoid receptor modulators CpdX and CpdX-D3 exhibit the same in vivo antiinflammatory activities as synthetic glucocorticoids"],"prefix":"10.1073","volume":"116","author":[{"given":"Guoqiang","family":"Hua","sequence":"first","affiliation":[{"name":"Institut de G\u00e9n\u00e9tique et de Biologie Mol\u00e9culaire et Cellulaire (IGBMC), CNRS UMR7104, INSERM U1258, 67404 Illkirch, France;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Naimah","family":"Zein","sequence":"additional","affiliation":[{"name":"Institut de G\u00e9n\u00e9tique et de Biologie Mol\u00e9culaire et Cellulaire (IGBMC), CNRS UMR7104, INSERM U1258, 67404 Illkirch, France;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fran\u00e7ois","family":"Daubeuf","sequence":"additional","affiliation":[{"name":"Laboratoire d\u2019Innovation Th\u00e9rapeutique, Unit\u00e9 Mixte de Recherche 7200, Facult\u00e9 de Pharmacie, Centre National de la Recherche Scientifique-Universit\u00e9 de Strasbourg, F-67400 Illkirch, France;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7861-6046","authenticated-orcid":false,"given":"Pierre","family":"Chambon","sequence":"additional","affiliation":[{"name":"Institut de G\u00e9n\u00e9tique et de Biologie Mol\u00e9culaire et Cellulaire (IGBMC), CNRS UMR7104, INSERM U1258, 67404 Illkirch, France;"},{"name":"University of Strasbourg Institute for Advanced Study, 67404 Illkirch, France;"},{"name":"Coll\u00e8ge de France, 67404 Illkirch, France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"341","published-online":{"date-parts":[[2019,6,21]]},"reference":[{"key":"e_1_3_3_1_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.pharmthera.2011.12.004"},{"key":"e_1_3_3_2_2","doi-asserted-by":"publisher","DOI":"10.1126\/science.1164265"},{"key":"e_1_3_3_3_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2011.03.027"},{"key":"e_1_3_3_4_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.mce.2012.12.014"},{"key":"e_1_3_3_5_2","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.1524215113"},{"key":"e_1_3_3_6_2","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.1522821113"},{"key":"e_1_3_3_7_2","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.1522826113"},{"key":"e_1_3_3_8_2","doi-asserted-by":"publisher","DOI":"10.1021\/jm050345y"},{"key":"e_1_3_3_9_2","unstructured":"M. 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