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Regulation of Expression of Sterol Regulatory Element-binding Protein 1 in Thyroid Cancer Cells

Background/aim: Expression of sterol regulatory element-binding protein 1 (SREBP1) is upregulated in thyroid cancer and associated with shorter disease-specific survival. The molecular regulatory mechanisms governing SREBP1 over-expression in thyroid cancer are still unclear.

Materials and methods: Thyroid cancer cell lines BHT-101 (with the BRAF V600E mutation) and FTC-131 (wild-type for BRAF) were treated with specific inhibitors. The expression of SREBP1 was determined at the mRNA level using quantitative real-time PCR and at the protein level using immunoblotting.

Results: Lenvatinib and a MEK inhibitor, selumetinib, suppressed SREBP1 expression in BHT-101 but not FTC-133 cells. Olitigaltin, a galectin-3 inhibitor, decreased SREBP1 expression in a time- and dose-dependent manner in both cells. MK2206, an allosteric AKT inhibitor, did not change SREBP1 expression in either cell line.

Conclusion: The galectin-3 inhibitor attenuates SREBP1 expression in thyroid cancer cells, likely independent of AKT phosphorylation. Lenvatinib and selumetinib decreases SREBP1 expression in the BRAF-mutant cell line BHT-101.

Related Products

Cat.No. Product Name Information
S0471 Olitigaltin (TD-139) Olitigaltin (TD-139, GB0-139) is a potent and selective inhibitor of galectin-3 with Kd of 0.036 µM over galectin-1 and galectin-7 with Kd of 2.2 µM and 32 µM, respectively. TD-139 is used potentially for the treatment of idiopathic pulmonary fibrosis (IPF).

Related Targets

Galectin