Critical role of cholesterol transfer protein in atherosclerosis development


  • D. A. Dorovsky National University of Pharmacy, Ukraine
  • A. L. Zagayko National University of Pharmacy, Ukraine



CETP, lipoproteins, atherosclerosis


Cholesterol ester transfer protein (CETP) is a plasma protein that facilitates the transport of cholesterol esters and triglicerides between the lipoproteins. CETP collects triglycerides from very-low-density lipoproteins (VLDL) or low-density lipoproteins (LDL) and exchanges them for cholesterol esters from high-density lipoproteins (HDL). Mutations wich lead to the cholesterol ester transfer protein function reduction have been involved in atherosclerosis development. This mutations also increase the prevalence of coronary heart disease in patients with hypertriglyceridemia. There is a wide variety of HDL-C increase therapies that have been tested during the last ten years. Among them is the modification of cholesterol ester transfer protein function. A novel pharmacologic strategy was proposed where drugs are designed to modify the lipid substrate preference of cholesterol ester transfer protein instead of simply blocking its activity. This approach provides an opportunity to improve the lipid transfer properties of cholesterol ester transfer protein and to harness its capacity to alter lipid metabolism to achieve specific beneficial outcomes.


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