Development of novel activity assay for GCPII/GCPIII based on fluorescence anisotropy that, in turn, will be exploited for the identification of novel inhibitor scaffolds targeting GCPII/GCPIII. Identification of novel GCPII/GCPIII inhibitors using in silico and in vitro testing. Structure-based modifications of novel as well as existing GCPII/GCPIII inhibitors to simplify synthesis, improve their pharmacokinetic properties and/or increase liphophilicity and/or affinity. Biochemical and physiological characterization of optimized and newly identified GCPII/GCPIII inhibitors. (en)
Vývoj nového aktivitního stanovení využitelného k identifikaci a optimalizaci inhibitorů GCPII a GCPIII. Optimalizace inhibitorů uvedených enzymů s využitím rentgenostrukturní analýzy. (cs)