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

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-Mora, Molly C. McCloskey, Samuel L.M. Arnold, Robert C. Hackman, Kennan C. Marsh, James J. Lynch, Gail M. Freiberg, Bruce E. Leroy, Dale J. KempfRobert K.M. Choy, Eugenio L. de Hostos, Dustin J. Maly, Erkang Fan, Kayode K. Ojo, Wesley C. Van Voorhis

Research output: Contribution to journalReview article

1 Scopus citations

Abstract

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.

Original languageEnglish (US)
JournalInternational Journal for Parasitology
DOIs
StateAccepted/In press - Jan 1 2020

Keywords

  • Apicomplexa
  • Bumped Kinase Inhibitor
  • Calcium-dependent Protein Kinases
  • Cryptosporidium
  • Gatekeeper
  • Neospora
  • Sarcocystis
  • Toxoplasma

ASJC Scopus subject areas

  • Parasitology
  • Infectious Diseases

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    Choi, R., Hulverson, M. A., Huang, W., Vidadala, R. S. R., Whitman, G. R., Barrett, L. K., Schaefer, D. A., Betzer, D. P., Riggs, M. W., Doggett, J. S., Hemphill, A., Ortega-Mora, L. M., McCloskey, M. C., Arnold, S. L. M., Hackman, R. C., Marsh, K. C., Lynch, J. J., Freiberg, G. M., Leroy, B. E., ... Van Voorhis, W. C. (Accepted/In press). Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned. International Journal for Parasitology. https://doi.org/10.1016/j.ijpara.2020.01.006