| http://purl.uniprot.org/citations/15056000 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/15056000 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/15056000 | http://www.w3.org/2000/01/rdf-schema#comment | "A series of tetrahydrobenzofuranyl and tetrahydrobenzothienyl propenoic acids that showed potent agonist activity against RXRalpha were synthesized via a structure-based design approach. Among the compounds studied, 46a,b showed not only very good potency against RXRalpha (K(i) = 6 nM) but was also found to be greater than 167-fold selective vs RARalpha (K(i) > 1000 nM). This compound profiled out as a full agonist in a cell-based transient transfection assay (EC(50) = 3 nM). The two antipodes were separated via chiral chromatography, and 46b was found to be 40-fold more potent than 46a. Interestingly, cocrystallization of 46a,b with the RXRalpha protein generated a liganded structure whereby the (S)-antipode was found in the binding pocket. Given orally in db/db mice or ZDF rats, 46a,b showed a significant glucose-lowering effect and an increase in liver mass. Triglycerides decreased significantly in db/db mice but increased in the ZDF rats. A dose-dependent decrease of nonesterified free fatty acids was seen in ZDF rats but not in db/db mice. These differences indicate a species specific effect of RXR agonists on lipid metabolism."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm030565g"xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm030565g"xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Blanchard S."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Blanchard S."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Xu H.E."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Xu H.E."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Miller A.B."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Miller A.B."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Consler T.G."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Consler T.G."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Lenhard J.M."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Lenhard J.M."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Gampe R.T. Jr."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Gampe R.T. Jr."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Bledsoe R.K."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Bledsoe R.K."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Montana V.G."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Montana V.G."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Haffner C.D."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Haffner C.D."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Ayscue A."xsd:string |
| http://purl.uniprot.org/citations/15056000 | http://purl.uniprot.org/core/author | "Ayscue A."xsd:string |