Affinage

CETP

Cholesteryl ester transfer protein · UniProt P11597

Length
493 aa
Mass
54.8 kDa
Annotated
2026-04-28
100 papers in source corpus 21 papers cited in narrative 21 extracted findings

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

CETP is a secreted plasma glycoprotein that mediates the bidirectional transfer of cholesteryl esters and triglycerides between HDL and apoB-containing lipoproteins (VLDL/LDL), thereby serving as a central regulator of plasma lipoprotein remodeling, HDL metabolism, and reverse cholesterol transport. Transcription of CETP is driven by LXRα/RXR heterodimers binding a DR4 element in the promoter in response to sterols, with LXRα—not LXRβ—being the essential subtype (PMID:10683381, PMID:20494359); adipose tissue and liver are the principal sources of circulating CETP (PMID:16751623, PMID:9712344). Functionally, CETP accelerates hepatic HDL-cholesteryl ester uptake, delays postprandial triglyceride-rich lipoprotein clearance in part by suppressing LPL expression, and preferentially acts on HDL3 through modulation by lipid transfer inhibitor protein (LTIP) (PMID:16806230, PMID:19191759, PMID:12907677). Loss-of-function mutations (including premature stop codons and splice-site variants) cause primary hyperalphalipoproteinemia, and alternatively spliced Δ9 isoforms act as dominant-negative inhibitors of CETP secretion, linking common intronic/exonic polymorphisms to elevated HDL-C (PMID:18926541, PMID:22403620).

Mechanistic history

Synthesis pass · year-by-year structured walk · 14 steps
  1. 1998 Medium

    Establishing that adipose tissue is a physiologically important source of plasma CETP resolved where the circulating protein originates beyond the liver.

    Evidence Correlation of adipose CETP mRNA with plasma CETP concentration (r=0.85) in two human cohorts using ex vivo organ culture

    PMID:9712344

    Open questions at the time
    • Correlational design; no causal manipulation of adipose CETP in humans
    • Relative hepatic vs. adipose contribution not quantified in the same subjects
  2. 2000 High

    Identification of the DR4 element and LXR/RXR-dependent sterol-responsive transcription of CETP established the core transcriptional control mechanism linking dietary cholesterol to plasma CETP levels.

    Evidence Promoter-luciferase mutagenesis, EMSA, and transgenic mice with normal vs. mutated CETP promoter

    PMID:10683381

    Open questions at the time
    • Other transcription factors acting on the CETP promoter not characterized
    • Tissue-specific differences in LXR-dependent regulation not resolved
  3. 2003 High

    Demonstrating that LTIP modulates CETP substrate specificity—stimulating CE transfer from HDL3 while suppressing it from HDL2—explained the observed in vivo HDL-subclass selectivity of CETP.

    Evidence Reconstituted in vitro CE transfer assays with radiolabeled substrates and multiple lipoprotein fractions

    PMID:12907677

    Open questions at the time
    • In vivo relevance of LTIP modulation not tested in animal models
    • Structural basis of LTIP–CETP interaction unknown
  4. 2005 Medium

    The finding that apoCI-induced hyperlipidemia overrides apoCI's direct CETP inhibition via LXR-mediated CETP gene induction revealed a feedback loop in which substrate accumulation amplifies CETP expression.

    Evidence Double-transgenic (CETPTg/apoCITg) mice with hepatic gene expression and plasma CE transfer activity measurements

    PMID:15339254

    Open questions at the time
    • Precise LXR ligand(s) generated by apoCI-induced hyperlipidemia not identified
    • Relevance to human apoCI–CETP axis not confirmed
  5. 2006 High

    Adipose-specific CETP transgenic mice proved causally that adipose-derived CETP contributes substantially to circulating CETP mass and produces systemic lipoprotein remodeling (reduced HDL-C, increased non-HDL cholesterol).

    Evidence Adipose-tissue-specific transgenic mouse model with plasma CETP mass/activity and lipoprotein profiling

    PMID:16751623

    Open questions at the time
    • Quantitative contribution of adipose vs. hepatic CETP in humans remains unresolved
  6. 2006 High

    Radiolabeled HDL-CE kinetic studies in CETP transgenic mice demonstrated that CETP accelerates hepatic (and other tissue) CE uptake without altering VLDL secretion or biliary excretion, defining the catabolic arm of CETP's effect on HDL.

    Evidence In vivo isotopic HDL-CE kinetics in CETP transgenic vs. non-transgenic mice with tissue uptake measurements

    PMID:16806230

    Open questions at the time
    • Receptor(s) mediating enhanced hepatic CE uptake in the presence of CETP not identified
    • Biliary cholesterol secretion pathway may differ in humans
  7. 2008 High

    Discovery and functional characterization of alternatively spliced CETP isoforms (Δ9 and Alu-exon insertions) that are secretion-incompetent and act as dominant-negative inhibitors of wild-type CETP secretion revealed a post-transcriptional layer of CETP regulation and linked CETP expression to ER stress.

    Evidence Cell-based secretion assays, Western blot, ER stress gene induction; variant activity reconstitution; human liver mRNA quantification

    PMID:18468607 PMID:18509195 PMID:22403620

    Open questions at the time
    • Physiological triggers that shift the splicing ratio in vivo are unknown
    • ER stress induction mechanism by CETP variants not elucidated
  8. 2008 High

    Identification of loss-of-function CETP mutations (Q165X, R268X, IVS15+2T>C) causing hyperalphalipoproteinemia in Italian subjects, with functional validation by minigene assays, established that CETP deficiency is a Mendelian cause of elevated HDL-C in Europeans as well as Asians.

    Evidence CETP gene sequencing, minigene splicing assay in COS-1 cells, plasma CETP activity measurement

    PMID:18926541

    Open questions at the time
    • Cardiovascular outcome in European CETP-deficient subjects not resolved
    • Compound heterozygote phenotypes not characterized
  9. 2009 High

    Showing that CETP delays postprandial TG-rich lipoprotein clearance both by remodeling remnant composition and by suppressing LPL expression/activity explained CETP's proatherogenic role beyond HDL lowering.

    Evidence Oral fat load kinetics, double-labeled chylomicron-like emulsion clearance, post-heparin LPL activity, and adipose LPL mRNA in CETP transgenic mice

    PMID:19191759

    Open questions at the time
    • Mechanism by which CETP reduces LPL transcription is not defined
    • Human postprandial studies with CETP inhibitors needed for translation
  10. 2010 High

    Establishing that LXRα—not LXRβ—is the obligate mediator of sterol-responsive CETP transcription refined the transcriptional model and identified a druggable regulatory node.

    Evidence siRNA knockdown in HepG2 cells plus LXRα-knockout CETP transgenic mice

    PMID:20494359

    Open questions at the time
    • Whether LXRα-selective agonists differentially regulate CETP in human liver is untested
  11. 2015 High

    Dissection of anacetrapib's dual mechanism—CETP-dependent VLDL remodeling plus CETP-independent PCSK9/LDL-receptor regulation—revealed that pharmacological CETP inhibitors have off-target effects on hepatic cholesterol homeostasis.

    Evidence Anacetrapib treatment in E3L.CETP and E3L (non-CETP) transgenic mice; liver microarray; ChIP for SREBP on PCSK9 promoter; VLDL clearance assays

    PMID:26015437 PMID:26342106

    Open questions at the time
    • CETP-independent PCSK9-lowering mechanism of anacetrapib not fully resolved at the molecular level
    • Translation to human hepatocytes awaits confirmation
  12. 2016 Medium

    Demonstrating that CETP lowers TLR4 expression and NF-κB activation in macrophages and endothelial cells, improving sepsis survival, uncovered a direct anti-inflammatory function independent of lipoprotein remodeling.

    Evidence CETP transgenic mice in CLP sepsis model; recombinant CETP added to macrophages; TLR4/NF-κB/IL-6 measurements

    PMID:27293313

    Open questions at the time
    • Mechanism by which CETP reduces TLR4 expression is unknown
    • Single-lab finding; not independently replicated
  13. 2021 Medium

    In vivo stable-isotope tracer kinetics resolved that CETP is secreted into and circulates predominantly on alpha1 and alpha2 HDL subfractions, providing a biophysical framework for its site of action in lipoprotein remodeling.

    Evidence Stable isotope tracer kinetics with targeted mass spectrometry and compartmental modeling in 6 human participants

    PMID:33351780

    Open questions at the time
    • Small sample size (n=6)
    • Whether CETP's HDL subfraction distribution changes in dyslipidemia is unknown
  14. 2022 Medium

    Showing that macrophage CETP expression reduces mitochondrial ROS, promotes mitochondrial fusion (via mitofusin-2/OPA1), and enhances HDL-mediated cholesterol efflux extended CETP's intracellular functions to mitochondrial dynamics and oxidative stress regulation.

    Evidence CETP transgenic mouse macrophages and CETP-knockdown THP1 cells; mitochondrial respiration/ROS assays; cholesterol efflux; gene expression

    PMID:36139808

    Open questions at the time
    • Mechanism linking CETP to mitofusin-2 induction unknown
    • Single-lab finding; no independent replication
    • Physiological relevance of macrophage-endogenous CETP expression in humans unclear

Open questions

Synthesis pass · forward-looking unresolved questions
  • Key unresolved questions include the structural basis of CETP's interaction with specific HDL subclasses and LTIP, the molecular mechanism by which CETP suppresses LPL and TLR4 expression, and whether the intracellular (ER stress, mitochondrial) functions of CETP are physiologically significant in humans.
  • No high-resolution structure of CETP bound to HDL or LTIP
  • Mechanism of LPL transcriptional suppression by CETP undefined
  • Intracellular CETP functions tested only in transgenic models and cell lines

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0008289 lipid binding 3 GO:0016740 transferase activity 3
Localization
GO:0005576 extracellular region 4 GO:0005783 endoplasmic reticulum 2
Pathway
R-HSA-1430728 Metabolism 4 R-HSA-382551 Transport of small molecules 4 R-HSA-74160 Gene expression (Transcription) 3 R-HSA-168256 Immune System 1
Partners
APOA1APOC1LPLLXRAMFN2RXRA

Evidence

Reading pass · 21 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2000 The CETP gene is transcriptionally upregulated by dietary sterols via a DR4 (direct repeat-4) nuclear receptor binding element in its promoter (-384 to -399). LXR/RXR heterodimers bind this element and transactivate the CETP promoter in a sterol-responsive fashion, as demonstrated by promoter mutagenesis, gel retardation assays, and transgenic mouse studies with normal or mutated promoter sequences. Promoter-luciferase reporter assay, promoter mutagenesis, gel retardation/EMSA, transgenic mouse models with normal vs. mutated CETP promoter The Journal of clinical investigation High 10683381
2010 LXRα (but not LXRβ) is the essential subtype mediating LXR-dependent CETP transcriptional regulation. LXRα knockdown in HepG2 cells abolished LXR-agonist-induced CETP expression, and LXRα-deficient CETP transgenic mice failed to upregulate plasma CETP activity or hepatic CETP expression in response to synthetic LXR agonist, whereas LXRβ deficiency had no effect. siRNA knockdown in HepG2 cells, LXRα/LXRβ knockout CETP transgenic mice, CETP promoter-reporter assays Atherosclerosis High 20494359
2003 Lipid transfer inhibitor protein (LTIP) modulates CETP-mediated lipid transfer in an HDL-subclass-specific manner: LTIP suppresses CETP activity on HDL2 and LDL while stimulating CETP activity on HDL3, resulting in a strong CETP preference for HDL3. TG enrichment of HDL2 further abolishes LTIP's stimulatory effect, keeping CETP activity on HDL2 low. In vitro CETP-mediated cholesteryl ester transfer assays with [3H]CE-labeled VLDL and various lipoprotein substrates; long-term mass transfer experiments The Journal of biological chemistry High 12907677
2006 Adipose tissue is a major source of circulating CETP. Adipose-tissue-specific CETP transgenic mice with predominant adipose CETP mRNA expression showed readily detectable plasma CETP mass and activity, marked reductions in HDL cholesterol and apoA-I, and increases in non-HDL lipids and apoB, demonstrating that adipose-derived CETP makes a major contribution to circulating CETP and its lipoprotein-remodeling effects. Adipose-tissue-specific transgenic mouse model; plasma CETP mass and activity assays; lipoprotein analysis; adipocyte size and lipid content measurements; gene expression analysis Journal of lipid research High 16751623
1998 Adipose tissue CETP mRNA levels are strongly correlated with plasma CETP concentrations (r=0.85, P<0.002) in humans, indicating that adipose tissue is a significant contributor to the plasma pool of CETP. CETP mRNA abundance in adipose tissue is negatively correlated with adipocyte size (TG-poor adipocytes express more CETP). Pericardiac adipose tissue CETP mRNA measurement (organ culture, correlation with plasma CETP); subcutaneous adipose tissue from healthy females; organ culture secretion assays Atherosclerosis Medium 9712344
2006 CETP expression in transgenic mice accelerates HDL cholesteryl ester (CE) fractional catabolic rate and enhances CE uptake by liver, adrenals, adipose tissue, and spleen. HDL fractions from both CETP transgenic and non-transgenic mice are cleared faster from plasma of CETP-expressing mice, indicating a direct role of CETP in accelerating tissue CE uptake independent of HDL particle origin. However, CETP expression does not alter hepatic VLDL-cholesterol/TG output or biliary lipid/fecal bile acid excretion. Radiolabeled HDL-CE kinetic studies in CETP transgenic vs. non-transgenic mice; hepatic VLDL secretion rate measurements; biliary lipid and fecal bile acid assays Atherosclerosis High 16806230
2009 CETP expression in transgenic mice delays postprandial plasma clearance of triglyceride-rich lipoproteins by two mechanisms: (1) transferring TG to HDL and enriching remnant particles with CE, making them less susceptible to LPL-mediated lipolysis; and (2) reducing LPL expression and activity (~50% reduction in post-heparin plasma LPL activity and ~39% reduction in adipose LPL mRNA). Oral fat load postprandial TG curves; double-labeled chylomicron-like emulsion kinetics; VLDL secretion assay; post-heparin LPL activity; adipose LPL mRNA; CETP-Tg vs. non-Tg mice The Biochemical journal High 19191759
2012 CETP polymorphisms affecting mRNA splicing have functional consequences: an alternatively spliced isoform lacking exon 9 (Δ9) prevents CETP secretion in a dominant-negative manner. rs9930761 (intron 8) alters a key splicing branch point nucleotide and rs5883 (exon 9) alters an exonic splicing enhancer sequence, together increasing Δ9 isoform formation (10–48% of total CETP mRNA in human livers), independently raising HDL-C and influencing cardiovascular risk. Allelic CETP mRNA expression in 56 human livers; splice isoform measurements; SNP genotyping; functional association in Whitehall II (n=4745) and INVEST-GENE cohorts PloS one High 22403620
2008 Novel alternatively spliced CETP isoforms (skipping exon 9 sequences with insertion of Alu-derived in-frame exons) are not efficiently secreted and co-expression of them inhibits wild-type CETP secretion in a dominant-negative manner. Expression of all CETP variants (including wild-type) induces ER stress responses, suggesting CETP plays a role in modulating ER stress independent of its lipid transfer activity. Cell expression studies of splice variants; Western blot of secretion efficiency; ER stress gene induction assays Journal of lipid research Medium 18509195
2008 CETP variants found in Asian individuals (Y332, Q296, G442) are secreted less efficiently than wild-type protein but retain significant cholesteryl ester transfer activity in vitro, while P151 variant is not secreted and shows no transfer activity. A null splice variant causing protein truncation was found in Europeans on the same haplotype as in Asians, suggesting common origin. In vitro secretion efficiency by Western blot; fluorescent substrate CE transfer activity assay; exon resequencing Atherosclerosis Medium 18468607
2008 Novel CETP loss-of-function mutations (Q165X, R268X introducing premature stop codons; IVS15+2T>C abolishing a splice donor site) cause reduced CETP activity (38–60% reduction) and primary hyperalphalipoproteinemia in Italian subjects. Minigene analysis in COS-1 cells showed the IVS15+2T>C mutation causes exon 14–16 direct joining, producing a truncated 435-amino acid peptide. CETP gene sequencing; minigene splicing assay in COS-1 cells; plasma CETP activity assay Atherosclerosis High 18926541
2016 CETP expression in macrophages and endothelial cells lowers TLR4 expression and NF-κB activation, reducing LPS uptake, TLR4-dependent signaling, and IL-6 secretion. In transgenic mice, CETP expression improves survival in polymicrobial sepsis (CLP model) and reduces plasma IL-6. Recombinant human CETP added to wild-type macrophages recapitulates these effects. CETP transgenic mice CLP sepsis model; macrophage LPS stimulation with/without recombinant CETP; TLR4/NF-κB/IL-6 measurements; survival analysis Mediators of inflammation Medium 27293313
2021 CETP expression in endothelial cells generates vascular oxidative stress and endothelial dysfunction. CETP transgenic mice show impaired acetylcholine-induced endothelium-dependent relaxation, increased superoxide and H2O2 production in aortas, and enhanced eNOS activation. Silencing CETP in human aortic endothelial cells reduces mitochondrial and NOX2-derived ROS, decreases ER stress markers, lowers TNFα, ICAM-1, and VCAM-1 expression, and reduces monocyte adhesion. Aortic ring relaxation assay in CETP transgenic mice; ROS measurement; eNOS activation assay; CETP siRNA knockdown in human endothelial cells; ER stress marker analysis; monocyte adhesion assay Biomolecules Medium 33430172
2022 CETP expression in macrophages reduces mitochondrial superoxide and H2O2 production, increases maximal mitochondrial respiration, promotes mitochondrial network elongation (increased mitofusin-2 and OPA1 expression), attenuates pro-inflammatory gene expression and phagocytic activity, reduces unesterified cholesterol accumulation under basal conditions and after oxidized-LDL exposure, and enhances HDL-mediated cholesterol efflux. CETP knockdown in THP1 cells increased unesterified cholesterol and abolished mitofusin-2 and TNFα effects. CETP transgenic mouse macrophages vs. non-transgenic; mitochondrial ROS/respiration assays; gene expression; CETP knockdown in THP1 cells; cholesterol efflux assay Antioxidants (Basel, Switzerland) Medium 36139808
2014 HDL isolated from carriers of CETP null mutations (genetic CETP deficiency) is significantly less effective than control HDL in stimulating nitric oxide (NO) production in endothelial cells due to reduced eNOS-activating capacity, likely because of reduced sphingosine-1-phosphate (S1P) content in structurally altered HDL particles. However, CETP-deficient HDL retains the ability to downregulate cytokine-induced VCAM-1 expression. HDL isolation from CETP-deficient human subjects; eNOS activation and NO production assays in cultured endothelial cells; VCAM-1 expression assays; S1P content analysis PloS one Medium 24830642
2021 Using in vivo stable isotope tracer studies and compartmental modeling, CETP is secreted mainly in alpha1 and alpha2 HDL subfractions and remains in these sizes during circulation (unlike PLTP which transfers between HDL sizes). CETP metabolism on multiple HDL sizes was resolved by targeted mass spectrometry on the Orbitrap Fusion Lumos. In vivo stable isotope tracer kinetics; targeted mass spectrometry (Orbitrap Fusion Lumos); compartmental modeling of CETP on HDL subfractions from 6 participants JCI insight Medium 33351780
2007 Atorvastatin increases HDL-cholesterol in CETP-expressing (E3L.CETP) but not in non-CETP-expressing (E3L) mice by reducing hepatic CETP mRNA expression (-57%), lowering total plasma CETP mass (-29%) and CE transfer activity (-36%), thereby reducing CETP-dependent transfer of cholesterol from HDL to (V)LDL. Atorvastatin treatment of E3L and E3L.CETP transgenic mice; hepatic CETP mRNA quantification; plasma CETP mass and activity assays; lipoprotein cholesterol analysis Atherosclerosis Medium 17868678
2015 Anacetrapib reduces (V)LDL cholesterol by two CETP-related and CETP-independent mechanisms: (1) inhibition of CETP activity producing remodeled VLDL particles more susceptible to hepatic uptake; and (2) CETP-independent downregulation of hepatic PCSK9 expression (-28%), resulting in reduced plasma PCSK9 (-47%), increased hepatic LDL receptor content (+64%), and accelerated VLDL clearance. The PCSK9-lowering effect was confirmed in E3L mice lacking CETP. Anacetrapib treatment in E3L.CETP and E3L (non-CETP) transgenic mice; liver microarray; hepatic Pcsk9 and LDLr expression; plasma PCSK9 measurement; [14C]cholesteryl-oleate VLDL-mimicking particle clearance assay Journal of lipid research High 26342106
2018 CETP inhibition with anacetrapib in high-fat-diet-fed CETP transgenic mice improves HDL functionality (reverse cholesterol transport, antioxidative capacity) but worsens anti-inflammatory HDL capacity, markedly alters the HDL proteome, and causes hepatic triglyceride accumulation and insulin resistance, revealing context-dependent (obese vs. lean) effects of CETP inhibition. Anacetrapib treatment in chow- and HFD-fed CETP transgenic mice; reverse cholesterol transport assay; HDL antioxidative and anti-inflammatory capacity assays; HDL proteomics; liver TG measurement; insulin resistance assessment Diabetes Medium 30213825
2015 Novel CETP inhibitor K-312 decreases PCSK9 expression in human primary hepatocytes and HepG2 cells by a CETP-independent mechanism: it reduces active forms of SREBP-1 and SREBP-2 and decreases their occupancy on the sterol regulatory element of the PCSK9 promoter, as demonstrated by chromatin immunoprecipitation. CETP siRNA silencing did not abolish PCSK9 suppression by K-312. In vitro human primary hepatocyte and HepG2 cell assays; CETP siRNA knockdown; SREBP Western blot; chromatin immunoprecipitation (ChIP); PCSK9 protein measurement in rabbit blood by mass spectrometry American journal of physiology. Endocrinology and metabolism Medium 26015437
2005 Apolipoprotein CI (apoCI) is a potent inhibitor of CETP specific activity in plasma. However, apoCI overexpression in CETP transgenic mice paradoxically increases total plasma CE transfer activity because the resulting hyperlipidemia activates LXR, upregulating hepatic CETP mRNA ~4-fold and CETP mass ~3-fold, demonstrating that LXR-mediated CETP gene induction can override pharmacological inhibition of specific CETP activity. CETPTg/apoCITg double transgenic mice; plasma CE transfer activity assays; hepatic CETP mRNA measurement; LXR-target gene expression (ABCG5, SREBP-1c) The Biochemical journal Medium 15339254

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2000 Sterol upregulation of human CETP expression in vitro and in transgenic mice by an LXR element. The Journal of clinical investigation 285 10683381
2017 Association of Genetic Variants Related to CETP Inhibitors and Statins With Lipoprotein Levels and Cardiovascular Risk. JAMA 250 28846118
2017 Trials and Tribulations of CETP Inhibitors. Circulation research 221 29018035
2004 A review of CETP and its relation to atherosclerosis. Journal of lipid research 204 15342674
2012 Genetic inhibition of CETP, ischemic vascular disease and mortality, and possible adverse effects. Journal of the American College of Cardiology 129 23083790
2003 The safety and immunogenicity of a CETP vaccine in healthy adults. Atherosclerosis 108 12860257
2021 Cholesteryl ester transfer protein (CETP) as a drug target for cardiovascular disease. Nature communications 95 34561430
2007 Atorvastatin increases HDL cholesterol by reducing CETP expression in cholesterol-fed APOE*3-Leiden.CETP mice. Atherosclerosis 67 17868678
2018 Association of CETP Gene Variants With Risk for Vascular and Nonvascular Diseases Among Chinese Adults. JAMA cardiology 61 29141072
2012 New molecular insights into CETP structure and function: a review. Journal of lipid research 60 22679067
2013 Future of cholesteryl ester transfer protein (CETP) inhibitors: a pharmacological perspective. Clinical pharmacokinetics 57 23658137
2006 Cholesteryl ester transfer protein (CETP) inhibition beyond raising high-density lipoprotein cholesterol levels: pathways by which modulation of CETP activity may alter atherogenesis. Arteriosclerosis, thrombosis, and vascular biology 57 16439711
2016 CETP Inhibition: Past Failures and Future Hopes. Clinical Medicine Insights. Cardiology 56 26997876
2004 CETP gene variation: relation to lipid parameters and cardiovascular risk. Current opinion in lipidology 56 15243211
2012 Cholesteryl Ester Transfer Protein (CETP) polymorphisms affect mRNA splicing, HDL levels, and sex-dependent cardiovascular risk. PloS one 54 22403620
2019 Akkermansia muciniphila Exerts Lipid-Lowering and Immunomodulatory Effects without Affecting Neointima Formation in Hyperlipidemic APOE*3-Leiden.CETP Mice. Molecular nutrition & food research 53 31389129
2000 Taq1B CETP polymorphism, plasma CETP, lipoproteins, apolipoproteins and sex differences in a Jewish population sample characterized by low HDL-cholesterol. Atherosclerosis 51 10924728
2016 Association and interaction of APOA5, BUD13, CETP, LIPA and health-related behavior with metabolic syndrome in a Taiwanese population. Scientific reports 49 27827461
2011 Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction. Clinical pharmacology and therapeutics 49 22130116
2018 Therapy with cholesteryl ester transfer protein (CETP) inhibitors and diabetes risk. Diabetes & metabolism 47 29523487
2022 Joint Genetic Inhibition of PCSK9 and CETP and the Association With Coronary Artery Disease: A Factorial Mendelian Randomization Study. JAMA cardiology 46 35921096
2017 Dyslipidaemia: Revealing the effect of CETP inhibition in cardiovascular disease. Nature reviews. Cardiology 45 28980665
2014 APOE*3Leiden.CETP transgenic mice as model for pharmaceutical treatment of the metabolic syndrome. Diabetes, obesity & metabolism 45 24373179
2005 Cholesteryl ester transfer protein (CETP) I405V polymorphism and longevity in Italian centenarians. Mechanisms of ageing and development 45 15888337
1998 Relationship of adipose tissue cholesteryl ester transfer protein (CETP) mRNA to plasma concentrations of CETP in man. Atherosclerosis 45 9712344
2014 Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. British journal of clinical pharmacology 44 24628035
2003 Lipid transfer inhibitor protein defines the participation of high density lipoprotein subfractions in lipid transfer reactions mediated by cholesterol ester transfer protein (CETP). The Journal of biological chemistry 44 12907677
2014 Cholesteryl ester transfer protein (CETP) deficiency and CETP inhibitors. Molecules and cells 43 25410905
2007 Cholesteryl ester transfer protein (CETP) expression protects against diet induced atherosclerosis in SR-BI deficient mice. Arteriosclerosis, thrombosis, and vascular biology 43 17272756
2015 CETP/LPL/LIPC gene polymorphisms and susceptibility to age-related macular degeneration. Scientific reports 42 26503844
2023 Obicetrapib: Reversing the Tide of CETP Inhibitor Disappointments. Current atherosclerosis reports 41 38133847
2005 The association of common SNPs and haplotypes in the CETP and MDR1 genes with lipids response to fluvastatin in familial hypercholesterolemia. Atherosclerosis 41 16002074
2001 Influence of CETP gene variation on plasma lipid levels and coronary heart disease: a survey in Taiwan. Atherosclerosis 40 11730826
1994 Competitive enzyme-linked immunosorbent assay of the human cholesteryl ester transfer protein (CETP). Clinica chimica acta; international journal of clinical chemistry 40 7889597
2002 Lipoprotein lipase deficiency and CETP in streptozotocin-treated apoB-expressing mice. Journal of lipid research 39 12032161
2013 CETP gene polymorphisms and risk of coronary atherosclerosis in a Chinese population. Lipids in health and disease 38 24283500
2008 HDL metabolism and CETP inhibition. Cardiology in review 38 18414186
2004 Role of CETP inhibitors in the treatment of dyslipidemia. Current opinion in lipidology 37 15529021
2015 New CETP inhibitor K-312 reduces PCSK9 expression: a potential effect on LDL cholesterol metabolism. American journal of physiology. Endocrinology and metabolism 36 26015437
1989 "Variability gene" effect of cholesteryl ester transfer protein (CETP) genes. Clinical genetics 36 2567644
2022 The effect of CETP inhibitors on new-onset diabetes: a systematic review and meta-analysis. European heart journal. Cardiovascular pharmacotherapy 35 35441656
2008 PXR agonism decreases plasma HDL levels in ApoE3-Leiden.CETP mice. Biochimica et biophysica acta 35 19150509
2016 Genetic variants in CETP increase risk of intracerebral hemorrhage. Annals of neurology 34 27717122
2006 Atherosclerosis is enhanced by testosterone deficiency and attenuated by CETP expression in transgenic mice. Journal of lipid research 34 16603720
2016 CETP Lowers TLR4 Expression Which Attenuates the Inflammatory Response Induced by LPS and Polymicrobial Sepsis. Mediators of inflammation 33 27293313
2006 Adipose tissue-specific CETP expression in mice: impact on plasma lipoprotein metabolism. Journal of lipid research 33 16751623
2006 Inhibition of CETP as a novel therapeutic strategy for reducing the risk of atherosclerotic disease. European heart journal 33 17121756
2020 A Novel Role for CETP as Immunological Gatekeeper: Raising HDL to Cure Sepsis? Trends in endocrinology and metabolism: TEM 32 32033866
2018 CETP Inhibition Improves HDL Function but Leads to Fatty Liver and Insulin Resistance in CETP-Expressing Transgenic Mice on a High-Fat Diet. Diabetes 32 30213825
2018 Mendelian randomization reveals unexpected effects of CETP on the lipoprotein profile. European journal of human genetics : EJHG 31 30420679
2016 Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach. ACS medicinal chemistry letters 31 26985312
2010 LXRalpha regulates human CETP expression in vitro and in transgenic mice. Atherosclerosis 31 20494359
2009 The end of the road for CETP inhibitors after torcetrapib? Current opinion in cardiology 31 19522058
2001 ApoA-II expression in CETP transgenic mice increases VLDL production and impairs VLDL clearance. Journal of lipid research 31 11181754
2018 Plasma lipid transfer proteins: The role of PLTP and CETP in atherogenesis. Advances in clinical and experimental medicine : official organ Wroclaw Medical University 29 29558025
2014 Elevated cholesteryl ester transfer protein (CETP) activity, a major determinant of the atherogenic dyslipidemia, and atherosclerotic cardiovascular disease in South Asians. European journal of preventive cardiology 29 24659026
2014 eNOS activation by HDL is impaired in genetic CETP deficiency. PloS one 29 24830642
2010 Update on CETP inhibition. Journal of clinical lipidology 28 21122682
2015 Anacetrapib reduces (V)LDL cholesterol by inhibition of CETP activity and reduction of plasma PCSK9. Journal of lipid research 27 26342106
2009 Taq1B polymorphism of cholesteryl ester transfer protein (CETP) gene in primary combined hyperlipidaemia. The Indian journal of medical research 26 19491422
2021 The Presence of Cholesteryl Ester Transfer Protein (CETP) in Endothelial Cells Generates Vascular Oxidative Stress and Endothelial Dysfunction. Biomolecules 25 33430172
2019 Dose Effects of Ammonium Perfluorooctanoate on Lipoprotein Metabolism in APOE*3-Leiden.CETP Mice. Toxicological sciences : an official journal of the Society of Toxicology 25 30657992
2012 Xanthohumol prevents atherosclerosis by reducing arterial cholesterol content via CETP and apolipoprotein E in CETP-transgenic mice. PloS one 25 23166663
2006 High-density genotyping and functional SNP localization in the CETP gene. Journal of lipid research 25 17108362
2018 Inflammatory cytokine oncostatin M induces endothelial activation in macro- and microvascular endothelial cells and in APOE*3Leiden.CETP mice. PloS one 24 30273401
2017 CETP: Pharmacogenomics-Based Response to the CETP Inhibitor Dalcetrapib. Arteriosclerosis, thrombosis, and vascular biology 24 28126828
2014 Serum cholesterol and variant in cholesterol-related gene CETP predict white matter microstructure. Neurobiology of aging 24 24997672
2009 Co-administration of a CpG adjuvant (VaxImmune, CPG 7909) with CETP vaccines increased immunogenicity in rabbits and mice. Human vaccines 24 18670196
2006 Effects of cholesterol ester transfer protein (CETP) gene on adiposity in response to long-term overfeeding. Atherosclerosis 24 17196207
2000 Genetic polymorphisms and activity of cholesterol ester transfer protein (CETP): should we be measuring them? Clinical chemistry and laboratory medicine 24 11140626
2022 A Nutrigenetic Update on CETP Gene-Diet Interactions on Lipid-Related Outcomes. Current atherosclerosis reports 23 35098451
2017 Evacetrapib: Another CETP Inhibitor for Dyslipidemia With No Clinical Benefit. Cardiology in review 23 28099220
2008 Cholesteryl ester transfer protein (CETP) genetic variation and early onset of non-fatal myocardial infarction. Annals of human genetics 23 18637884
2008 Novel mutations of CETP gene in Italian subjects with hyperalphalipoproteinemia. Atherosclerosis 23 18926541
2022 Novel Role of CETP in Macrophages: Reduction of Mitochondrial Oxidants Production and Modulation of Cell Immune-Metabolic Profile. Antioxidants (Basel, Switzerland) 22 36139808
2006 CETP expression enhances liver HDL-cholesteryl ester uptake but does not alter VLDL and biliary lipid secretion. Atherosclerosis 22 16806230
2013 The promise of cholesteryl ester transfer protein (CETP) inhibition in the treatment of cardiovascular disease. Current pharmaceutical design 20 23317399
2009 Cholesterol ester transfer protein (CETP), postprandial lipemia and hypolipidemic drugs. Current medicinal chemistry 20 19835569
2018 Relationship between CETP gene polymorphisms with coronary artery disease in Polish population. Molecular biology reports 19 30178218
2008 Cholesteryl ester transfer protein (CETP) inhibitors: is there life after torcetrapib? Cardiology clinics 19 18929230
2005 Apolipoprotein CI overexpression is not a relevant strategy to block cholesteryl ester transfer protein (CETP) activity in CETP transgenic mice. The Biochemical journal 19 15339254
2017 Associations of cholesteryl ester transfer protein (CETP) gene variants with predisposition to age-related macular degeneration. Gene 18 28918250
2009 Cholesteryl ester transfer protein (CETP) increases postprandial triglyceridaemia and delays triacylglycerol plasma clearance in transgenic mice. The Biochemical journal 18 19191759
2008 Expression of CETP and of splice variants induces the same level of ER stress despite secretion efficiency differences. Journal of lipid research 18 18509195
2023 Combined GIP receptor and GLP1 receptor agonism attenuates NAFLD in male APOE∗3-Leiden.CETP mice. EBioMedicine 17 37379656
2017 Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias? Diseases (Basel, Switzerland) 17 28961179
2014 Production of a plant-derived immunogenic protein targeting ApoB100 and CETP: toward a plant-based atherosclerosis vaccine. Molecular biotechnology 17 25143122
2010 Gene-environment interactions of CETP gene variation in a high cardiovascular risk Mediterranean population. Journal of lipid research 17 20581105
1995 CETP and LCAT activities are unrelated to smoking and moderate alcohol consumption in healthy normolipidemic men. Japanese circulation journal 17 7474298
2024 Obicetrapib-the Rebirth of CETP Inhibitors? Current atherosclerosis reports 16 39150671
2021 Metabolism of PLTP, CETP, and LCAT on multiple HDL sizes using the Orbitrap Fusion Lumos. JCI insight 16 33351780
2018 The therapeutic potential of CETP inhibitors: a patent review. Expert opinion on therapeutic patents 16 29424255
2014 Relationships between CETP genetic polymorphisms and Alzheimer's disease risk: a meta-analysis. DNA and cell biology 16 25105518
2009 Cholesteryl ester transfer protein (CETP) inhibitors. Current topics in medicinal chemistry 16 19519458
2021 Interaction between CETP polymorphism and dietary insulin index and load in relation to cardiovascular risk factors in diabetic adults. Scientific reports 15 34354158
2022 Can we revive CETP-inhibitors for the prevention of cardiovascular disease? Current opinion in lipidology 14 36345867
2017 Association between Six CETP Polymorphisms and Metabolic Syndrome in Uyghur Adults from Xinjiang, China. International journal of environmental research and public health 14 28629169
2009 Two novel mutations and functional analyses of the CETP and LIPC genes underlying severe hyperalphalipoproteinemia. Metabolism: clinical and experimental 14 19428034
2008 Frequency and function of CETP variants among individuals of Asian ancestry. Atherosclerosis 14 18468607
2021 Cannabinoid type 1 receptor inverse agonism attenuates dyslipidemia and atherosclerosis in APOE∗3-Leiden.CETP mice. Journal of lipid research 13 33766515