http://purl.uniprot.org/citations/21391689 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/21391689 | http://www.w3.org/2000/01/rdf-schema#comment | "The crystal structure of LRH-1 ligand binding domain bound to our previously reported agonist 3-(E-oct-4-en-4-yl)-1-phenylamino-2-phenyl-cis-bicyclo[3.3.0]oct-2-ene 5 is described. Two new classes of agonists in which the bridgehead anilino group from our first series was replaced with an alkoxy or 1-ethenyl group were designed, synthesized, and tested for activity in a peptide recruitment assay. Both new classes gave very active compounds, particularly against SF-1. Structure-activity studies led to excellent dual-LRH-1/SF-1 agonists (e.g., RJW100) as well as compounds selective for LRH-1 (RJW101) and SF-1 (RJW102 and RJW103). The series based on 1-ethenyl substitution was acid stable, overcoming a significant drawback of our original bridgehead anilino-substituted series. Initial studies on the regulation of gene expression in human cell lines showed excellent, reproducible activity at endogenous target genes."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm1014296"xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Cai F."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Xu R."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Williams S.P."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Willson T.M."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Dixon S."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Orband-Miller L.A."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Zuercher W.J."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Blind R.D."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Ingraham H.A."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Leesnitzer L.M."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Stec J."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/author | "Whitby R.J."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/date | "2011"xsd:gYear |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/name | "J Med Chem"xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/pages | "2266-2281"xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/title | "Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2)."xsd:string |
http://purl.uniprot.org/citations/21391689 | http://purl.uniprot.org/core/volume | "54"xsd:string |
http://purl.uniprot.org/citations/21391689 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/21391689 |
http://purl.uniprot.org/citations/21391689 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/21391689 |
http://purl.uniprot.org/uniprot/#_Q15596-mappedCitation-21391689 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/21391689 |
http://purl.uniprot.org/uniprot/#_O00482-mappedCitation-21391689 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/21391689 |
http://purl.uniprot.org/uniprot/Q15596 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/21391689 |