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New publication in International Journal for Parasitology: Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned

30 abr 2020 - 15:19 CET

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. Kempf, Robert K.M. Choy, Eugenio L. de Hostos, Dustin J. Maly, Erkang Fan, Kayode K. Ojo, Wesley C. Van Voorhis.

 

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.

Highlights

  • BKIs that target CDPK1 in apicomplexan parasites with a glycine gatekeeper are promising new therapeutics.
  • Numerous challenges have shaped our selection of pre-clinical BKI candidates.
  • These include chirality, hERG, teratogenicity, cardiovascular, GI, and toxicity issues, and poor efficacy due to PK/PD.
New publication in International Journal for Parasitology: Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned - 1

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