Lipid conjugates of antiretroviral agents: release of antiretroviral nucleoside monophosphates by a nucleoside diphosphate diglyceride hydrolase activity from rat liver mitochondria.

Autor: van Wijk GM; Centre for Biomembranes and Lipid Enzymology, University of Utrecht, The Netherlands., Hostetler KY, van den Bosch H
Jazyk: angličtina
Zdroj: Biochimica et biophysica acta [Biochim Biophys Acta] 1991 Jul 30; Vol. 1084 (3), pp. 307-10.
DOI: 10.1016/0005-2760(91)90074-r
Abstrakt: The release of the 5'-monophosphates of the antiretroviral nucleoside analogs 3'-azido-3'-deoxythymidine, 3'-deoxythymidine and 2',3'-dideoxycytidine from the corresponding nucleoside diphosphate diglycerides as a result of rat liver mitochondrial enzymatic activity is shown. The three analogs appeared to be about equally active as substrate for this pyrophosphatase activity which showed maximum conversion rates of 3-6 nmol min-1 mg protein-1 at substrate concentrations between 500 to 800 microM. These results may contribute to the biochemical explanation for the observed anti-HIV activity of this type of phospholipid conjugates in vitro.
Databáze: MEDLINE