Modulation of Transcription Mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor ÃÂ´ in the Presence of GW0742 AnalogsKelly Teske, Premchendar Nandhikonda, Jonathan W Bogart, Belaynesh Feleke, Preetpal Sidhu, Nina Yuan, Joshua Preston, Robin Goy and Leggy A Arnold*
Department of Chemistry and Biochemistry, University of Wisconsin-Milwaukee, WI 53211, USA
- *Corresponding Author:
- Leggy A Arnold
Department of Chemistry and Biochemistry
University of Wisconsin-Milwaukee, WI 53211, USA
E-mail: [email protected]
Received date: December 05, 2013; Accepted date: February 04, 2014; Published date: February 10, 2014
Citation: Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, et al. (2014) Modulation of Transcription Mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor d in the Presence of GW0742 Analogs. J Biomol Res Ther 3:111. doi: 10.4172/2167-7956.1000111
Copyright: © 2014 Teske K, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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 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.