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Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516.
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.
Bioorg Med Chem Lett ; 28(3): 533-536, 2018 02 01.
Article in English | MEDLINE | ID: mdl-29275935

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.


Subject(s)
PPAR delta/metabolism , Thiazoles/pharmacology , Animals , Cell Proliferation/drug effects , Disease Models, Animal , Dose-Response Relationship, Drug , Humans , Mice , Molecular Structure , Rats , Structure-Activity Relationship
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