Valacyclovir and Acyclovir as Substrates of Cypin
Author Information
Author(s): Keith R. Lange, Noor Rasheed, Xiaoyang Su, M. Elena Diaz‐Rubio, Bonnie L. Firestein
Primary Institution: Rutgers, The State University of New Jersey
Hypothesis
Are valacyclovir and acyclovir deaminated by cypin or do they act as inhibitors?
Conclusion
Valacyclovir and acyclovir are substrates of cypin, which deaminates them and allows their metabolites to be processed further.
Supporting Evidence
- Valacyclovir and acyclovir were confirmed as substrates of cypin using multiple assays.
- The study determined K_m values for guanine and valacyclovir, showing that cypin processes guanine more efficiently.
- Binding of valacyclovir to cypin caused a conformational change in the enzyme.
- Deaminated products of valacyclovir and acyclovir can be further processed by xanthine oxidase and uricase.
Takeaway
This study shows that two antiviral drugs, valacyclovir and acyclovir, can be changed by an enzyme in the body called cypin, which helps break them down.
Methodology
The study used various biochemical assays including NADH-coupled assays, tryptophan fluorescence quenching assays, and LC-MS to analyze the interaction of cypin with valacyclovir and acyclovir.
Limitations
The study did not determine the effects of higher concentrations of valacyclovir and acyclovir on cypin activity.
Statistical Information
P-Value
0.05
Statistical Significance
p<0.05
Digital Object Identifier (DOI)
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