Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516. Issue 3 (1st February 2018)

• Record Type: Journal Article
• Authors: Lagu, Bharat; Kluge, Arthur F.; Goddeeris, Matthew M.; Tozzo, Effie; Fredenburg, Ross A.; Chellur, Shekar; Senaiar, Ramesh S.; Jaleel, Mahaboobi; Babu, D. Ravi Krishna; Tiwari, Nirbhay K.; Takahashi, Taisuke; Patane, Michael A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 3(2018)
• Page Start: 533
• Page End: 536
• Publication Date: 2018-02-01
• Subjects: PPARδ modulator -- GW501516 -- Gene expression -- Thermal injury model -- Ki-67; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.11.006
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Comparison of gene regulation profiles, efficacy in thermal injury model and 14-day rat toxicity studies. Abstract: Compound 1 regulates significantly fewer genes than the PPARδ modulator, GW501516. Both compounds are efficacious in a thermal injury model of muscle regeneration. The restricted gene profile of 1 relative to GW501516 suggests that 1 may be pharmacoequivalent to GW501516 with fewer PPAR-related safety concerns.