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Glycogen synthase kinase-3: a new therapeutic target in renal cell carcinoma
1Department of Urology, Yamagata University School of Medicine, Iida-nishi 2-2-2, Yamagata 990-9585, Japan.
Background:
Renal cell carcinoma (RCC) is highly resistant to chemotherapy because of a high apoptotic threshold. Recent evidences suggest that GSK-3beta positively regulates human pancreatic cancer and leukaemia cell survival in part through regulation of nuclear factor (NF-kappaB)-mediated expression of anti-apoptotic molecules. Our objectives were to determine the expression pattern of GSK-3beta and to assess the anti-cancer effect of GSK-3beta inhibition in RCC.
Methods:
Immunohistochemistry and nuclear/cytosolic fractionation were performed to determine the expression pattern of GSK-3beta in human RCCs. We used small molecule inhibitor, RNA interference, western blotting, quantitative RT-PCR, BrDU incorporation and MTS assays to study the effect of GSK-3beta inactivation on renal cancer cell proliferation and survival.
Results:
We detected aberrant nuclear accumulation of GSK-3beta in RCC cell lines and in 68 out of 74 (91.89%) human RCCs. We found that pharmacological inhibition of GSK-3 led to a decrease in proliferation and survival of renal cancer cells. We observed that inhibition of GSK-3 results in decreased expression of NF-kappaB target genes Bcl-2 and XIAP and a subsequent increase in renal cancer cell apoptosis. Moreover, we show that GSK-3 inhibitor and Docetaxel synergistically suppress proliferation and survival of renal cancer cells.
Conclusions:
Our results show nuclear accumulation of GSK-3beta as a new marker of human RCC, identify that GSK-3 positively regulates RCC cell survival and proliferation and suggest inhibition of GSK-3 as a new promising approach in the treatment of human renal cancer.
Insights
Inhibiting GSK-3beta, a protein found to accumulate in renal cell carcinoma (RCC), decreases cancer cell survival and proliferation. This suggests targeting GSK-3beta is a promising new strategy for treating RCC.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Renal cell carcinoma (RCC) exhibits resistance to chemotherapy due to a high apoptotic threshold.
- Glycogen synthase kinase 3 beta (GSK-3beta) is implicated in cancer cell survival via nuclear factor-kappaB (NF-kappaB) signaling.
- Understanding GSK-3beta's role in RCC is crucial for developing new therapeutic strategies.
Purpose of the Study:
- To determine the expression pattern of GSK-3beta in human RCC.
- To evaluate the anti-cancer effects of inhibiting GSK-3beta in RCC.
Main Methods:
- Immunohistochemistry and subcellular fractionation to assess GSK-3beta expression.
- Pharmacological inhibition and RNA interference to study GSK-3beta's effects.
- Cell proliferation and apoptosis assays (MTS, BrDU) and molecular analyses (Western blot, RT-PCR).
Main Results:
- Aberrant nuclear accumulation of GSK-3beta was observed in 91.89% of human RCC samples.
- GSK-3beta inhibition reduced renal cancer cell proliferation and survival.
- Inhibition decreased NF-kappaB target genes (Bcl-2, XIAP), increasing apoptosis.
- GSK-3beta inhibitor and Docetaxel showed synergistic effects.
Conclusions:
- Nuclear GSK-3beta accumulation serves as a novel biomarker for human RCC.
- GSK-3beta positively regulates RCC cell survival and proliferation.
- Inhibiting GSK-3beta represents a promising therapeutic approach for renal cancer treatment.
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