|
| PPARs ligand | PPAR-independent effect | Experimental strategies | Ref. |
|
| PPAR ligands | | | |
| Troglitazone in LNCaP prostate cancer cells | Androgen receptor (AR) suppression by facilitating the
ubiquitin-dependent proteasomal degradation of the transcriptional factor
Sp-1 | STG28, a PPAR-inactive analogue of troglitazone. | [143] |
| Troglitazone in
mice | Rapidly AMP-activated protein kinase (AMPK)
activation through a yet undefined
PPAR--independent mechanism, leading to
the suppression of insulin-like growth factor-I tumor-promoting activity
(IGF-1) | Expression of a dominant-negative AMPK | [144] |
| Troglitazone and ciglitazone in MCF-7 breast
cancer | Repression of cyclin D1 expression, though a
post transcriptional mechanism, via proteasome-facilitated proteolysis | Proteasome inhibitors | [145] |
| Ciglitazone in HT1080
human fibrosarcoma | Increase of
MMP-2 expression through ROS
production and ERK activation | PPAR antagonist GW9662 | [146] |
| Troglitazone and 15-deoxy-prostaglandin J2
(15dPGJ2) in prostate and bladder cancer cells | Troglitazone
induces G0/G1 growth arrest and PGJ2 induces apoptosis | PPAR antagonist GW9662 | [147] |
| Troglitazone in B cell acute lymphoblastic
leukemia cell lines | Apoptosis and cell growth inhibition
associated with G1 cell cycle arrest | PPAR antagonists | [148] |
| Thiazolidinediones (TZD) in human breast
cancer | Inhibition of Cyclin D3 expression by
decreasing cyclin mRNA levels and by inducing its proteasomal degradation | A dominant negative mutant of PPAR | [149] |
| Troglitazone in mouse skin keratinocytes | Inhibition of cyclin D1 expression | PPAR antagonist GW9662 and
dominant Dominant negative PPAR. | [150] |
| Thiazolidinediones (TGZ) in human colon
cancer cells HTC-116 | Egr-1 promoter activity increase | Different PPAR ligands | [140] |
| 15-deoxy-prostaglandin
J2 (15dPGJ2) in colon carcinoma cells | COX2 and VEGF
inhibition via AP-1 activity
repression | Dominant negative form of PPAR and a PPAR antagonist | [151] |
| 15-deoxy-prostaglandin J2 (15dPGJ2) induces
apoptosis in human B lymphocytes | Apoptosis through the induction of ROS and
depletion of glutathione | Dominant negative form of PPAR and a PPAR antagonist | [152] |
| 15-deoxy-prostaglandin J2 (15dPGJ2) in Jurkat
human leukemic cells and PC3 human prostate cancer cells | Apoptosis
by increasing the mRNA stability of death Receptor 5 (DR5), a specific
receptor for tumor-necrosis factor-related apoptosis-inducing ligand (TRAIL) | PPAR antagonist GW9662 | [153] |
|
| PPAR ligands | | | |
| DEHP in mice | Induction of hepatic tumorigenesis | Wild-type and PPAR-null mice in comparison | [154] |
| WY14,643 in activated splenocytes isolated from C57BL/6 mice | Apoptosis | Wild-type and PPAR-null mice in comparison | [155] |
|
| PPAR/ ligands | | | |
| GW0742 in PPAR-null mouse model | Induction of keratinocyte terminal differentiation and inhibition of
keratinocyte proliferation | PPAR-null mice | [86] |
|
