ADMS 3502 Chapter Notes - Chapter 3.3: Reverse Cholesterol Transport, Pregnane, Guggulsterone
22 May 2020
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Document Summary
Controls cholesterol intestinal absorption, cholesterol catabolism, reverse cholesterol transport from peripheral tissues to liver for excretion of bile. One target of lxr is cyp7a1 which converts cholesterol to bile acids. Drug are entering clinical testing: promotes reverse cholesterol transport and reduces atherosclerosis in mice. Potential therapeutic target for controlling bile acid diarrhea. Regulates phase i and ii enzymes esp cyp3a4 and ugts (important for drug metabolism cyp3a4 metabolizes 50% of drugs in market; so altering it can lead to many ddi"s) Obeticholic acid (phase ii clinical trial for secondary bile acid malabsorption and chronic diarrhea) Rifampicin, phenobarbital, nifedipine, clotrimazole, ru486, tamoxifen, taxol, hyperforin (st. Guggulsterone (native herbal indian med; resin from commiphora mukul tree) Phenobarbitol (doesnt bind to car but activates it via phosphorylation - causing car to translocate to the nucleus and w/in the nucleus its going to be activated) But high conc of bile acids n bilirubin act as agonist. Steroid like androstanes act as inverse agonists.
