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https://www.readbyqxmd.com/read/29038350/male-apoe-3-leiden-cetp-mice-on-high-fat-high-cholesterol-diet-exhibit-a-biphasic-dyslipidemic-response-mimicking-the-changes-in-plasma-lipids-observed-through-life-in-men
#1
Yared Paalvast, Albert Gerding, Yanan Wang, Vincent W Bloks, Theo H van Dijk, Rick Havinga, Ko Willems van Dijk, Patrick C N Rensen, Barbara M Bakker, Jan Albert Kuivenhoven, Albert K Groen
Physiological adaptations resulting in the development of the metabolic syndrome in man occur over a time span of several decades. This combined with the prohibitive financial cost and ethical concerns to measure key metabolic parameters repeatedly in subjects for the major part of their life span makes that comprehensive longitudinal human data sets are virtually nonexistent. While experimental mice are often used, little is known whether this species is in fact an adequate model to better understand the mechanisms that drive the metabolic syndrome in man...
October 2017: Physiological Reports
https://www.readbyqxmd.com/read/29035537/discovery-of-a-novel-piperidine-based-inhibitor-of-cholesteryl-ester-transfer-protein-cetp-that-retains-activity-in-hypertriglyceridemic-plasma
#2
Ken Yamada, Margaret Brousseau, Wataru Honma, Akiko Iimura, Hidetomo Imase, Yuki Iwaki, Toshio Kawanami, Daniel LaSala, Guiqing Liang, Hironobu Mitani, Kazuhiko Nonomura, Osamu Ohmori, Meihui Pan, Dean F Rigel, Ichiro Umemura, Kayo Yasoshima, Guoming Zhu, Muneto Mogi
Herein we describe the discovery and characterization of a novel, piperidine-based inhibitor of cholesteryl ester transfer protein (CETP) with a core structure distinct from other reported CETP inhibitors. A versatile synthesis starting from 4-methoxypyridine enabled an efficient exploration of the SAR, giving a lead molecule with potent CETP inhibition in human plasma. The subsequent optimization focused on improvement of pharmacokinetics and mitigation of off-target liabilities, such as CYP inhibition, whose improvement correlated with increased lipophilic efficiency...
October 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29018035/the-trials-and-tribulations-of-cetp-inhibitors
#3
Alan R Tall, Daniel J Rader
The development of CETP inhibitors has had a long and difficult course with three compounds failing in phase III clinical trials. Finally, the REVEAL trial has shown that the CETP inhibitor anacetrapib decreased coronary heart disease when added to statin therapy. While the result is different to earlier studies, this is likely related to the size and duration of the trial. The benefit of anacetrapib appears to be largely explained by lowering of non-HDL cholesterol, rather than increases in HDL cholesterol...
October 10, 2017: Circulation Research
https://www.readbyqxmd.com/read/28984832/the-role-of-omega-3-fatty-acids-in-reverse-cholesterol-transport-a-review
#4
REVIEW
Alex Pizzini, Lukas Lunger, Egon Demetz, Richard Hilbe, Guenter Weiss, Christoph Ebenbichler, Ivan Tancevski
The beneficial effects of omega-3 polyunsaturated fatty acids (n-3 PUFAs) on cardiovascular disease have been studied extensively. However, it remains unclear to what extent n-3 PUFAs may impact Reverse Cholesterol Transport (RCT). RCT describes a mechanism by which excess cholesterol from peripheral tissues is transported to the liver for hepatobiliary excretion, thereby inhibiting foam cell formation and the development of atherosclerosis. The aim of this review is to summarize the literature and to provide an updated overview of the effects of n-3 PUFAs on key players in RCT, including apoliprotein AI (apoA-I), ATP-binding cassette transporter A1 (ABCA1), ABCG1, apoE, scavenger receptor class B type I (SR-BI), cholesteryl ester transfer protein (CETP), low-density lipoprotein receptor (LDLr), cholesterol 7 alpha-hydroxylase (CYP7A1) and ABCG5/G8...
October 6, 2017: Nutrients
https://www.readbyqxmd.com/read/28980665/dyslipidaemia-revealing-the-effect-of-cetp-inhibition-in-cardiovascular-disease
#5
Michael V Holmes, George Davey Smith
No abstract text is available yet for this article.
November 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/28972557/design-synthesis-and-biological-evaluation-of-n-n-substituted-amine-derivatives-as-cholesteryl-ester-transfer-protein-inhibitors
#6
Xinran Wang, Lijuan Hao, Xuanqi Xu, Wei Li, Chunchi Liu, Dongmei Zhao, Maosheng Cheng
N,N-Substituted amine derivatives were designed by utilizing a bioisosterism strategy. Consequently, twenty-two compounds were synthesized and evaluated for their inhibitory activity against CETP. Structure-activity relationship (SAR) studies indicate that hydrophilic groups at the 2-position of the tetrazole and 3,5-bistrifluoromethyl groups on the benzene ring provide important contributions to the potency. Among these compounds, compound 17 exhibited excellent CETP inhibitory activity (IC50 = 0.38 ± 0.08 μM) in vitro...
October 3, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28972399/angptl3-serum-concentration-and-rare-genetic-variants-in-finnish-population
#7
Anna Tikka, Jari Metso, Matti Jauhiainen
Genetic variants of angiopoietin-like protein 3 (ANGPTL3) are associated with serum triglyceride (TG) and low-density lipoprotein cholesterol (LDL-C) concentration in GWASs. ANGPTL3 deficiency causes declined TG, total cholesterol (TC), LDL-C, high-density lipoprotein cholesterol (HDL-C), apolipoprotein B (apoB) and apolipoprotein A-I (apoA-I) serum concentration, a phenotype defined as familial combined hypolipidaemia (FHBL2). Our aim is to establish whether ANGPTL3 serum protein concentration correlates with lipoproteins and lipids in hyper- or hypolipidaemic subjects, and whether ANGPTL3 sequence variants are associated with untypical lipid profiles...
October 3, 2017: Scandinavian Journal of Clinical and Laboratory Investigation
https://www.readbyqxmd.com/read/28965203/assessment-of-carrot-callus-as-biofactories-of-an-atherosclerosis-oral-vaccine-prototype
#8
Dania O Govea-Alonso, Marlene A Tello-Olea, Josué Beltrán-López, Elizabeth Monreal-Escalante, Jorge A Salazar-Gonzalez, Bernardo Bañuelos-Hernández, Sergio Rosales-Mendoza
Atherosclerosis is a pathology leading to cardiovascular diseases with high epidemiologic impact; thus, new therapies are required to fight this global health issue. Immunotherapy is a feasible approach to treat atherosclerosis and given that genetically engineered plants are attractive hosts for vaccine development; we previously proved that the plant cell is able to synthesize a chimeric protein called CTB:p210:CETPe, which is composed of the cholera toxin B subunit (CTB) as immunogenic carrier and target epitopes from the cholesteryl ester transfer protein (CETP461-476) and apolipoprotein B100 (p210)...
September 30, 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/28961179/anacetrapib-a-new-cetp-inhibitor-the-new-tool-for-the-management-of-dyslipidemias
#9
REVIEW
Theodosios D Filippatos, Anastazia Kei, Moses S Elisaf
Cholesteryl ester transfer protein (CETP) inhibitors significantly increase serum high-density lipoprotein cholesterol (HDL) cholesterol levels and decrease low-density lipoprotein cholesterol (LDL) cholesterol concentration. However, three drugs of this class failed to show a decrease of cardiovascular events in high-risk patients. A new CETP inhibitor, anacetrapib, substantially increases HDL cholesterol and apolipoprotein (Apo) AI levels with a profound increase of large HDL2 particles, but also pre-β HDL particles, decreases LDL cholesterol levels mainly due to increased catabolism of LDL particles through LDL receptors, decreases lipoprotein a (Lp(a)) levels owing to a decreased Apo (a) production and, finally, decreases modestly triglyceride (TRG) levels due to increased lipolysis and increased receptor-mediated catabolism of TRG-rich particles...
September 29, 2017: Diseases (Basel)
https://www.readbyqxmd.com/read/28959945/cetp-inhibitors-stumble-on
#10
Asher Mullard
No abstract text is available yet for this article.
September 29, 2017: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/28953440/cetp-inhibitors-a-new-inning
#11
EDITORIAL
Robert A Hegele
New England Journal of Medicine, Volume 377, Issue 13, Page 1284-1285, September 2017.
September 28, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28948955/factors-affecting-high-density-lipoprotein-cholesterol-in-hiv-infected-patients-on-nevirapine-based-antiretroviral-therapy
#12
C Padmapriyadarsini, K Ramesh, L Sekar, Geetha Ramachandran, Devaraj Reddy, G Narendran, S Sekar, C Chandrasekar, D Anbarasu, Christine Wanke, Soumya Swaminathan
BACKGROUND & OBJECTIVES: Cardiovascular disease (CVD) risk with low high-density lipoprotein cholesterol (HDL-C) and high triglycerides is common in the general population in India. As nevirapine (NVP)-based antiretroviral therapy (ART) tends to increase HDL-C, gene polymorphisms associated with HDL-C metabolism in HIV-infected adults on stable NVP-based ART were studied. METHODS: A cross-sectional study was conducted between January 2013 and July 2014 among adults receiving NVP-based ART for 12-15 months...
May 2017: Indian Journal of Medical Research
https://www.readbyqxmd.com/read/28944433/pharmacogenetics-of-lipid-lowering-agents-an-update-review-on-genotype-dependent-effects-of-hdl-targetingand-statin-therapies
#13
REVIEW
Nathan Messas, Marie-Pierre Dubé, Jean-Claude Tardif
PURPOSE OF REVIEW: High-density lipoproteins (HDL) are involved in reverse cholesterol transport. Results from randomized trials of HDL-targeting therapies, including cholesteryl ester transfer protein (CETP) inhibitors, have shown a lack of benefit in unsegmented populations. These observations could be explained by inter-individual variability of clinical responses to such agents depending on the patients' genotypes. In parallel, although lowering of LDL cholesterol (LDL-c) with statin therapy reduces the risk of vascular events in a wide range of individuals, inter-individual variability exists with regard to LDL-c-lowering response as well as efficacy in reducing major cardiovascular events...
September 25, 2017: Current Atherosclerosis Reports
https://www.readbyqxmd.com/read/28918250/associations-of-cholesteryl-ester-transfer-protein-cetp-gene-variants-with-predisposition-to-age-related-macular-degeneration
#14
Rasa Liutkeviciene, Alvita Vilkeviciute, Greta Streleckiene, Loresa Kriauciuniene, Romanas Chaleckis, Vytenis Pranas Deltuva
PURPOSE: To determine the frequency of the genotypes of single nucleotide polymorphisms (SNPs) in the gene encoding cholesteryl ester transfer protein (CETP) and their associations with age-related macular degeneration (AMD) in the Lithuanian population. STUDY DESIGN: A total of 1264 subjects were examined: 251 patients with early AMD, 206 patients with exudative AMD, and 807 healthy controls. METHODS: The genotyping of CETP (rs5882, rs708272, rs3764261, rs1800775, rs2303790) was carried out using the RT-PCR...
December 15, 2017: Gene
https://www.readbyqxmd.com/read/28915626/hdl-cholesterol-concentration-in-pregnant-chinese-han-women-of-late-second-trimester-associated-with-genetic-variants-in-cetp-abca1-apoc3-and-galnt2
#15
Mingxuan Cui, Wei Li, Liangkun Ma, Fan Ping, Juntao Liu, Xueyan Wu, Jiangfeng Mao, Xi Wang, Min Nie
OBJECTIVE: To investigate whether HDL-C level in pregnant Chinese Han women of late second trimester correlated with loci in high-density lipoprotein-cholesterol (HDL-C)-related genes found in genome-wide association studies (GWAS). METHODS: Seven single-nucleotide polymorphisms (rs3764261 in CETP, rs1532085 in LIPC, rs7241918 in LIPG, rs1883025 in ABCA1, rs4225 in APOC3, rs1059611 in LPL, and rs16851339 in GALNT2) were genotyped using the Sequenom MassArray system for 1,884 pregnant women...
August 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28911944/assessing-the-mechanisms-of-cholesteryl-ester-transfer-protein-inhibitors
#16
Meng Zhang, Dongsheng Lei, Bo Peng, Mickey Yang, Lei Zhang, M Art Charles, Kerry-Anne Rye, Ronald M Krauss, Douglas G Johns, Gang Ren
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...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28906356/shared-polymorphisms-and-modifiable-behavior-factors-for-myocardial-infarction-and-high-cholesterol-in-a-retrospective-population-study
#17
Yulan Liang, Arpad Kelemen
Genetic and environmental (behavior, clinical, and demographic) factors are associated with increased risks of both myocardial infarction (MI) and high cholesterol (HC). It is known that HC is major risk factor that may cause MI. However, whether there are common single nucleotide polymorphism (SNPs) associated with both MI and HC is not firmly established, and whether there are modulate and modified effects (interactions of genetic and known environmental factors) on either HC or MI, and whether these joint effects improve the predictions of MI, is understudied...
September 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28902926/down-regulation-of-single-stranded-dna-binding-protein-1-expression-induced-by-hcmv-infection-promotes-lipid-accumulation-in-cells
#18
N Guo, N Zhang, L Yan, X Cao, F Lv, J Wang, Y Wang, H Cong
The objective of this study was to observe the infection of human cytomegalovirus (HCMV) to human umbilical vein endothelial cells, and its effect on the expression of single-stranded DNA-binding protein (SSBP1) and on lipid metabolism in endothelial cells. We screened the differential expression of mRNAs after HCMV infection by suppression subtractive hybridization and the expression levels of SSBP1 mRNA and protein after HCMV infection by real-time PCR and western blot. After verification of successful infection by indirect immunofluorescent staining and RT-PCR, we found a differential expression of lipid metabolism-related genes including LDLR, SCARB, CETP, HMGCR, ApoB and LPL induced by HCMV infection...
September 12, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28893253/a-novel-swine-model-for-evaluation-of-dyslipidemia-and-atherosclerosis-induced-by-human-cetp-overexpression
#19
Tao Chen, Meng Sun, Jia-Qiang Wang, Jin-Jin Cui, Zhong-Hua Liu, Bo Yu
BACKGROUND: The mechanism of cholesteryl ester transfer protein (CETP) in lipid metabolism is still unclear. Furthermore, the relationship of CETP and atherosclerosis (AS) has been controversial. As pigs are a good model for both lipid and AS research, we investigated the lipid metabolism of human CETP (hCETP) transgenic pigs and explored the mechanism of CETP in lipid modulation. METHODS: Plasmids expressing the hCETP gene were designed, successfully constructed, and transfected into porcine fetal fibroblasts by liposomes...
September 11, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28884824/pharmacokinetics-and-pharmacodynamics-of-anacetrapib-following-single-doses-in-healthy-young-japanese-and-white-male-subjects
#20
Rajesh Krishna, Ferdous Gheyas, Yang Liu, Josee Cote, Omar Laterza, Jon L Ruckle, John A Wagner, Andrew E Denker
Anacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor being developed for the treatment of mixed dyslipidemia. The aim of the study was to evaluate the pharmacokinetic, pharmacodynamic, and safety characteristics of anacetrapib following single doses in healthy, young Japanese men. In a double-blind, randomized, placebo-controlled, 3-panel, single-rising-dose study, 6 healthy young Japanese male or white male subjects (aged 19 to 44 years) received single oral doses of 5 to 500 mg anacetrapib, and 2 received placebo...
September 8, 2017: Journal of Clinical Pharmacology
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