sr9243 and Weight-Loss

sr9243 has been researched along with Weight-Loss* in 1 studies

Other Studies

1 other study(ies) available for sr9243 and Weight-Loss

Article	Year
Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer cell, 2015, Jul-13, Volume: 28, Issue:1 Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress. The nuclear receptor liver-X-receptor (LXR) directly regulates expression of key glycolytic and lipogenic genes. To disrupt these oncogenic metabolism pathways, we designed an LXR inverse agonist SR9243 that induces LXR-corepressor interaction. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression. SR9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Our results suggest that LXR inverse agonists may be an effective cancer treatment approach. Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Glycolysis; Hep G2 Cells; HT29 Cells; Humans; Lipogenesis; Liver X Receptors; Mice; Molecular Targeted Therapy; Neoplasms; Organ Specificity; Orphan Nuclear Receptors; Small Molecule Libraries; Sulfonamides; Weight Loss; Xenograft Model Antitumor Assays	2015

Article

Year

Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis.

Cancer cell, 2015, Jul-13, Volume: 28, Issue:1

Malignant cells exhibit aerobic glycolysis (the Warburg effect) and become dependent on de novo lipogenesis, which sustains rapid proliferation and resistance to cellular stress. The nuclear receptor liver-X-receptor (LXR) directly regulates expression of key glycolytic and lipogenic genes. To disrupt these oncogenic metabolism pathways, we designed an LXR inverse agonist SR9243 that induces LXR-corepressor interaction. In cancer cells, SR9243 significantly inhibited the Warburg effect and lipogenesis by reducing glycolytic and lipogenic gene expression. SR9243 induced apoptosis in tumors without inducing weight loss, hepatotoxicity, or inflammation. Our results suggest that LXR inverse agonists may be an effective cancer treatment approach.

Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Glycolysis; Hep G2 Cells; HT29 Cells; Humans; Lipogenesis; Liver X Receptors; Mice; Molecular Targeted Therapy; Neoplasms; Organ Specificity; Orphan Nuclear Receptors; Small Molecule Libraries; Sulfonamides; Weight Loss; Xenograft Model Antitumor Assays

2015