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ATP-binding domain of NTPase-helicase as a target for hepatitis C antiviral therapy

100%

Borowski P., Mueller O., Niebuhr A., Kalitzky M., Hwang L. H., Schmitz H., Siwecka M. A., Kulikowski T.

Acta Biochimica Polonica

2000

tom 47

nr 1

To enhance the inhibitory potential of 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin) vs hepatitis C virus (HCV) NTPase/helicase, ribavirin-5'-triphosphate (ribavirin-TP) was synthesized and investigated. Ribavirin-TP was prepared with the use of modified Yoshikawa-Ludwig-Mishra-Broom procedure (cf. Mishra & Broom, 1991, J. Chem. Soc., Chem. Commun, 1276-1277) involving phosphorylation of unprotected nucleoside. Kinetic analysis revealed enhanced inhibitory potential of ribavirin-TP (IC50=40 µM) as compared to ribavirin (IC50 > 500 µM). Analysis of the inhibition type by means of graphical methods showed a competitive type of inhibition with respect to ATP. In view of the relatively low specificity towards nucleoside-5'-triphosphates (NTP) of the viral NTPase/helicases, it could not be ruled out that the investigated enzyme hydrolyzed the ribavirin-TP to less potent products. Investigations on non- hydrolysable analogs of ribavirin-TP or ribavirin-5'-diphosphate (ribavirin-DP) are currently under way.

Existing and future therapeutic options for hepatitis C virus infection

100%

Bretner M.

Acta Biochimica Polonica

2005

tom 52

nr 1

Hepatitis C virus (HCV) infection is an important cause of chronic hepatitis, cirrhosis, hepatocellular carcinoma and liver failure worldwide. Chronic hepatitis C virus infection is treated with interferon-alpha (IFN-alpha), pegylated interferon-alpha (PEG-IFNalpha) alone or in combination with ribavirin; however, a significant fraction of patients either fail to respond or relapse after cessation of therapy. Efforts to identify and develop highly specific and potent HCV inhibitors have intensified recently. Each of the virally encoded replication enzymes has been a focus of studies as well as viral receptors and the host immune system. This review summarizes recent progress in the search for novel anti-HCV agents.

Ograniczanie wyników

2 Acta Biochimica Polonica

1 Borowski P.

1 Bretner M.

1 Hwang L. H.

1 Kalitzky M.

1 Kulikowski T.

1 Mueller O.

1 Niebuhr A.

1 Schmitz H.

1 Siwecka M. A.

1 2005

1 2000

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ATP-binding domain of NTPase-helicase as a target for hepatitis C antiviral therapy

Existing and future therapeutic options for hepatitis C virus infection