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- Publisher
- Wiley
- Copyright
- Copyright © 2008 Wiley Subscription Services
- ISSN
- 1860-7179
- eISSN
- 1860-7187
- DOI
- 10.1002/cmdc.200800193
- pmid
- 18924220
- Publisher site
- See Article on Publisher Site
Abstract
Phenylpropanoic acid‐derived PPAR agonist TIPP‐204, shows high selectivity for human (h)PPARδ while structurally related TIPP‐401 is a hPPARα/δ dual agonist. Computational docking of TIPP‐401 in the ligand binding domain (LBD) of hPPARα and hPPARδ, and inspection of the TIPP‐204–hPPARδ LBD co‐crystal structure identified key amino acids responsible for the differences in selectivity of the two analogues. These results were confirmed using mutagenesis assays. The amino acids determining the potency and selectivity of TIPP‐204 are different to those of the PPARδ‐ selective agonist GW‐501516, which belongs to a different chemical class.
Journal
ChemMedChem – Wiley
Published: Jan 17, 2008
Keywords: ; ; ; ;