Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis

Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite . The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1 -pyrazolo[3,4- ]pyrimidine-4-amine (PP) compounds that are bulky ATP mi...

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Veröffentlicht in:	Journal of medicinal chemistry 2020-06, Vol.63 (11), p.6144-6163
Hauptverfasser:	Janetka, James W, Hopper, Allen T, Yang, Ziping, Barks, Jennifer, Dhason, Mary Savari, Wang, Qiuling, Sibley, L David
Format:	Artikel
Sprache:	eng
Schlagworte:	Acute Disease Animals Binding Sites Cell Line Cell Proliferation - drug effects Chronic Disease Crystallography, X-Ray Cytochrome P-450 Enzyme System - metabolism Half-Life Humans Mice Molecular Conformation Molecular Dynamics Simulation Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Protein Kinases - chemistry Protein Kinases - metabolism Protozoan Proteins - antagonists & inhibitors Protozoan Proteins - metabolism Pyrimidines - chemistry Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Pyrimidines - therapeutic use Structure-Activity Relationship Toxoplasma - drug effects Toxoplasma - enzymology Toxoplasmosis - drug therapy
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