Skip to main content
SLU:s publikationsdatabas (SLUpub)
Forskningsartikel - Refereegranskat, 2001

Antiviral Guanosine Analogs as Substrates for Deoxyguanosine Kinase: Implications for Chemotherapy

Herrström Sjöberg, Anita; Wang, Liya; Eriksson, Staffan


A highly active form of human recombinant deoxyguanosine kinase (dGK) phosphorylated purine nucleoside analogs active against cytomegalovirus, hepatitis B virus, and human immunodeficiency virus, such as penciclovir, 2',3'-dideoxyguanosine and 3'-fluoro-2',3'-dideoxyguanosine. The antiherpesvirus drug ganciclovir, which is also used in gene therapy, was a substrate for dGK, but with low efficiency. ATP and UTP were both good phosphate donors, with apparent K-m values of 6 and 4 muM and V-max values of 34 and 90 nmol of dGMP/mg of dGK/min, respectively. With a mixture of 5 mM ATP and 0.05 mM UTP, which represent physiologically relevant concentrations, the activities of dGK with ganciclovir and penciclovir was 1% and approximately 10%, respectively, of that with dGuo, The levels of dGK in different tissues were determined with a selective enzyme assay and the total activities per gram of tissues were similar in liver, brain, heart, and thymus extracts. The fact that the cellular dGK enzyme can phosphorylate antiviral guanosine analogs may help to explain the efficacies and side effects of several forms of chemotherapy.

Publicerad i

Antimicrobial Agents and Chemotherapy
2001, Volym: 45, nummer: 3, sidor: 739-742

      SLU författare

    • Herrström Sjöberg, Anita

      • Institutionen för veterinärmedicinsk kemi, Sveriges lantbruksuniversitet
      • Wang, Liya

        • Institutionen för veterinärmedicinsk kemi, Sveriges lantbruksuniversitet
        • Eriksson, Staffan

          • Institutionen för veterinärmedicinsk kemi, Sveriges lantbruksuniversitet

        UKÄ forskningsämne

        Biochemistry and Molecular Biology
        Medicinal Chemistry

        Publikationens identifierare


        Permanent länk till denna sida (URI)