Bifunctional molecules and methods for their use in the production of
binary or tripartite complexes in a host are provided. The bifunctional molecule
is a conjugate of a drug moiety and a presenter protein ligand. The molecular weight
of the bifunctional molecule is less than about 5000 daltons. In the methods, an
effective amount of the bifunctional molecule is administered to the host. In certain
embodiments the bifunctional molecule binds to the presenter protein and a drug
target to produce a tripartite complex, while in other embodiments the bifunctional
molecule binds to either the presenter protein or the drug target, but not both,
to produce a binary complex The subject methods and compositions find use in a
variety of therapeutic applications.