Modulation of Transcription Mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the Presence of GW0742 Analogs | Zendy

Kelly A. Teske | Zendy; Premchendar Nandhikonda | Zendy; Jonathan W. Bogart | Zendy; Belaynesh Feleke | Zendy; Preetpal S. Sidhu | Zendy; Nina Y. Yuan | Zendy; Joshua Preston | Zendy; Robin Goy | Zendy; Leggy A. Arnold | Zendy

Open Access

Modulation of Transcription Mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the Presence of GW0742 Analogs

Author(s) -

Kelly A. Teske,

Premchendar Nandhikonda,

Jonathan W. Bogart,

Belaynesh Feleke,

Preetpal S. Sidhu,

Nina Y. Yuan,

Joshua Preston,

Robin Goy,

Leggy A. Arnold

Publication year - 2014

Publication title -

journal of biomolecular research and therapeutics

Language(s) - English

Resource type - Journals

ISSN - 2167-7956

DOI - 10.4172/2167-7956.1000111

Subject(s) - calcitriol receptor , peroxisome proliferator activated receptor , chemistry , receptor , nuclear receptor , peroxisome proliferator activated receptor delta , carboxylic acid , transcription factor , alcohol , peroxisome , biochemistry , pharmacology , biology , gene

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.

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