Polyisoprenoid amphiphilic compounds as inhibitors of squalene synthesis and other microsomal enzymes.
Analogues of farnesyl pyrophosphate containing a farnesyl moiety and a variety of amine residues replacing the pyrophosphate have been synthesized. Most of these compounds were effective inhibitors of the synthesis of squalene and presqualene pyrophosphate from farnesyl pyrophosphate. 50% inhibition was obtained at concentrations between 50 and 100 micron. These analogues also inhibited other microsomal enzymes so they apparently function as general inhibitors of microsomal enzymes.
D003579:Cytochrome Reductases / Q000037:antagonists & inhibitors; D005204:Farnesol / Q000031:analogs & derivatives* / Q000494:pharmacology; D005952:Glucose-6-Phosphatase / Q000037:antagonists & inhibitors; D007535:Isomerases / Q000378:metabolism; D007810:Lanosterol; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D011106:Polyisoprenyl Phosphates / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000378:metabolism*; D013185:Squalene / Q000031:analogs & derivatives / Q000096:biosynthesis*; D013329:Structure-Activity Relationship
D011106:Polyisoprenyl Phosphates; D007810:Lanosterol; D005204:Farnesol; D013185:Squalene; D003579:Cytochrome Reductases; D005952:Glucose-6-Phosphatase; D007535:Isomerases