Table 2.
Potential effects of nuclear receptor ligands on osteosarcoma tumors.
Ligand | Experimental Setup | Effect | Mechanism | Reference | |
---|---|---|---|---|---|
PPARγ | Troglitazone | in vitro proliferation and apoptosis assays | inhibited proliferation | promotion of apoptosis, induce differentiation (alkaline phosphatase) | Haydon 2002, 2007 [9, 32] |
Ciglitazone | in vitro proliferation and apoptosis assays | minimal effect | unknown | Haydon2002 [32] | |
Troglitazone | in vitro MTT proliferation and apoptosis assays | increased proliferation | inhibition of apoptosis | Lucarelli 2002 [170] | |
Pioglitazone and PG J(2) | in vitro MTT and apoptosis assays of Chondrosarcoma Cells | inhibition of proliferation | promoted apoptosis | Nishida [171] | |
| |||||
Retinoic Acid | 9-cis retinoic acid | in vitro proliferation and apoptosis assays | inhibited proliferation | promotion of apoptosis | Haydon 2002, 2007 [9, 32] |
| |||||
Estrogen | 17-beta estradiol, Ospemifene | U2OS expressing ER, in vitro apoptosis assays | opposed Etoposide-induced cell death | oppose increases in IL-6 and decreases in OPG, preventing osteoclast activation | Kallio 2008 [172] |
Tamoxifen, Raloxifene | U2OS expressing ER, in vitro apoptosis assays | no effect on Etoposide-induced cell death | unknown | Kallio 2008 [172] | |
17-beta estradiol, SERMS (genistein, daidzein) | U2OS expressing ER, in vitro cell cycle, proliferation, apoptosis assays | inhibit proliferation, promote apoptosis | decrease EGFR, increased osteoblast maturation markers | Salvatori 2009 [173] | |
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Vitamin D | 1-alpha hydroxyvitamin D3 | oral administration in Dunn murine OS model | inhibits tumor growth and metastasis | increased necrosis, no cell cycle mitotic index effects | Hara 2001 [174] |
Prolactin + 1,25 (OH)2 Vitamin D3 | RT-PCR, western blots | PRL inhibits VDR expression in response to 1,25 (OH)2 Vitamin D3 | VDR expression is dependent on BRCA1 expression | Deng [175] | |
calcitriol | OS cells with increased RXR degradation, treated with calcitriol | increased expression of RXR restores anti-proliferative effects of calcitriol | calcitriol induced degradation is dependent on RXR expression | Prufer 2002 [176] |