The invented substances have been characterized with regard to the inhibition of the cPLA2 (IC50 in the submicromolar range) and metabolic stability (tested in rat liver homogenates). The inventors are currently conducting such experiments with further, newly generated derivatives of the same inhibitor family.
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Dennis EA, Cao J, Hsu YH, Magrioti V, Kokotos G. Phospholipase A2 enzymes: Physical structure, biological function, disease implication, chemical inhibition and therapeutic invention. Chem. Rev. 2011; 111: 6130-85.
Ghomashchi F, et al. Interfacial kinetic and binding properties of mammalian group IVB phospholipase A2 (cPLA2) and comparison with other cPLA2 isoforms. J. Biol. Chem. 2010; 285: 36100-11.