Extended-spectrum antiprotozoal bumped kinase inhibitors: A review

Wesley C. Van Voorhis, J. Stone Doggett, Marilyn Parsons, Matthew A. Hulverson, Ryan Choi, Samuel L.M. Arnold, Michael W. Riggs, Andrew Hemphill, Daniel K. Howe, Robert H. Mealey, Audrey O.T. Lau, Ethan A. Merritt, Dustin J. Maly, Erkang Fan, Kayode K. Ojo

Research output: Contribution to journalArticlepeer-review

41 Scopus citations


Many life-cycle processes in parasites are regulated by protein phosphorylation. Hence, disruption of essential protein kinase function has been explored for therapy of parasitic diseases. However, the difficulty of inhibiting parasite protein kinases to the exclusion of host orthologues poses a practical challenge. A possible path around this difficulty is the use of bumped kinase inhibitors for targeting calcium-dependent protein kinases that contain atypically small gatekeeper residues and are crucial for pathogenic apicomplexan parasites' survival and proliferation. In this article, we review efficacy against the kinase target, parasite growth in vitro, and in animal infection models, as well as the relevant pharmacokinetic and safety parameters of bumped kinase inhibitors.

Original languageEnglish
Pages (from-to)71-83
Number of pages13
JournalExperimental Parasitology
StatePublished - Sep 2017

Bibliographical note

Funding Information:
This work was supported by the US National Institutes of Health (NICHHD R01HD080670 & NIAID R01AI111341, R01AI089441) and the USDA (2014-06183). This work was also supported by Swiss National Science Foundation (grant No. 310030_165782) and in part by Career Development Award # BX002440 to J. Stone Doggett from the United States Department of Veterans Affairs Biomedical Laboratory Research and Development.

Publisher Copyright:
© 2017 Elsevier Inc.


  • Bumped kinase inhibitors
  • Calcium-dependent protein kinase
  • Gatekeeper residue

ASJC Scopus subject areas

  • Parasitology
  • Immunology
  • Infectious Diseases


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