ArticleBiochimica et biophysica acta. Molecular and cell biology of lipids2017
Assessing the mechanisms of cholesteryl ester transfer protein inhibitors.
Article in Biochimica et biophysica acta. Molecular and cell biology of lipids, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.
- Duration-dependent effects of water-only fasting on blood lipids: a systematic review, meta-analysis, and threshold meta-regression.Frontiers in nutrition · 2026Pooled it
- In silico discovery of CETP inhibitors from ZINC15 compounds using docking, ADMET filtering, and molecular dynamics simulations.Research in pharmaceutical sciences · 2026Article
- Phospholipids that Plug the Pores of Cholesteryl Ester Transfer Protein Control Its Triglyceride Transfer.Computational and structural biotechnology journal · 2026Article
- Imaging Lipid-Associated Macromolecular Structures by Optimized Negative-Staining Transmission Electron Microscopy.Methods in molecular biology (Clifton, N.J.) · 2026Article
- In Silico Strategies for Characterizing Inner Cavities of Lipid-Binding Proteins.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Chemical Synthesis, Biological Evaluation, and Cheminformatics Analysis of a Group of Chlorinated Diaryl Sulfonamides: Promising Inhibitors of Cholesteryl Ester Transfer Protein.Current computer-aided drug design · 2025Article
- Understanding the heterogeneity and dysfunction of HDL in chronic kidney disease: insights from recent reviews.BMC nephrology · 2024Review
- Zebrafish ApoB-Containing Lipoprotein Metabolism: A Closer Look.Arteriosclerosis, thrombosis, and vascular biology · 2024Review
- Triglyceride-Rich Lipoprotein Metabolism: Key Regulators of Their Flux.Journal of clinical medicine · 2023Review
- Structure-based mechanism and inhibition of cholesteryl ester transfer protein.Current atherosclerosis reports · 2023Review
- HDL and Cholesterol Ester Transfer Protein (CETP).Advances in experimental medicine and biology · 2022Article
- Single-Molecule 3D Images of "Hole-Hole" IgG1 Homodimers by Individual-Particle Electron Tomography.Scientific reports · 2019Article
- Optimized Negative-Staining Protocol for Lipid-Protein Interactions Investigated by Electron Microscopy.Methods in molecular biology (Clifton, N.J.) · 2019Article
- An Algorithm for Enhancing the Image Contrast of Electron Tomography.Scientific reports · 2018Article
- Clinical Pharmacokinetics and Pharmacodynamics of Dalcetrapib.Clinical pharmacokinetics · 2018Review
- Structural basis of the lipid transfer mechanism of phospholipid transfer protein (PLTP).Biochimica et biophysica acta. Molecular and cell biology of lipids · 2018Article
- Trials and Tribulations of CETP Inhibitors.Circulation research · 2018Review
Corrections and comments
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Authors and funding
10 authors at 5 institutions in 2 countries.
Funding
Abstract
Cholesteryl ester transfer protein (CETP) inhibitors are a new class of therapeutics for dyslipidemia that simultaneously improve two major cardiovascular disease (CVD) risk factors: elevated low-density lipoprotein (LDL) cholesterol and decreased high-density lipoprotein (HDL) cholesterol. However, the detailed molecular mechanisms underlying their efficacy are poorly understood, as are any potential mechanistic differences among the drugs in this class. Herein, we used electron microscopy (EM) to investigate the effects of three of these agents (Torcetrapib, Dalcetrapib and Anacetrapib) on CETP structure, CETP-lipoprotein complex formation and CETP-mediated cholesteryl ester (CE) transfer. We found that although none of these inhibitors altered the structure of CETP or the conformation of CETP-lipoprotein binary complexes, all inhibitors, especially Torcetrapib and Anacetrapib, increased the binding ratios of the binary complexes (e.g., HDL-CETP and LDL-CETP) and decreased the binding ratios of the HDL-CETP-LDL ternary complexes. The findings of more binary complexes and fewer ternary complexes reflect a new mechanism of inhibition: one distal end of CETP bound to the first lipoprotein would trigger a conformational change at the other distal end, thus resulting in a decreased binding ratio to the second lipoprotein and a degraded CE transfer rate among lipoproteins. Thus, we suggest a new inhibitor design that should decrease the formation of both binary and ternary complexes. Decreased concentrations of the binary complex may prevent the inhibitor was induced into cell by the tight binding of binary complexes during lipoprotein metabolism in the treatment of CVD.
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Registered trials
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