Maribavir effectively inhibits the autophosphorylation of both wild-type and major Ganciclovir (GCV) resistant UL97 mutants, with an average IC50 of 35 nM. The M460I mutation exhibits increased sensitivity to Maribavir, having an IC50 of 4.8 nM, while the Maribavir-resistant UL97 mutant L397R shows reduced kinase activity to about 10% of the wild type. Enzyme kinetics reveal Maribavir acts as a competitive inhibitor of ATP with a Ki of 10 nM[1]. Additionally, Maribavir suppresses viral replication dose-dependently with an IC50 of 0.12±0.01 μM in multicycle DNA hybridization assays, and strongly inhibits the pUL97 protein kinase at a 50% inhibition concentration of 3 nM[2].
体外研究
Maribavir effectively inhibits the autophosphorylation of both wild-type and major Ganciclovir (GCV) resistant UL97 mutants, with an average IC50 of 35 nM. The M460I mutation exhibits increased sensitivity to Maribavir, having an IC50 of 4.8 nM, while the Maribavir-resistant UL97 mutant L397R shows reduced kinase activity to about 10% of the wild type. Enzyme kinetics reveal Maribavir acts as a competitive inhibitor of ATP with a Ki of 10 nM[1].
Additionally, Maribavir suppresses viral replication dose-dependently with an IC50 of 0.12±0.01 μM in multicycle DNA hybridization assays, and strongly inhibits the pUL97 protein kinase at a 50% inhibition concentration of 3 nM[2].
Cytomegalovirus Infections
... 展开 >> HIV Infections 收起 <<
Phase 1
Completed
-
United States, California
... 展开 >>
Univ of California/ San Francisco / Dept of Medicine
San Francisco, California, United States, 94110
Dr Jacob Lalezari
San Francisco, California, United States, 94115 收起 <<
Cytomegalovirus Infections
... 展开 >> HIV Infections 收起 <<
Phase 1
Completed
-
United States, California
... 展开 >>
Univ of California/ San Francisco / Dept of Medicine
San Francisco, California, United States, 94110
Dr Jacob Lalezari
San Francisco, California, United States, 94115 收起 <<
United States, California
... 展开 >>
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