Bazhin, Arkadiy A.Chambon, MarcVesin, JonathanBortoli, JulienCollins, James W.Turcatti, GerardoChou, Chieh JasonGoun, Elena A.2019-01-232019-01-232019-01-232019-01-0110.1021/acs.analchem.8b04672https://infoscience.epfl.ch/handle/20.500.14299/153933WOS:000455076400086Aminopeptidases, 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 amino-peptidase 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.Chemistry, AnalyticalChemistrybioluminescent assaysensitive detectionprotease activityivinhibitorleukemiatext::journal::journal article::research article