Cholesteryl ester transfer protein and its inhibitors.

Journal of Lipid Research
Sudichhya ShresthaKerry-Anne Rye

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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Citations

Feb 28, 2018·Journal of Lipid Research·Godfrey S Getz
May 8, 2019·European Journal of Preventive Cardiology·Cesare R SirtoriMassimiliano Ruscica
Mar 6, 2019·The Journal of Clinical Endocrinology and Metabolism·Maria Pia AdorniMassimiliano Ruscica
Jan 16, 2020·Expert Review of Cardiovascular Therapy·Shirya Rashid
Feb 5, 2019·Current Medicinal Chemistry·Eleni PappaVasilis K Tsimihodimos
Jun 15, 2018·Nutrients·Milessa Silva AfonsoAna Maria Lottenberg
Jun 25, 2020·Pharmaceutics·Choon Ok KimDong-Seok Yim
Dec 29, 2020·Clinica Chimica Acta; International Journal of Clinical Chemistry·Xin SuDong Chang
Sep 24, 2019·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Xinyu JiYongyan Wang
Jun 24, 2020·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Yihan ZhaoDazhuo Shi
Apr 4, 2021·International Journal of Molecular Sciences·Stanislav Kotlyarov
Sep 22, 2020·Cardiology in Review·Steven G Chrysant, George S Chrysant
Nov 16, 2021·International Reviews of Immunology·Azin AghamajidiNazanin Mojtabavi

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