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In direct binding assays, 4-OHT had a\n            <jats:italic>K<\/jats:italic>\n            <jats:sub>d<\/jats:sub>\n            value of 35 nM, and both DES and TAM displaced radiolabeled 4-OHT with\n            <jats:italic>K<\/jats:italic>\n            <jats:sub>i<\/jats:sub>\n            values of 870 nM. In cell-based assays, 4-OHT binding caused a dissociation of the complex between ERR\u03b3 and the steroid receptor coactivator-1, and led to an inhibition of the constitutive transcriptional activity of ERR\u03b3. ERR\u03b1 did not bind 4-OHT, but replacing a single amino acid predicted to be in the ERR\u03b1 ligand-binding pocket with the corresponding ERR\u03b3 residue allowed high-affinity 4-OHT binding. These results demonstrate the existence of high-affinity ligands for the ERR family of orphan receptors, and identify 4-OHT as a molecule that can regulate the transcriptional activity of ERR\u03b3.\n          <\/jats:p>","DOI":"10.1073\/pnas.151244398","type":"journal-article","created":{"date-parts":[[2002,7,26]],"date-time":"2002-07-26T14:34:10Z","timestamp":1027694050000},"page":"8880-8884","update-policy":"https:\/\/doi.org\/10.1073\/pnas.cm10313","source":"Crossref","is-referenced-by-count":227,"title":["4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor \u03b3"],"prefix":"10.1073","volume":"98","author":[{"given":"Peter","family":"Coward","sequence":"first","affiliation":[{"name":"Tularik, Inc., 2 Corporate Drive, South San Francisco, CA 94080"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Doris","family":"Lee","sequence":"additional","affiliation":[{"name":"Tularik, Inc., 2 Corporate Drive, South San Francisco, CA 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