@article{8602b641d6fd47e795cef6ec4dcfd404,
title = "Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis",
abstract = "Improvements have been made to the safety and efficacy of bumped kinase inhibitors, and they are advancing toward human and animal use for treatment of cryptosporidiosis. As the understanding of bumped kinase inhibitor pharmacodynamics for cryptosporidiosis therapy has increased, it has become clear that better compounds for efficacy do not necessarily require substantial systemic exposure. We now have a bumped kinase inhibitor with reduced systemic exposure, acceptable safety parameters, and efficacy in both the mouse and newborn calf models of cryptosporidiosis. Potential cardiotoxicity is the limiting safety parameter to monitor for this bumped kinase inhibitor. This compound is a promising pre-clinical lead for cryptosporidiosis therapy in animals and humans.",
keywords = "BKI 1369, Calcium-dependent protein kinase 1, Cryptosporidiosis, Drug target, Gatekeeper residue",
author = "Hulverson, {Matthew A.} and Ryan Choi and Arnold, {Samuel L.M.} and Schaefer, {Deborah A.} and Andrew Hemphill and McCloskey, {Molly C.} and Betzer, {Dana P.} and Joachim M{\"u}ller and Vidadala, {Rama S.R.} and Whitman, {Grant R.} and Rivas, {Kasey L.} and Barrett, {Lynn K.} and Hackman, {Robert C.} and Love, {Melissa S.} and McNamara, {Case W.} and Shaughnessy, {Thomas K.} and Alison Kondratiuk and Matthew Kurnick and Banfor, {Patricia N.} and Lynch, {James J.} and Freiberg, {Gail M.} and Kempf, {Dale J.} and Maly, {Dustin J.} and Riggs, {Michael W.} and Ojo, {Kayode K.} and {Van Voorhis}, {Wesley C.}",
note = "Funding Information: The authors thank Geno De Hostos and Robert Choy from PATH Drug Solutions (San Francisco, CA, USA) for their consultation in the drug development pathway. Research studies reported in this publication were supported by National Institute of Allergy and Infectious Diseases (NIAID) of the National Institutes of Health (NIH), USA, under award numbers R01AI089441, R01AI111341 and R01HD080670. The work was also supported by award number 2014-06183 from the United States Department of Agriculture National Institute of Food and Agriculture. Publisher Copyright: {\textcopyright} 2017 Australian Society for Parasitology",
year = "2017",
month = oct,
doi = "10.1016/j.ijpara.2017.08.006",
language = "English (US)",
volume = "47",
pages = "753--763",
journal = "International Journal for Parasitology",
issn = "0020-7519",
publisher = "Elsevier Limited",
number = "12",
}