The paper reviews some of the new approaches to the targeting of bioac
tive compounds. In particular, the results of artificially rendering m
acromolecules hydrophobic by nonpolar substituents are considered. Thi
s principle enabled us to develop a method for suppressing virus repro
duction in cells with fatty acylated antiviral antibodies and also to
enhance antisense activity of short complementary oligonucleotides. So
me ideas for creation of drug-targeting systems based on self-assembli
ng supramolecular complexes have been tested. In this respect, a possi
bility of using interpolyelectrolyte complexes of nucleic acids with p
olycations for targeting genetic material into cells is discussed. Wit
hin the limits of this concept, a new class of highly selective immuno
toxins ('respecrins') representing supramolecular protein complexes in
which toxin molecules are reversibly masked by antibodies to specific
antigens of target cells has been developed.