Allosteric Controls of Nuclear Receptor Function in the Regulation of Transcription

Nuclear receptors control a large number of physiological events through the regulation of gene transcription. Their activation function involves and is controlled by ligands and multiple cofactors (repressors, activators and bridging proteins). Further post-translational modifications resulting from the crosstalk between different signaling pathways provide additional regulations. The numerous players involved allow the sophisticated fine-tuning of transcriptional regulation. The present review describes how allosteric mechanisms are used in the control of the sequential and ordered binding of nuclear receptors and the various protein effectors to target DNA.

Graphical AbstractFigure optionsDownload high-quality image (282 K)Download as PowerPoint slideHighlights
► Two classes of nuclear receptors.
► Crosstalk between different signaling pathways.
► Structural basis for an allosteric control mechanism of cofactor binding.
► The structural role and the allosteric contribution of DNA in the control of coactivator positioning and transcriptional regulation.
► Specificity of the oxosteroid subfamily of the steroid hormone nuclear receptors.