Role of LXRs in control of lipogenesis

Genes and Development - Tập 14 Số 22 - Trang 2831-2838 - 2000
Joshua R. Schultz1, Hua Tu1, Alvin Luk1, Joyce J. Repa2, Julio C. Medina1, Leping Li, Susan W. Schwendner1, Shelley Wang1, Martin Thoolen1, David J. Mangelsdorf2,1, Kevin D. Lustig1, Bei Shan1
1Tularik, Inc., South San Francisco, California 94080, USA
2Howard Hughes Medical Institute and Department of Pharmacology, University of Texas Southwestern Medical Center, Dallas, Texas 75390, USA

Tóm tắt

The discovery of oxysterols as the endogenous liver X receptor (LXR) ligands and subsequent gene targeting studies in mice provided strong evidence that LXR plays a central role in cholesterol metabolism. The identification here of a synthetic, nonsteroidal LXR-selective agonist series represented by T0314407 and T0901317 revealed a novel physiological role of LXR. Oral administration of T0901317 to mice and hamsters showed that LXR activated the coordinate expression of major fatty acid biosynthetic genes (lipogenesis) and increased plasma triglyceride and phospholipid levels in both species. Complementary studies in cell culture and animals suggested that the increase in plasma lipids occurs via LXR-mediated induction of the sterol regulatory element-binding protein 1 (SREBP-1) lipogenic program.

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