Tamoxifen-Based Probes for the Study of Estrogen Receptor-Mediated Transcription.

Autor: Stock, G., Lessl, M., Jaroch, S., Weinmann, H., Trebley, J. P., Rickert, E. L., Reyes, P. T., Weatherman, R. V.
Zdroj: Chemical Genomics; 2006, p75-87, 13p
Abstrakt: The nuclear receptors are ideal targets to control the expression of specific genes with small molecules. Estrogen receptor can activate or repress transcription though a number of different pathways. As part of an effort to develop reagents that selectively target specific transcriptional regulatory pathways, analogs of 4-hydroxytamoxifen were synthesized with variations in the basic side chain. In vitro binding assays and cell-based luciferase reporter gene assays confirm that all the derivatives have high affinity for the receptor and high potency at repressing direct estrogen receptor-mediated transcription. [ABSTRACT FROM AUTHOR]
Databáze: Supplemental Index