2 research outputs found
Investigating Polypharmacology through Targeting Known Human Neutrophil Elastase Inhibitors to Proteinase 3
Using a combination of multisite 位鈭抎ynamics
(MS位D)
together with in vitro IC50 assays, we
evaluated the polypharmacological potential of a scaffold currently
in clinical trials for inhibition of human neutrophil elastase (HNE),
targeting cardiopulmonary disease, for efficacious inhibition of Proteinase
3 (PR3), a related neutrophil serine proteinase. The affinities we
observe suggest that the dihydropyrimidinone scaffold can serve as
a suitable starting point for the establishment of polypharmacologically
targeting both enzymes and enhancing the potential for treatments
addressing diseases like chronic obstructive pulmonary disease
Investigating Polypharmacology through Targeting Known Human Neutrophil Elastase Inhibitors to Proteinase 3
Using a combination of multisite 位鈭抎ynamics
(MS位D)
together with in vitro IC50 assays, we
evaluated the polypharmacological potential of a scaffold currently
in clinical trials for inhibition of human neutrophil elastase (HNE),
targeting cardiopulmonary disease, for efficacious inhibition of Proteinase
3 (PR3), a related neutrophil serine proteinase. The affinities we
observe suggest that the dihydropyrimidinone scaffold can serve as
a suitable starting point for the establishment of polypharmacologically
targeting both enzymes and enhancing the potential for treatments
addressing diseases like chronic obstructive pulmonary disease