Lipid conjugates of antiretroviral agents. II. Disodium palmityl phosphonoformate: anti-HIV activity, physical properties, and interaction with plasma proteins.

Autor: Camaioni Neto C; Department of Chemistry, Brown University, Providence, RI 02912., Steim JM, Sarin PS, Sun DK, Bhongle NN, Piratla RK, Turcotte JG
Jazyk: angličtina
Zdroj: Biochemical and biophysical research communications [Biochem Biophys Res Commun] 1990 Aug 31; Vol. 171 (1), pp. 458-64.
DOI: 10.1016/0006-291x(90)91415-o
Abstrakt: Disodium palmityl phosphonoformate, a novel lipid phosphoester of the anti HIV agent phosphonoformate (foscarnet), inhibits HIV replication in H9 cells and syncytia formation in MOLT-3 cells as effectively as foscarnet itself, as shown by dose-response data from assays for expression of p17 and p24 viral antigens and syncytia formation. Protein binding studies indicate that in serum, the derivative exists bound to albumin and the lipoproteins, and would therefore be likely to exhibit improved serum lifetime in vivo.
Databáze: MEDLINE