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7 H-Pyrrolo[2,3- d]pyrimidin-4-amine-Based Inhibitors of Calcium-Dependent Protein Kinase 1 Have Distinct Inhibitory and Oral Pharmacokinetic Characteristics Compared with 1 H-Pyrazolo[3,4- d]pyrimidin-4-amine-Based Inhibitors.

ACS Infectious Diseases. 2018; 
Rama Subba Rao Vidadala, Martin Golkowski, Matthew A. Hulverson, Ryan Choi, MollyC. McCloskey, Grant R. Whitman, Wenlin Huang, Samuel L.M. Arnold, Lynn K Barrett,Erkang Fan, Ethan A Merritt, Wesley C. Van Voorhis, Kayode K Ojo, and Dustin J Maly
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Peptide Synthesis Inhibitory effects of BKIs on CpCDPK1 and TgCDPK1;20-21 and off-target inhibition of small gatekeeper human tyrosine kinase, SRC, was determined by indirect measurement of changes in initial reaction ATP concentration after phosphorylation of peptide substrate Syntide 2 (PLARTLSVAGLPGKK) and (Ac-EIYGEFKKK) (GenScript, Piscataway, NJ), respectively, via luminescence with Kinaseglo® as previously described. Get A Quote

摘要

关键词

Cryptosporidium parvum; Calcium-Dependent Protein Kinase 1 (CpCDPK1) inhibitors; 7H-pyrrolo[2,3-d]pyrimidin-4-amine; 1H-pyrazolo[3,4-d]pyrimidin-4-amine