AI Article Synopsis
- - We created new PPARdelta antagonists by studying the crystal structure of the PPARdelta full agonist TIPP-204 and applying our theory about how helix 12 in nuclear receptors folds.
- - Our research focuses on adjusting the chemical structure to target PPARdelta more effectively.
- - The compound identified as 3a specifically shows strong antagonistic activity only towards PPARdelta.
Article Abstract
We designed and synthesized novel PPARdelta antagonists based on the crystal structure of the PPARdelta full agonist TIPP-204 bound to the PPARdelta ligand-binding domain, in combination with our nuclear receptor helix 12 folding modification hypothesis. Representative compound 3a exhibits PPARdelta-preferential antagonistic activity.
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| http://dx.doi.org/10.1016/j.bmcl.2009.10.021 | DOI Listing |
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Article Synopsis
- - We created new PPARdelta antagonists by studying the crystal structure of the PPARdelta full agonist TIPP-204 and applying our theory about how helix 12 in nuclear receptors folds.
- - Our research focuses on adjusting the chemical structure to target PPARdelta more effectively.
- - The compound identified as 3a specifically shows strong antagonistic activity only towards PPARdelta.
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