Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis.

Hulverson, Matthew A; Choi, Ryan; Arnold, Samuel L M; Schaefer, Deborah A; Hemphill, Andrew; McCloskey, Molly C; Betzer, Dana P; Müller, Joachim; Vidadala, Rama S R; Whitman, Grant R; Rivas, Kasey L; Barrett, Lynn K; Hackman, Robert C; Love, Melissa S; McNamara, Case W; Shaughnessy, Thomas K; Kondratiuk, Alison; Kurnick, Matthew; Banfor, Patricia N; Lynch, James J; ... (2017). Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis. International journal for parasitology, 47(12), pp. 753-763. Elsevier 10.1016/j.ijpara.2017.08.006

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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.

Item Type:

Journal Article (Original Article)

Division/Institute:

05 Veterinary Medicine > Research Foci > Host-Pathogen Interaction
05 Veterinary Medicine > Department of Infectious Diseases and Pathobiology (DIP) > Institute of Parasitology
05 Veterinary Medicine > Department of Infectious Diseases and Pathobiology (DIP)

UniBE Contributor:

Hemphill, Andrew and Müller, Joachim

Subjects:

600 Technology > 630 Agriculture
500 Science > 540 Chemistry
500 Science > 570 Life sciences; biology

ISSN:

0020-7519

Publisher:

Elsevier

Language:

English

Submitter:

Andrew Hemphill

Date Deposited:

17 May 2018 17:17

Last Modified:

16 Aug 2018 14:52

Publisher DOI:

10.1016/j.ijpara.2017.08.006

PubMed ID:

28899690

Uncontrolled Keywords:

BKI 1369 Calcium-dependent protein kinase 1 Cryptosporidiosis Drug target Gatekeeper residue

BORIS DOI:

10.7892/boris.113111

URI:

https://boris.unibe.ch/id/eprint/113111

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