Natural products as starting materials for development of second-generation SERCA inhibitors targeted towards prostate cancer cells

2006 ◽  
Vol 14 (8) ◽  
pp. 2810-2815 ◽  
Author(s):  
Helmer Søhoel ◽  
Anne-Marie Lund Jensen ◽  
Jesper V. Møller ◽  
Poul Nissen ◽  
Samuel R. Denmeade ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Natural Products ◽  
Cancer Cells ◽  
Second Generation ◽  
Prostate Cancer Cells

scholarly journals Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells

2016 ◽  
Vol 76 (9) ◽  
pp. 2731-2742 ◽  
Author(s):  
Roberta Ferraldeschi ◽  
Jonathan Welti ◽  
Marissa V. Powers ◽  
Wei Yuan ◽  
Tomoko Smyth ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptor ◽  
Cancer Cells ◽  
Second Generation ◽  
Hsp90 Inhibitor ◽  
Mrna Splicing ◽  
Prostate Cancer Cells

A key regulator of cholesterol homoeostasis, SREBP-2, can be targeted in prostate cancer cells with natural products

2012 ◽  
Vol 446 (2) ◽  
pp. 191-201 ◽  
Author(s):  
James R. Krycer ◽  
Lisa Phan ◽  
Andrew J. Brown
Keyword(s):  
Prostate Cancer ◽  
Natural Products ◽  
Cell Viability ◽  
Cancer Treatment ◽  
Cancer Cells ◽  
Tree Bark ◽  
Prostate Cancer Cells ◽  
Prostate Cancer Treatment ◽  
Cholesterol Levels ◽  
Birch Tree

There is growing evidence showing that prostate cancer cells have perturbed cholesterol homoeostasis, accumulating cholesterol to promote cell growth. Consequently, cholesterol-lowering drugs such as statins are being evaluated in prostate cancer treatment. Furthermore, natural products such as betulin (from birch tree bark) and tocotrienol (a minor form of vitamin E) have been shown to lower cholesterol levels. Using these drugs and oxysterols, we have determined which aspects of cholesterol homoeostasis should be targeted in prostate cancer, e.g. cellular cholesterol levels are increased by the transcription factor SREBP-2 (sterol-regulatory-element-binding protein isoform 2), whereas LXR (liver X receptor) promotes cholesterol efflux. Whereas betulin exerted non-specific effects on cell viability, tocotrienols produced a strong direct correlation between SREBP-2 activity and cell viability. Mechanistically, tocotrienols lowered SREBP-2 activity by degrading mature SREBP-2 independently of the proteasome. In contrast, no correlation was seen between LXR activity and cell viability, implying that SREBP-2 is a better target than LXR for prostate cancer treatment. Lastly, androgen-dependent and -independent LNCaP cells were both sensitive to tocotrienols. Overall, this suggests that tocotrienols and other drugs targeting the SREBP-2 pathway are a potential therapeutic option for prostate cancer.

279: Inhibition of Cyclooxygenase-2 Pathway Overcomes the Heat-Resistance in Prostate Cancer Cells

2007 ◽  
Vol 177 (4S) ◽  
pp. 93-93
Author(s):  
Makoto Sumitomo ◽  
Kenji Kuroda ◽  
Takako Asano ◽  
Akio Horiguchi ◽  
Keiichi Ito ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Heat Resistance ◽  
Cancer Cells ◽  
Cyclooxygenase 2 ◽  
Prostate Cancer Cells
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