Transcript Slide 1

PPARγ-RXR nuclear receptor complex and
transcriptional activity (activation)
Coactivator protein
Ligand
PPARγ
RXRα
Ligand
DNA
PPRE
PPARγ forms a heterodimer with RXR (PPARγ-RXR Complex) to bind to DNA. If
ligand binds to either PPAR or RXR, changes in the heterodimer are induced which
lead to the release of corepressor molecules and the recruitment of coactivator
proteins resulting in the formation of a transcriptional regulatory complex as
shown above. This complex then binds to specific PPAR response elements (PPRE)
resulting in transcriptional activation of target genes, regulating physiological
processes such as adipocyte differentiation, glucose homeostasis, antiinflammation etc.
PPARγ-RXR nuclear receptor complex and
transcriptional activity (inhibition)
Corepressor protein
Mutant PPARγ
RXR
DNA
PPRE
Human PPARγ mutants are able to heterodimerise with RXR on DNA but cannot bind
ligand. This leads to the recruitment of a corepressor instead of a coactivator protein
leading to silencing of target gene transcription.