• Inhibitors as drug targets in the treatment of atherosclerosis
  • asal ahmadzadeh,1,* nafiseh ghorbani,2
    1. Department of Microbiology, Faculty of Basic Sciences, Lahijan Branch, Islamic Azad University, Lahijan, Iran.
    2. Department of Microbiology, Faculty of Basic Sciences, Lahijan Branch, Islamic Azad University, Lahijan, Iran.


  • Introduction: Cardiovascular disease (CVD) may begin in middle age. This disease is responsible for a third of all deaths globally (30% of men and 24% of women). Atherosclerosis is the major cause of cardiovascular disease. Atherosclerosis is a multifactorial and complex progression. It happens when the arteries become narrow and blood flow becomes difficult in them. Atherosclerosis increases the risk of heart attack and stroke. A persistent increase in circulating low-density lipoprotein (LDL) levels in the body is one of the most important causes of the initiation and progression of atherosclerosis. Cigarette smoking, diabetes mellitus, serum cholesterol, and hypertension, are associated with risk factors for atherosclerotic disease. It is known that enzymes are involved in many pathological conditions, such as inflammation, diabetes, microbial infections, HIV, neoplastic, neglected diseases, and others. Many drug molecules are enzyme inhibitors that inhibit an aberrant human enzyme. This study aims to review inhibitors as drug targets in the treatment of atherosclerosis
  • Methods: To study the inhibitors as drug targets in the treatment of atherosclerosis, this article summarizes currently available articles in MEDLINE, EMBASE, Scopus, and other databases about inhibitors and drugs in atherosclerosis treatment
  • Results: Cholesteryl ester transfer protein (CETP) is a plasma lipid transfer protein, responsible for moving cholesterol esters and triglycerides between lipoproteins. CETP inhibitors are the best choice in the treatment of atherosclerosis. Cholesterol acyltransferases (ACATs) are other targeted proteins for enzyme inhibition in atherosclerosis. These proteins are attached to the membrane and use long-chain fatty acyl-CoA and cholesterol as substrates to form cholesterol esters. Inhibition of ACAT1 may prevent the progression of atherosclerosis. Diglyceride acyltransferase (DGAT) enzymes are involved in triglyceride synthesis. Inhibition of this enzyme may reduce the risk of atherosclerosis. Microsomal triglyceride transfer protein (MTP) is a lipid transfer protein. This protein assembles very low-density lipoproteins. The inhibition of MTTP causes a reduction in plasma triglyceride levels which thereby reduces the risk of atherosclerosis. The key enzyme in cholesterol biosynthesis is squalene synthase and inhibitors of this enzyme suppress triglyceride biosynthesis. Furthermore, Diacylglycerol acyltransferases (DGAT) are the enzymes that catalyze the final step in the assembly of TAG, and Inhibition of DGAT may reduce the risk of atherosclerosis.
  • Conclusion: Based on my review many inhibitors can be used as drug targets in the treatment of atherosclerosis. Inhibitors of key enzyme reactions play a major role in the selection
  • Keywords: Inhibitors, drug targets, treatment, atherosclerosis, enzyme