AI Article Synopsis
- The majority of cholesterol in the bloodstream is in an esterified form, primarily produced by cardioprotective high-density lipoproteins (HDLs).
- Cholesteryl ester transfer protein (CETP) plays a key role in transferring cholesteryl esters and triglycerides between different lipoproteins, leading to a net movement of cholesterol out of HDLs, which could affect cardiovascular risk.
- Efforts to inhibit CETP activity have led to the creation of various treatments like monoclonal antibodies and small molecule inhibitors, with ongoing research into their effectiveness in reducing cardiovascular disease through large-scale clinical trials.
Article Abstract
Most of the cholesterol in plasma is in an esterified form that is generated in potentially cardioprotective HDLs. Cholesteryl ester transfer protein (CETP) mediates bidirectional transfers of cholesteryl esters (CEs) and triglycerides (TGs) between plasma lipoproteins. Because CE originates in HDLs and TG enters the plasma as a component of VLDLs, activity of CETP results in a net mass transfer of CE from HDLs to VLDLs and LDLs, and of TG from VLDLs to LDLs and HDLs. As inhibition of CETP activity increases the concentration of HDL-cholesterol and decreases the concentration of VLDL- and LDL-cholesterol, it has the potential to reduce atherosclerotic CVD. This has led to the development of anti-CETP neutralizing monoclonal antibodies, vaccines, and antisense oligonucleotides. Small molecule inhibitors of CETP have also been developed and four of them have been studied in large scale cardiovascular clinical outcome trials. This review describes the structure of CETP and its mechanism of action. Details of its regulation and nonlipid transporting functions are discussed, and the results of the large scale clinical outcome trials of small molecule CETP inhibitors are summarized.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5928430 | PMC |
| http://dx.doi.org/10.1194/jlr.R082735 | DOI Listing |
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