Development of 5-Aminopyrazole-4-carboxamide-based Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy

Autor: Ryan Choi, Wesley C. Van Voorhis, Grant R. Whitman, Zhongsheng Zhang, Kayode K. Ojo, Wenlin Huang, Molly C. McCloskey, Lynn K. Barrett, Robert C. Hackman, Samuel L.M. Arnold, Kasey Rivas, Erkang Fan, Matthew A. Hulverson

Publikováno v: Journal of Medicinal Chemistry. 62:3135-3146

Cryptosporidium is a leading cause of pediatric diarrhea worldwide. Currently there is neither a vaccine nor a consistently effective drug available for this disease. Selective 5-aminopyrazole-4-carboxamide-based bumped-kinase inhibitors (BKIs) are e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7863df51de4d643de4abd6950dc3ce76
https://doi.org/10.1021/acs.jmedchem.9b00069

Safety and efficacy of the bumped kinase inhibitor BKI-1553 in pregnant sheep experimentally infected with Neospora caninum tachyzoites

Autor: Matthew A. Hulverson, Luis Miguel Ortega-Mora, Javier Blanco-Murcia, Andrew Hemphill, Luis Miguel Ferrer, Marta González-Huecas, Kasey Rivas, Wesley C. Van Voorhis, Javier Regidor-Cerrillo, Lynn K. Barrett, Patricia Vázquez, Paula García-Lunar, Michela Re, Julio Benavides, Ignacio Ferre, Kayode K. Ojo, Ryan Choi, Enrique Tabanera, Manuel Pizarro Díaz, Grant R. Whitman, Roberto Sánchez-Sánchez, Pablo Castaño

Publikováno v: Sánchez-Sánchez, Roberto; Ferre, Ignacio; Re, Michela; Vázquez, Patricia; Ferrer, Luis Miguel; Blanco-Murcia, Javier; Regidor-Cerrillo, Javier; Pizarro Díaz, Manuel; González-Huecas, Marta; Tabanera, Enrique; García-Lunar, Paula; Benavides, Julio; Castaño, Pablo; Hemphill, Andrew; Hulverson, Matthew A; Whitman, Grant R; Rivas, Kasey L; Choi, Ryan; Ojo, Kayode K; Barrett, Lynn K; ... (2018). Safety and efficacy of the bumped kinase inhibitor BKI-1553 in pregnant sheep experimentally infected with Neospora caninum tachyzoites. International journal for parasitology. Drugs and drug resistance, 8(1), pp. 112-124. Elsevier 10.1016/j.ijpddr.2018.02.003
Zaguán. Repositorio Digital de la Universidad de Zaragoza
instname
International Journal for Parasitology: Drugs and Drug Resistance, Vol 8, Iss 1, Pp 112-124 (2018)
International Journal for Parasitology: Drugs and Drug Resistance
Digital.CSIC. Repositorio Institucional del CSIC

13 páginas, 2 tablas, 7 figuras.
Neospora caninum is one of the main causes of abortion in cattle, and recent studies have highlighted its relevance as an abortifacient in small ruminants. Vaccines or drugs for the control of neosporosis are la

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e65eac8993ea2125eb8ddd31690e2b2
https://doi.org/10.1016/j.ijpddr.2018.02.003

Selective inhibition of Sarcocystis neurona calcium-dependent protein kinase 1 for equine protozoal myeloencephalitis therapy

Autor: Amy E. DeRocher, Dustin J. Maly, Suzanne Scheele, Daniel K. Howe, Sriveny Dangoudoubiyam, Marilyn Parsons, Tess R. Smith, Matthew A. Hulverson, Wesley C. Van Voorhis, Lynn K. Barrett, Jitender P. Dubey, Shiv K. Verma, Ryan Choi, Michelle R. Yeargan, Kayode K. Ojo, Kasey Rivas, Erkang Fan

Publikováno v: International Journal for Parasitology. 46:871-880

Sarcocystis neurona is the most frequent cause of equine protozoal myeloencephalitis, a debilitating neurological disease of horses that can be difficult to treat. We identified SnCDPK1, the S. neurona homologue of calcium-dependent protein kinase 1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5154f5c56e03ddb58fadde930be1674b
https://doi.org/10.1016/j.ijpara.2016.08.003

Bumped-Kinase Inhibitors for Cryptosporidiosis Therapy

Autor: Alejandro Castellanos-Gonzalez, Wesley C. Van Voorhis, Lynn K. Barrett, Samuel L.M. Arnold, Sumiti Vinayak, Dana P. Betzer, Michael W. Riggs, Dustin J. Maly, Kasey Rivas, Boris Striepen, Gillian T. Herbert, Kayode K. Ojo, Carrie F. Brooks, Rama Subba Rao Vidadala, Ryan Choi, A. Clinton White, Grant R. Whitman, Deborah A. Schaefer, Hayley Sparks, Matthew A. Hulverson

Publikováno v: The Journal of infectious diseases. 215(8)

Bumped kinase inhibitors (BKIs) of Cryptosporidium parvum calcium-dependent protein kinase 1 (CpCDPK1) are leading candidates for treatment of cryptosporidiosis-associated diarrhea. Potential cardiotoxicity related to anti-human ether-a-go-go potassi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d941441f145f6833a3b4aea55caca56c
https://pubmed.ncbi.nlm.nih.gov/29309678

Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation

Autor: Wesley C. Van Voorhis, Andrew D. Hamilton, Michael H. Gelb, Steven Fletcher, Kasey Rivas, William P. Katt, Christopher G. Cummings, Frederick S. Buckner, Debopam Chakrabarti, Saïd M. Sebti, Carrie Hornéy

New chemotherapeutics are urgently needed to combat malaria. We previously reported on a novel series of antimalarial, ethylenediamine-based inhibitors of protein farnesyltransferase (PFT). In the current study, we designed and synthesized a series o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74272a2eeefc79dcc51eb99fefd088a1
https://ora.ox.ac.uk/objects/uuid:83a0a956-1a28-4b39-b6e1-f088289d6c02