Regulation of gene expression by synthetic dimerizers with novel specificity.


New synthetic chemical inducers of dimerization, comprising homodimeric FKBP ligands with engineered specificity for the designed point mutant F36V, have been evaluated for inducing targeted gene expression in mammalian cells. Structure-activity studies indicated that high-affinity dimerizers such as AP1903 are ineffective, perhaps due to kinetic trapping of non-productive dimers, whereas lower-affinity molecules, exemplified by AP1889 and AP1966, potently activate transcription.


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@article{Yang2003RegulationOG, title={Regulation of gene expression by synthetic dimerizers with novel specificity.}, author={Wu Yang and Terence P Keenan and Leonard W Rozamus and Xiurong Wang and Victor M Rivera and Carl T Rollins and Tim Clackson and Dennis A Holt}, journal={Bioorganic & medicinal chemistry letters}, year={2003}, volume={13 19}, pages={3181-4} }