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Anal Chem. 2018 Dec 4. doi: 10.1021/acs.analchem.8b04672. [Epub ahead of print]

A UNIVERSAL ASSAY FOR AMINOPEPTIDASE ACTIVITY AND ITS APPLICATION FOR DIPEPTIDYL PEPTIDASE-4 DRUG DISCOVERY.

Abstract

Aminopeptidases, such as dipeptidyl peptidase-4 (DPP-4, CD26), are potent therapeutic targets for pharmacological interventions because they play key roles in many important pathological pathways. To analyze aminopeptidase activity in vitro (including high throughput screening [HTS]), in vivo, and ex vivo, we developed a highly sensitive and quantitative bioluminescence-based readout method. We successfully applied this method to screening drugs with potential DPP-4 inhibitory activity. Using this method, we found that cancer drug mitoxantrone possesses significant DPP-4 inhibitory activity both in vitro and in vivo. The pharmacophore of mitoxantrone was further investigated by testing a variety of its structural analogues.

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