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Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-11-04 , DOI: 10.1016/j.bmcl.2017.11.006
Bharat Lagu , Arthur F. Kluge , Matthew M. Goddeeris , Effie Tozzo , Ross A. Fredenburg , Shekar Chellur , Ramesh S. Senaiar , Mahaboobi Jaleel , D. Ravi Krishna Babu , Nirbhay K. Tiwari , Taisuke Takahashi , Michael A. Patane

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.



中文翻译:

与GW501516相比,高选择性过氧化物酶体增殖物激活受体δ(PPARδ)调节剂显示出改善的安全性

与PPARδ调节剂GW501516相比,化合物1调节的基因明显少得多。两种化合物在肌肉再生的热损伤模型中都是有效的。相对于GW501516而言,受限制的1个基因图谱表明1可能与GW501516在药理上等效,而与PPAR相关的安全性问题较少。

更新日期:2017-11-04
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