How does entecavir (ETV) affect the phosphorylation of deoxyguanosine (dG) and deoxyadenosine (dA) in different tissues?
Label:chem
Topic
A study examines the phosphorylation of dG and dA in mitochondria isolated from the brain, heart, kidney, and liver of rats. The effects of ETV on these processes are also evaluated.
Answer
In all tested tissues, dG was phosphorylated 10–30 times more efficiently than dA. ETV was phosphorylated 2.5–4 times better than dA but 15–20% as efficiently as dG. The liver had the highest rate of phosphorylation for all three substrates, while the heart had the lowest. ETV inhibited dG phosphorylation with an IC50 of 15.3 ± 2.2 μM and dA phosphorylation with an IC50 of 0.028 ± 0.006 μM, indicating tissue-specific differences in sensitivity to ETV.
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