What is the role of entecavir (ETV) in inhibiting the phosphorylation of deoxyguanosine (dG) and deoxyadenosine (dA) in mitochondria?

Label:chem

Topic
Entecavir (ETV) is an antiviral nucleoside analog used to treat chronic hepatitis B. A study investigates whether ETV can competitively inhibit the phosphorylation of deoxyguanosine (dG) and deoxyadenosine (dA) by deoxyguanosine kinase (dGK) in isolated mitochondria and perfused rat hearts.
Answer
ETV competitively inhibits the phosphorylation of dG and dA in rat mitochondria. It has an IC50 of 15.3 ± 2.2 μM for inhibiting dG phosphorylation and an IC50 of 0.028 ± 0.006 μM for inhibiting dA phosphorylation. ETV is a more potent inhibitor of dA phosphorylation than dG phosphorylation, suggesting it could affect the synthesis of dATP and potentially lead to mitochondrial toxicity.
Return to Home Chemical List
Knowledge you may be interested in
How does the amount of triethylborane (TEB) affect the reactivity ratio of ethylene oxide (EO) in the copolymerization with anhydrides? What are the functions of succinic anhydride (SA) and phthalic anhydride (PA) in the copolymerization process? What is the role of tetrabutylammonium chloride (TBACl) in the copolymerization process? What is the role of triethylborane (TEB) in the copolymerization of epoxides and anhydrides? What is the significance of the alternating copolymer structure formed by butyl acrylate (BA) and vinyl butyl ether (VBE)? How does the presence of triethylborane (TEB) affect the structure of the resulting graft copolymer? What is the significance of vinyl butyl ether (VBE) in the graft copolymerization process? How does butyl acrylate (BA) contribute to the formation of graft copolymers with cod collagen? What is the role of triethylborane (TEB) in the synthesis of graft copolymers of cod collagen? What is the role of the E ring fragment 35 in the synthesis of the CDE ring fragment of pectenotoxin-4? What are the roles of deoxyguanosine kinase (dGK) in the mitochondrial purine salvage pathway? How does entecavir (ETV) affect the phosphorylation of deoxyguanosine (dG) and deoxyadenosine (dA) in different tissues? What are the potential implications of entecavir (ETV) inhibiting deoxyguanosine kinase (dGK) in mitochondrial DNA (mtDNA) synthesis? How do deoxyguanosine (dG) and entecavir (ETV) competitively inhibit each other's phosphorylation by deoxyguanosine kinase (dGK)? What are the kinetic properties of deoxyguanosine (dG) and entecavir (ETV) phosphorylation by deoxyguanosine kinase (dGK)? What is the role of 2-methyltetrahydrofuran (2-MeTHF) in the extraction of Actinostemma lobatum kernel oil? What are the primary bioactive compounds found in Actinostemma lobatum kernel oil? What is the impact of solvent type on the oxidative stability of Actinostemma lobatum kernel oil? What are the major fatty acids in Actinostemma lobatum kernel oil? How does 2-methylpentane (2-MP) compare to n-hexane in terms of oil yield and oxidative stability?