Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned


International Journal for Parasitology


Ryan Choi, Matthew A. Hulverson, Wenlin Huang, Rama S.R. Vidadala, Grant R.Whitman, Lynn K.Barrett, Deborah A. Schaefer, Dana P.Betzer, Michael W. Riggs, J. Stone Doggett, Andrew Hemphill, Luis Miguel Ortega-Morag Molly C. McCloskey, Samuel L.M. Arnold, Robert C.Hackmanhi, Kennan C.Marsh, James J. Lynch, Gail M. Freiberg, Bruce E. Leroy, Dale J.Kempf, Robert K.M.Choy, Eugenio L .de Hostos, Dustin J.Maly, Erkang Fan, Kayode K. Ojo, Wesley C. Van Voorhis



Bumped Kinase Inhibitors, targeting Calcium-dependent Protein Kinase 1 in apicomplexan parasites with a glycine gatekeeper, are promising new therapeutics for apicomplexan diseases. Here we will review advances, as well as challenges and lessons learned regarding efficacy, safety, and pharmacology that have shaped our selection of pre-clinical candidates.

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