Characterization of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG): Antiparasitic activity of a PKG inhibitor☆

2006 ◽  
Vol 146 (1) ◽  
pp. 78-88 ◽  
Author(s):  
Carmen A. Diaz ◽  
John Allocco ◽  
Mary Ann Powles ◽  
Lai Yeung ◽  
Robert G.K. Donald ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Protein Kinase ◽  
Dependent Protein Kinase ◽  
Antiparasitic Activity ◽  
Cgmp Dependent Protein Kinase ◽  
Dependent Protein

scholarly journals Discovery of novel potent, cell-permeable inhibitors of P. falciparum cGMP-dependent protein kinase.

2021 ◽  
Author(s):  
Rammohan R. Yadav Bheemanaboina ◽  
Mariana Lozano Gonzalez ◽  
Shams Ul Mahmood ◽  
Tyler Eck ◽  
Tamara Kreiss ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Protein Kinase ◽  
Murine Model ◽  
Dependent Protein Kinase ◽  
Antiparasitic Activity ◽  
Cgmp Dependent Protein Kinase ◽  
Structure Activity ◽  
Dependent Protein ◽  
Parasitic Activity

The discovery of new targets for treatment of malaria advanced with the demonstration that orally administered inhibitors of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG) could clear infection in a murine model. This enthusi-asm was tempered by unsatisfactory safety and/or pharmacokinetic issues found with these chemotypes. To address the urgent need for new scaffolds, we recently reported the discovery and optimization of novel, potent isoxazole-based PfPKG inhibitors that lacked any obvious safety warnings. This manuscript presents representative in vitro ADME, hERG charac-terization and cell-based antiparasitic activity of these PfPKG inhibitors. We also report the discovery and structure-activity relationships of a new series with good potency, low hERG activity and cell-based anti-parasitic activity comparable to a literature standard.

scholarly journals Mechanism of Allosteric Inhibition of Plasmodium falciparum CGMP-Dependent Protein Kinase

2020 ◽  
Vol 118 (3) ◽  
pp. 522a
Author(s):  
Olivia Byun ◽  
Katherine Van ◽  
Philipp Henning ◽  
Friedrich W. Herberg ◽  
Giuseppe Melacini
Keyword(s):  
Plasmodium Falciparum ◽  
Protein Kinase ◽  
Dependent Protein Kinase ◽  
Allosteric Inhibition ◽  
Cgmp Dependent Protein Kinase ◽  
Dependent Protein

scholarly journals The role of a parasite-specific D-site in activation of Plasmodium falciparum cGMP-dependent protein kinase

2015 ◽  
Vol 16 (S1) ◽  
Author(s):  
Eugen Franz ◽  
Jeong Joo Kim ◽  
Olga Schneider ◽  
Daniela Bertinetti ◽  
Choel Kim ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Protein Kinase ◽  
Dependent Protein Kinase ◽  
Cgmp Dependent Protein Kinase ◽  
Dependent Protein
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