Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516

Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516

Comparison of gene regulation profiles, efficacy in thermal injury model and 14-day rat toxicity studies. [Display omitted] Compound 1 regulates significantly fewer genes than the PPARδ modulator, GW501516. Both compounds are efficacious in a thermal injury model of muscle regeneration. The restrict...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2018-02, Vol.28 (3), p.533-536
Hauptverfasser: 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.
Format: Artikel
Sprache:eng
Schlagworte:
Gene expression
GW501516
Ki-67
PPARδ modulator
Thermal injury model
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Comparison of gene regulation profiles, efficacy in thermal injury model and 14-day rat toxicity studies. [Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2017.11.006