Regulation of gene expression by synthetic dimerizers with novel specificity.

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Yang W, Keenan TP, Rozamus LW, Wang X, Rivera VM, Rollins CT, Clackson T, Holt DA

Regulation of gene expression by synthetic dimerizers with novel specificity.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3181-4.

PubMed ID

12951089 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
{3-[3-(3,4-Dimethoxy-Phenyl)-1-(1-{1-[2-(3,4,5-Trimethoxy-Phenyl)-Butyryl]-Piperidin-2yl}-Vinyloxy)-Propyl]-Phenoxy}-Acetic Acid	Peptidyl-prolyl cis-trans isomerase FKBP1A	IC 50 (nM)	8.2	N/A	N/A	Details