[P2.037] Synthesis and in vitro evaluation of magnolol based dimeric compounds as PPARγ agonists
نویسندگان
چکیده
Partial agonism is hypothesized to reduce these side effects. Recently, three different neolignans (dieugenol, tetrahydrodieugenol and magnolol) were found to be PPARγ partial agonists. Within this project we sought to optimize magnolol as a PPARγ ligand. Preliminary molecular dockings studies and the crystal structure of PPARγ with magnolol revealed that two molecules of magnolol bind to the active binding site of the receptor simultaneously.
منابع مشابه
Identification of PPARgamma Partial Agonists of Natural Origin (I): Development of a Virtual Screening Procedure and In Vitro Validation
BACKGROUND Although there are successful examples of the discovery of new PPARγ agonists, it has recently been of great interest to identify new PPARγ partial agonists that do not present the adverse side effects caused by PPARγ full agonists. Consequently, the goal of this work was to design, apply and validate a virtual screening workflow to identify novel PPARγ partial agonists among natural...
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