PPAR and Agonists against Cancer: Rational Design of Complementation Treatments
Figure 1
PPARγ structure and regulation. (a) Schematic representation of the domain structure of the PPARγ-1 and PPARγ-2. The mutations associated with
metabolic syndrome are indicated. LF: loss of function; GF: gain of function. (b) Positive and negative regulators of the PPARγ gene transcription. (c) The
regulation of PPARγ levels by Rb and E2F. (d) The
mechanism of ligand-dependent PPARγ activation. (e) The regulation
of PPARγ activity by MEK and Erk kinases: MEK1
activates Erk-1/2, which phosphorylates
PPARγ and targets it to proteasomes; in addition, MEK1 binds
PPARγ in the nucleus and exports it to the
cytoplasm. MEK5 can serve as coactivator for the PPARγ.
