ArticleJournal of lipid research2010
Biochemical characterization of cholesteryl ester transfer protein inhibitors.
Article in Journal of lipid research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 96 citations in OpenAlex.
- Cholesteryl Ester Transfer Protein Inhibition With Anacetrapib Decreases Fractional Clearance Rates of High-Density Lipoprotein Apolipoprotein A-I and Plasma Cholesteryl Ester Transfer Protein.Arteriosclerosis, thrombosis, and vascular biology · 2016Trial
- Effect of hepatic and renal impairment on the pharmacokinetics of dalcetrapib: altered distribution of the active thiol?Clinical pharmacokinetics · 2013Trial
- Article
- Clinical Pharmacokinetics and Pharmacodynamics of Dalcetrapib.Clinical pharmacokinetics · 2018Review
- Cholesteryl ester transfer protein and its inhibitors.Journal of lipid research · 2018Review
- Beneficial Effects of Monascus sp. KCCM 10093 Pigments and Derivatives: A Mini Review.Molecules (Basel, Switzerland) · 2018Review
- Assessing the mechanisms of cholesteryl ester transfer protein inhibitors.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2017Article
- Anti-Aging and Tissue Regeneration Ability of Policosanol Along with Lipid-Lowering Effect in Hyperlipidemic Zebrafish via Enhancement of High-Density Lipoprotein Functionality.Rejuvenation research · 2016Article
- Evaluation of CETP activity in vivo under non-steady-state conditions: influence of anacetrapib on HDL-TG flux.Journal of lipid research · 2016Article
- Indolinyl-Thiazole Based Inhibitors of Scavenger Receptor-BI (SR-BI)-Mediated Lipid Transport.ACS medicinal chemistry letters · 2015Article
- Modification of CETP function by changing its substrate preference: a new paradigm for CETP drug design.Journal of lipid research · 2015Article
- How anacetrapib inhibits the activity of the cholesteryl ester transfer protein? Perspective through atomistic simulations.PLoS computational biology · 2014Article
- Arginine-directed glycation and decreased HDL plasma concentration and functionality.Nutrition & diabetes · 2014Article
- Monogenic causes of elevated HDL cholesterol and implications for development of new therapeutics.Clinical lipidology · 2013Article
- Pharmacotherapies for lipid modification: beyond the statins.Nature reviews. Cardiology · 2013Review
- Antisense oligonucleotide inhibition of cholesteryl ester transfer protein enhances RCT in hyperlipidemic, CETP transgenic, LDLr-/- mice.Journal of lipid research · 2013Article
- In vivo effects of anacetrapib on preβ HDL: improvement in HDL remodeling without effects on cholesterol absorption.Journal of lipid research · 2013Article
- Targeting high density lipoproteins in the prevention of cardiovascular disease?Current cardiology reports · 2012Review
- Crystal structures of cholesteryl ester transfer protein in complex with inhibitors.The Journal of biological chemistry · 2012Article
- Cholesteryl ester transfer protein inhibition as a strategy to reduce cardiovascular risk.Journal of lipid research · 2012Review
Corrections and comments
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Authors and funding
21 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cholesteryl ester transfer protein (CETP) has been identified as a novel target for increasing HDL cholesterol levels. In this report, we describe the biochemical characterization of anacetrapib, a potent inhibitor of CETP. To better understand the mechanism by which anacetrapib inhibits CETP activity, its biochemical properties were compared with CETP inhibitors from distinct structural classes, including torcetrapib and dalcetrapib. Anacetrapib and torcetrapib inhibited CETP-mediated cholesteryl ester and triglyceride transfer with similar potencies, whereas dalcetrapib was a significantly less potent inhibitor. Inhibition of CETP by both anacetrapib and torcetrapib was not time dependent, whereas the potency of dalcetrapib significantly increased with extended preincubation. Anacetrapib, torcetrapib, and dalcetrapib compete with one another for binding CETP; however anacetrapib binds reversibly and dalcetrapib covalently to CETP. In addition, dalcetrapib was found to covalently label both human and mouse plasma proteins. Each CETP inhibitor induced tight binding of CETP to HDL, indicating that these inhibitors promote the formation of a complex between CETP and HDL, resulting in inhibition of CETP activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.