Details

Autor(en) / Beteiligte

• Shearer, Barry G
• Wiethe, Robert W
• Ashe, Adam
• Billin, Andrew N
• Way, James M
• Stanley, Thomas B
• Wagner, Craig D
• Xu, Robert X
• Leesnitzer, Lisa M
• Merrihew, Raymond V
• Shearer, Todd W
• Jeune, Michael R
• Ulrich, John C
• Willson, Timothy M

Titel

Identification and Characterization of 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a Selective and Irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) Antagonist

Ist Teil von

• Journal of medicinal chemistry, 2010-02, Vol.53 (4), p.1857-1861

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2010

Quelle

MEDLINE

Beschreibungen/Notizen

• 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide 3 (GSK3787) was identified as a potent and selective ligand for PPARδ with good pharmacokinetic properties. A detailed binding study using mass spectral analysis confirmed covalent binding to Cys249 within the PPARδ binding pocket. Gene expression studies showed that pyridylsulfone 3 antagonized the transcriptional activity of PPARδ and inhibited basal CPT1a gene transcription. Compound 3 is a PPARδ antagonist with utility as a tool to elucidate PPARδ cell biology and pharmacology.