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. Author manuscript; available in PMC: 2017 Sep 1.
Published in final edited form as: Biochim Biophys Acta. 2016 Feb 10;1859(9):1130–1140. doi: 10.1016/j.bbagrm.2016.02.006

Figure 2. Schematic illustration of Mechanisms of PXR Activation.

Figure 2

Direct Activation – PXR is retained in a cytoplasmic complex with HSP90 and CCRP, which dissociate upon ligand binding leading to PXR nuclear accumulation. Unbound PXR in the nucleus is complexed to corepressors NcoR and SMRT, which dissociate upon ligand stimulation, leading to the recruitment of coactivators SRC1 and GRIP1 and the transcription of target genes. Indirect Activation – This is a less well-developed mechanism of PXR activation, although the Ser350, Thr248, Thr290, and Thr408 phosphorylation sites of PXR are known to affect its activation. Compounds disturbing signaling pathways may influence the phosphorylation, nuclear translocation, and target gene express of PXR.