Trials and tribulations of CETP inhibitors

AR Tall, DJ Rader - Circulation research, 2018 - Am Heart Assoc
The development of CETP (cholesteryl ester transfer protein) inhibitors has had a long and
difficult course with 3 compounds failing in phase III clinical trials. Finally, the REVEAL …

Triglyceride-rich lipoprotein metabolism: key regulators of their flux

A Gugliucci - Journal of Clinical Medicine, 2023 - mdpi.com
The residual risk for arteriosclerotic cardiovascular disease after optimal statin treatment
may amount to 50% and is the consequence of both immunological and lipid disturbances …

Structure-based mechanism and inhibition of cholesteryl ester transfer protein

H Xue, M Zhang, J Liu, J Wang, G Ren - Current Atherosclerosis Reports, 2023 - Springer
Abstract Purpose of Review Cholesteryl ester transfer proteins (CETP) regulate plasma
cholesterol levels by transferring cholesteryl esters (CEs) among lipoproteins. Lipoprotein …

Deciphering structural aspects of reverse cholesterol transport: mapping the knowns and unknowns

S Sacher, A Mukherjee, A Ray - Biological Reviews, 2023 - Wiley Online Library
Atherosclerosis is a major contributor to the onset and progression of cardiovascular
disease (CVD). Cholesterol‐loaded foam cells play a pivotal role in forming atherosclerotic …

A novel role for CETP as immunological gatekeeper: raising HDL to cure sepsis?

LL Blauw, Y Wang, KW van Dijk… - Trends in Endocrinology & …, 2020 - cell.com
Raising HDL using cholesteryl ester transfer protein (CETP) inhibitors failed to show a
clinically relevant risk reduction of cardiovascular disease in clinical trials, inviting …

Invention of MK-8262, a cholesteryl ester transfer protein (CETP) inhibitor backup to anacetrapib with best-in-class properties

P Vachal, JL Duffy, LC Campeau… - Journal of Medicinal …, 2021 - ACS Publications
Cholesteryl ester transfer protein (CETP) represents one of the key regulators of the
homeostasis of lipid particles, including high-density lipoprotein (HDL) and low-density …

Cholesteryl ester transfer protein: an enigmatic pharmacology–antagonists and agonists

S Yamashita, M Ruscica, C Macchi, A Corsini… - Atherosclerosis, 2018 - Elsevier
The cholesteryl ester transfer protein (CETP) system moves cholesteryl esters (CE) from
high density lipoproteins (HDL) to lower density lipoproteins, ie very low-density lipoprotein …

HDL and cholesterol ester transfer protein (CETP)

S Deng, J Liu, C Niu - HDL Metabolism and Diseases, 2022 - Springer
Cholesterol ester transfer protein (CETP) is important clinically and is one of the major
targets in cardiovascular disease studies. With high conformational flexibility, its tunnel …

Structural basis of the lipid transfer mechanism of phospholipid transfer protein (PLTP)

M Zhang, X Zhai, J Li, JJ Albers, S Vuletic… - Biochimica et Biophysica …, 2018 - Elsevier
Human phospholipid transfer protein (PLTP) mediates the transfer of phospholipids among
atheroprotective high-density lipoproteins (HDL) and atherogenic low-density lipoproteins …

Zebrafish ApoB-Containing Lipoprotein Metabolism: A Closer Look

TOC Moll, SA Farber - Arteriosclerosis, Thrombosis, and Vascular …, 2024 - Am Heart Assoc
Zebrafish have become a powerful model of mammalian lipoprotein metabolism and lipid
cell biology. Most key proteins involved in lipid metabolism, including cholesteryl ester …