Mechanism of inhibition of human cytomegalovirus replication by oxetanocin G (cas 113269-46-8)

Add time:08/11/2019    Source:sciencedirect.com

SummaryOxetanocin G(9-(2-deoxy-2-hydroxymethyl-β-D-erythro-oxetanosyl)guanine, OXTG) is a potent and selective agent against human cytomegalovirus (HCMV). In this study we synthesized the triphosphate form of OXT-G, OXT-GTP, and examined its effect on the activities of HCMV DNA polymerase, herpes simplex type 2 (HSV-2) DNA polymerase and human DNA polymerase α. OXT-GTP was found to inhibit all these polymerases in a competitive manner with respect to dGTP. The Km for dGTP and the Ki for OXT-GTP of HCMV DNA polymerase were 0.86 and 0.53 μM, respectively, while the corresponding values of DNA polymerase a were 2.2 and 3.6 μM, respectively. HPLC analysis using [3H]OXT-G also revealed that OXT-G was converted to its triphosphate form 7- to 8-fold more efficiently in HCMV-infected cells than in uninfected cells. The results suggest that both the preferential phosphorylation of OXT-G in HCMV-infected cells and the preferential inhibition of HCMV DNA polymerase by OXT-GTP may contribute towards the selective activity of OXT-G against HCMV replication.

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