title: Regulation of p53 stability and apoptosis by a ROR agonist.
abstract: Activation of p53 function leading to cell-cycle arrest and/or apoptosis is a promising strategy for development of anti-cancer therapeutic agents. Here, we describe a novel mechanism for stabilization of p53 protein expression via activation of the orphan nuclear receptor, RORα. We demonstrate that treatment of cancer cells with a newly described synthetic ROR agonist, SR1078, leads to p53 stabilization and induction of apoptosis. These data suggest that synthetic ROR agonists may hold utility in the treatment of cancer.
authors.affiliation: The Scripps Research Institute, Jupiter, Florida, United States of America.
authors.forename: Yongjun
authors.initials: Y
authors.lastname: Wang
authors.forename: Laura A
authors.initials: LA
authors.lastname: Solt
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: Kojetin
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Burris
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001549:Benzamides / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects*; D056945:Hep G2 Cells; D006801:Humans; D057094:Nuclear Receptor Subfamily 1, Group F, Member 1 / Q000819:agonists* / Q000378:metabolism*; D055751:SOXC Transcription Factors / Q000235:genetics / Q000378:metabolism; D016159:Tumor Suppressor Protein p53 / Q000235:genetics / Q000378:metabolism*; D005466:Fluorocarbons
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D057094:Nuclear Receptor Subfamily 1, Group F, Member 1; D055751:SOXC Transcription Factors; D016159:Tumor Suppressor Protein p53; C539738:RORA protein, human; C083431:SOX4 protein, human; C559087:SR 1078; D005466:Fluorocarbons