Inducible gene expression and protein translocation using nontoxic ligands identified by a mammalian three-hybrid screen.

@article{Liberles1997InducibleGE,
  title={Inducible gene expression and protein translocation using nontoxic ligands identified by a mammalian three-hybrid screen.},
  author={Stephen D. Liberles and Steven T. Diver and David J. Austin and Stuart L. Schreiber},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1997},
  volume={94 15},
  pages={7825-30}
}
The natural product rapamycin has been used to provide temporal and quantitative control of gene expression in animals through its ability to interact with two proteins simultaneously. A shortcoming of this approach is that rapamycin is an inhibitor of cell proliferation, the result of binding to FKBP12-rapamycin-associated protein (FRAP). To overcome this limitation, nontoxic derivatives of rapamycin bearing bulky substituents at its C16-position were synthesized, each in a single step. The… CONTINUE READING