Mankertz J, Rokos K, Matthes E, Pauli G, Riedel E (1997): Cell specific uptake of antiviral drugs coupled to low density lipoproteins (LDL)
Biol. Chem. 378 suppl: S87.

The endocytosis in HIV infected human macrophages and lymphocytes was studied after covalent coupling of drugs to LDL. Internalization of nucleoside analogs (e.g. azidothymidine, AZT) and fluorothymidine (FLT) into HIV-1 infected human macrophages by the scavenger receptor pathway led to a dose-dependent inhibition of HIV replication. In HIV infected lymphocytes, which lack scavenger receptors, replication was not abolished. However, partial modification of LDL allowed endocytosis in nearly all cell types. Covalent coupling of drugs to LDL led to a cell specific transport. This strategy could possibly avoid toxic side-effects in the therapeutic use of antiretroviral drugs and thus may be a safer and more effective way for a chemotherapy even in the early phase of HIV infection.