Selective ACAT Inhibitors as Promising Antihyperlipidemic, Antiatherosclerotic and Anti-Alzheimer Drugs

摘要: Inhibition of ACAT, the enzyme which catalyses intracellular formation cholesteryl esters, is a very attractive target for treatment hypercholesterolaemia and atherosclerosis. However, in past years many ACAT inhibitors gave disappointing results clinical trials showing low efficacy. In addition, their development was affected by adrenotoxicity observed compounds. The discovery two isoforms enzyme, namely ACAT1 ACAT2, with different substrate specificity potential function, offers precious information planning selective reduced secondary effects. Today some potent, bioavailable non adrenotoxic are under evaluation. Amongst others, promising compound Avasimibe, presently phase III as anti-hyperlipidemic anti-atherosclerotic agent. Finally, have recently been proposed Alzheimer's disease.