[MTP inhibitors and ACAT inhibitors. An update].

Abstract

Currently, statin therapy is the first-line treatment for patients with hypercholesterolemia, although their effects on plasma triglyceride(TG) levels are modest and variable. Inhibition of microsomal triglyceride transfer protein(MTP), a key protein involved in the assembly of the apoB-containing lipoproteins, is an attractive lipid-lowering strategy. In animal models, MTP inhibitors have dramatic effects not only on plasma cholesterol and LDL levels but on TG levels as well, offering the potential for greater efficacy and plasma lipid control in both hypertriglyceridemia and mixed hyperlipidemia. Inhibitors of acyl-CoA: cholesterol acyltransferase(ACAT) present another strategy in treating atherosclerosis through direct inhibition of ACAT in macrophages of the arterial wall. Recent studies in mouse models of atherosclerosis lacking ACAT1, however, may argue against the selective inhibition of macrophage ACAT1.

• Authors: Ken Ohashi
• Journal: Nihon rinsho. Japanese journal of clinical medicine (Nihon Rinsho) Vol. 60 Issue 5 Pg. 975-83 (May 2002) ISSN: 0047-1852 [Print] Japan
• PMID: 12030002 (Publication Type: English Abstract, Journal Article, Review)

Chemical References

• Carrier Proteins
• Hypolipidemic Agents
• microsomal triglyceride transfer protein
• Sterol O-Acyltransferase

Topics

• Animals
• Arteriosclerosis (drug therapy)
• Carrier Proteins (antagonists & inhibitors)
• Humans
• Hypercholesterolemia (drug therapy)
• Hyperlipidemias (drug therapy)
• Hypolipidemic Agents (therapeutic use)
• Mice
• Sterol O-Acyltransferase (antagonists & inhibitors)