Journal of Medicinal Chemistry · 2006 · 131 citations · 8 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryStructure-activity RelationshipsLead Compound DesignLigand BindingLigand-based DesignNatural Product Drug DiscoveryReceptor PharmacologyReceptor-ligand InteractionsBinding Mode AnalysisBinding Mode OptimizationBinding Mode PredictionCocrystal FormationPeroxisome Proliferator-activated Receptor Gamma AgonismPeroxisome Proliferator-activated Receptor SignalingPeroxisome Proliferator-activated ReceptorsX-ray Structure Determination
Agonists of peroxisome proliferator-activated receptor gamma (PPAR gamma) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR gamma agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition to exhibiting a new binding mode in the X-ray cocrystal structure.
8
Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-γ
Robert T. Nolte, G. Bruce Wisely, Stefan Westin et al. · Nature · 1998 · 1.9K citations
Benzoyl 2-methyl indoles as selective PPARγ modulators
John J. Acton, Regina M. Black, A. Brian Jones et al. · Bioorganic & Medicinal Chemistry Letters · 2004 · 131 citations · Full text