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Mechanism of PPARγ activation. Upon ligand binding to the PPAR/RXR heterodimer, a conformational change leads to release of a corepressor and binding of a coactivator; this regulates the kinetics of the assembly of the transcription complex, resulting in increased affinity for the specific PPAR response element, which modulates gene transcription. RXR; Retinoic X receptor; PPRE; PPAR response element.
