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Regulation of gene expression by synthetic dimerizers with novel specificity
Wu Yang1, Terence P Keenan, Leonard W Rozamus
1ARIAD Gene Therapeutics, Inc., 26 Landsdowne Street, Cambridge, MA 02139-4234, USA.
Bioorganic & Medicinal Chemistry Letters
|September 3, 2003
Abstract:
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.