title: Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs.
abstract: Herein we describe the evaluation of GW0742 analogs in respect to their ability to modulate transcription mediated by the vitamin D receptor (VDR) and the peroxisome proliferator activated receptor (PPAR) δ. The GW0742 analog bearing a carboxylic ester functionality in place of the carboxylic acid was partially activating both nuclear receptors at low concentration and inhibited transcription at higher compound concentrations. The GW0742 alcohol derivative was more active than the ester in respect to VDR but less active in regard to PPARδ. Importantly, the alcohol derivative was significantly more toxic than the corresponding acid and ester.
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Kelly
authors.initials: K
authors.lastname: Teske
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Premchendar
authors.initials: P
authors.lastname: Nandhikonda
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Jonathan W
authors.initials: JW
authors.lastname: Bogart
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Belaynesh
authors.initials: B
authors.lastname: Feleke
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Preetpal
authors.initials: P
authors.lastname: Sidhu
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Nina
authors.initials: N
authors.lastname: Yuan
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Joshua
authors.initials: J
authors.lastname: Preston
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Robin
authors.initials: R
authors.lastname: Goy
authors.affiliation: Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA.
authors.forename: Leggy A
authors.initials: LA
authors.lastname: Arnold