BIOL 3051 Chapter Notes - Chapter 6.0: Drug Metabolism, Fatty Acid Metabolism, Peroxisome Proliferator-Activated Receptor
24 Apr 2020
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Xenobiotic metabolism: lxr is responsible for cholesterol metabolism thus tissue distribution in: liver, intestine, macrophages, ligand of lxr are sterols: epoxycholesterol, hydroxycholesterol, with hydroxyl group, targets genes of lxr receptor: Cholesterol trafficking cholesterol ester transfer protein, apoe. Cholesterol efflux abca1, abcg5/g68: lxr regulates bile acid synthesis b/c cholesterol is metabolized to bile acids to be removed from system. Cholesterol metabolized to bile acid: lxr involved in cholesterol efflux. If too much cholesterol inside cell, it will regulate expression of transporter that efflux cholesterol. Lxr knockout: no synthesis of bile acids from excess cholesterol. Adopted orphans common themes: ligand are: Binds to receptors at micromolar concentrations (less potent than steroids which are nanomolar: regulates feedforward metabolic cascades, protect body against toxic, lipophilic molecules. Xenobiotics: ex: ppars bind to fatty acid, promote fatty acid oxidation (breakdown) But most binding regions in introns: hormone response elements for nuclear receptor binding in various regions.
