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Title: SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1

Journal Article · · ACS Medicinal Chemistry Letters
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  1. Department of Biochemistry, University of Washington, Seattle, Washington 98195, United States
  2. Department of Medicine, Division of Allergy and Infectious Diseases, and the Center for Emerging and Re-emerging Infectious Diseases (CERID), University of Washington, Seattle, Washington 98109, United States
  3. Department of Chemistry, University of Washington, Seattle, Washington 98195, United States
  4. Center for Infectious Disease Research (formerly Seattle Biomedical Research Institute), Seattle, Washington 98109, United States
  5. Portland VA Medical Center, Portland, Oregon 97239, United States
  6. AbbVie, N. Chicago, Illinois 60064, United States
  7. PATH, San Francisco, California 94102, United States
  8. Department of Pharmaceutics, University of Washington, Seattle, Washington 98195, United States
  9. Center for Infectious Disease Research (formerly Seattle Biomedical Research Institute), Seattle, Washington 98109, United States, Department of Global Health, University of Washington, Seattle, Washington 98195, United States
  10. Department of Medicine, Division of Allergy and Infectious Diseases, and the Center for Emerging and Re-emerging Infectious Diseases (CERID), University of Washington, Seattle, Washington 98109, United States, Department of Global Health, University of Washington, Seattle, Washington 98195, United States

Sponsoring Organization:
USDOE Office of Science (SC), Basic Energy Sciences (BES)
Grant/Contract Number:
AC02-76SF00515
OSTI ID:
1227228
Journal Information:
ACS Medicinal Chemistry Letters, Journal Name: ACS Medicinal Chemistry Letters Vol. 6 Journal Issue: 12; ISSN 1948-5875
Publisher:
American Chemical SocietyCopyright Statement
Country of Publication:
United States
Language:
English
Citation Metrics:
Cited by: 29 works
Citation information provided by
Web of Science

References (21)

Attachment of Toxoplasma gondii to Host Cells Involves Major Surface Protein, SAG-1 (P-30) journal August 1994
Use of the Kinase Inhibitor Analog 1NM-PP1 Reveals a Role for Toxoplasma gondii CDPK1 in the Invasion Step journal April 2010
Calcium-Dependent Signaling and Kinases in Apicomplexan Parasites journal June 2009
Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol journal February 2015
Development and Applications of a Broad-Coverage, TR-FRET-Based Kinase Binding Assay Platform journal June 2009
Structures of apicomplexan calcium-dependent protein kinases reveal mechanism of activation by calcium journal May 2010
Potent and Selective Inhibitors of CDPK1 from T. gondii and C. parvum Based on a 5-Aminopyrazole-4-carboxamide Scaffold journal November 2013
Intracellular calcium stores in Toxoplasma gondii govern invasion of host cells journal July 2003
Generation of Monospecific Nanomolar Tyrosine Kinase Inhibitors via a Chemical Genetic Approach journal February 1999
Apical Organelle Discharge by Cryptosporidium parvum Is Temperature, Cytoskeleton, and Intracellular Calcium Dependent and Required for Host Cell Invasion journal December 2004
Discovery of Potent and Selective Inhibitors of CDPK1 from C. parvum and T. gondii journal July 2010
Development of Toxoplasma gondii Calcium-Dependent Protein Kinase 1 ( Tg CDPK1) Inhibitors with Potent Anti- Toxoplasma Activity journal February 2012
Kinetics of parasite burdens in blood and tissues during murine toxoplasmosis journal July 2012
Calcium-dependent protein kinase 1 is an essential regulator of exocytosis in Toxoplasma journal May 2010
Optimizing Small Molecule Inhibitors of Calcium-Dependent Protein Kinase 1 to Prevent Infection by Toxoplasma gondii journal March 2013
Fragment-Based Cocktail Crystallography by the Medical Structural Genomics of Pathogenic Protozoa Consortium journal December 2009
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1 journal August 2012
Toxoplasma gondii calcium-dependent protein kinase 1 is a target for selective kinase inhibitors journal May 2010
A second-site suppressor strategy for chemical genetic analysis of diverse protein kinases journal May 2005
Multiple Determinants for Selective Inhibition of Apicomplexan Calcium-Dependent Protein Kinase CDPK1 journal March 2012
Toxoplasmosis book January 2011