Inhibition of protein kinase activity from Trypanosoma cruzi and Trypanosoma gambiense by 3'-deoxyadenosine.
3'-Deoxydadenosine was found to be a potent inhibitor of nucleoside-stimulated protein kinase activity from culture forms of Trypanosoma cruzi and bloodstream forms of Trypanosoma gambiense. The type of inhibition by 3'-deoxyadenosine was competitive with respect to ATP. The inhibition constants for 3'-deoxyadenosine were determined to be 0.11mM and 0.085mM for the enzyme from T. cruzi and T. gambiense, respectively. The apparent Km value for ATP was 0.2mM for both enzymes. 2'-Deoxyadenosine was less effective as inhibitor of the protein kinase activity. The inhibition constants were calculated to be 0.8mM and 0.67mM, respectively.
D000255:Adenosine Triphosphate / Q000378:metabolism; D003839:Deoxyadenosines / Q000494:pharmacology*; D007700:Kinetics; D011494:Protein Kinases / Q000378:metabolism*; D012263:Ribonucleosides / Q000494:pharmacology; D014347:Trypanosoma brucei gambiense / Q000187:drug effects / Q000201:enzymology*; D014349:Trypanosoma cruzi / Q000187:drug effects / Q000201:enzymology*
D003839:Deoxyadenosines; D012263:Ribonucleosides; D000255:Adenosine Triphosphate; D011494:Protein Kinases