What is the inhibitory effect of 7-deazaguanine (7DG) on HsPNP enzyme activity?

Label:chem

Topic
To evaluate the inhibitory effect of 7-deazaguanine (7DG) on human purine nucleoside phosphorylase (HsPNP), enzymatic assays were performed to determine the IC50 value and the degree of inhibition at specific concentrations.

From: "Crystal structure and molecular dynamics studies of human purine nucleoside phosphorylase complexed with 7-deazaguanine", Journal of Structural Biology, Volume 169, Issue 3, March 2010, Pages 379-388
Answer
The IC50 value for 7-deazaguanine (7DG) was determined to be 251 ± 2 µM. At a concentration of 200 µM, 7DG inhibited HsPNP enzyme activity by 37.5%, indicating that it has a moderate inhibitory effect on the enzyme. The study also confirmed that 7DG binds to HsPNP with a dissociation constant (K0) of 217 ± 14 µM, showing a low degree of cooperativity in binding.
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