Abstract
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.
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© 2006 Springer-Verlag Berlin Heidelberg
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Trebley, J.P., Rickert, E.L., Reyes, P.T., Weatherman, R.V. (2006). Tamoxifen-Based Probes for the Study of Estrogen Receptor-Mediated Transcription. In: Jaroch, S., Weinmann, H. (eds) Chemical Genomics. Ernst Schering Research Foundation Workshop, vol 58. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-37635-4_6
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DOI: https://doi.org/10.1007/978-3-540-37635-4_6
Publisher Name: Springer, Berlin, Heidelberg
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