Chemical inducers of dimerization (dimerizers) are a new class of reag
ents used for controlling protein-protein interactions. Use of a small
-molecule, cell-permeable dimerizer to control the interaction of a tr
anscription activation domain and a DNA-binding domain allows the leve
l of expression of a target gene to be regulated by the concentration
of dimerizer. The modular design of components has facilitated the dev
elopment of multiple systems that can be used to readily generate cell
lines in which basal expression of the target gene is low and induced
to high levels by a nontoxic dimerizer. The development and use of on
e such system to control the expression of a gene in cultured cells ar
e described. (C) 1998 Academic Press.