Cholesterol metabolism. Effect of 26-thiacholesterol and 26-aminocholesterol, analogues of 26-hydroxycholesterol, on cholesterol synthesis and low-density-lipoprotein-receptor binding.
1. The effects of 26-aminocholesterol and 26-thiacholesterol on cholesterol synthesis and LDL (low-density lipoprotein)-receptor activity were compared with naturally occurring 26-hydroxycholesterol utilizing both human fibroblasts and hepatoma (Hep G2) cells. 2. At equimolar concentrations (0.625 microM), down-regulation of LDL-receptor activity and cholesterol synthesis was greater with human fibroblasts than with Hep G2 cells. 3. At much higher concentrations (5-20 microM) the 26-thia analogue had little effect on either cholesterol synthesis or LDL-receptor activity.
Miao
E
E
Department of Chemistry, New York University, NY 10003.
Wilson
S R
SR
Javitt
N B
NB
D000818:Animals; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000096:biosynthesis* / Q000494:pharmacology; D005347:Fibroblasts / Q000378:metabolism; D006801:Humans; D006888:Hydroxycholesterols / Q000494:pharmacology; D008077:Lipoproteins, LDL / Q000378:metabolism*; D008114:Liver Neoplasms, Experimental / Q000378:metabolism; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D018110:Receptors, Lipoprotein; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000378:metabolism
D006888:Hydroxycholesterols; D008077:Lipoproteins, LDL; D011956:Receptors, Cell Surface; D018110:Receptors, Lipoprotein; C058193:26-thiacholesterol; C007042:cholest-5-ene-3 beta,26-diol; C058194:26-aminocholesterol; D002784:Cholesterol