Proteins > Cholesteryl ester transfer protein
Page last updated: 2024-08-07 15:55:26
Cholesteryl ester transfer protein
A cholesteryl ester transfer protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11597]
Synonyms
Lipid transfer protein I
Research
Bioassay Publications (25)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (40.00) | 29.6817 |
| 2010's | 12 (48.00) | 24.3611 |
| 2020's | 3 (12.00) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.ACS medicinal chemistry letters, , Jun-13, Volume: 10, Issue:6, 2019
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein.ACS medicinal chemistry letters, , Jun-09, Volume: 2, Issue:6, 2011
Novel tetrahydrochinoline derived CETP inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
The biology and chemistry of hyperlipidemia.Bioorganic & medicinal chemistry, , Jul-15, Volume: 15, Issue:14, 2007
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Chiral N,N-disubstituted trifluoro-3-amino-2-propanols are potent inhibitors of cholesteryl ester transfer protein.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein.Journal of medicinal chemistry, , Nov-30, Volume: 43, Issue:24, 2000
Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein iJournal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
2D Quantitative structure-activity relationship studies on a series of cholesteryl ester transfer protein inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 15, Issue:18, 2007
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 32, 2021
Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Fragment-based discovery of novel pentacyclic triterpenoid derivatives as cholesteryl ester transfer protein inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Discovery of novel N,N-3-phenyl-3-benzylaminopropionanilides as potent inhibitors of cholesteryl ester transfer protein in vivo.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| phospholipid transporter activity | molecular function | Enables the directed movement of phospholipids into, out of or within a cell, or between cells. Phospholipids are a class of lipids containing phosphoric acid as a mono- or diester. [GOC:ai, ISBN:0198506732] |
| lipid binding | molecular function | Binding to a lipid. [GOC:ai] |
| cholesterol binding | molecular function | Binding to cholesterol (cholest-5-en-3-beta-ol); the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. [GOC:jl, ISBN:0198506732] |
| triglyceride binding | molecular function | Binding to a triester of glycerol. [GOC:jl, ISBN:0198506732] |
| phosphatidylcholine binding | molecular function | Binding to a phosphatidylcholine, a glycophospholipid in which a phosphatidyl group is esterified to the hydroxyl group of choline. [GOC:mah, ISBN:0198506732] |
| cholesterol transfer activity | molecular function | Removes cholesterol from a membrane or a monolayer lipid particle, transports it through the aqueous phase while protected in a hydrophobic pocket, and brings it to an acceptor membrane or lipid particle. [GOC:krc, PMID:20823909, PMID:24220498, PMID:25797198] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| vesicle | cellular component | Any small, fluid-filled, spherical organelle enclosed by membrane. [GOC:mah, GOC:pz, GOC:vesicles] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| high-density lipoprotein particle | cellular component | A lipoprotein particle with a high density (typically 1.063-1.21 g/ml) and a diameter of 5-10 nm that contains APOAs and may contain APOCs and APOE; found in blood and carries lipids from body tissues to the liver as part of the reverse cholesterol transport process. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:pde, GOC:rl] |
Involved In
This protein is involved in 19 target(s):
| Target | Category | Definition |
|---|
| triglyceride metabolic process | biological process | The chemical reactions and pathways involving triglyceride, any triester of glycerol. The three fatty acid residues may all be the same or differ in any permutation. Triglycerides are important components of plant oils, animal fats and animal plasma lipoproteins. [ISBN:0198506732] |
| lipid transport | biological process | The directed movement of lipids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Lipids are compounds soluble in an organic solvent but not, or sparingly, in an aqueous solvent. [ISBN:0198506732] |
| cholesterol metabolic process | biological process | The chemical reactions and pathways involving cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. It is a component of the plasma membrane lipid bilayer and of plasma lipoproteins and can be found in all animal tissues. [ISBN:0198506732] |
| negative regulation of macrophage derived foam cell differentiation | biological process | Any process that decreases the rate, frequency or extent of macrophage derived foam cell differentiation. Macrophage derived foam cell differentiation is the process in which a macrophage acquires the specialized features of a foam cell. A foam cell is a type of cell containing lipids in small vacuoles and typically seen in atherosclerotic lesions, as well as other conditions. [GOC:add, GOC:BHF, GOC:dph, GOC:tb] |
| regulation of cholesterol efflux | biological process | Any process that modulates the frequency, rate or extent of cholesterol efflux. Cholesterol efflux is the directed movement of cholesterol, cholest-5-en-3-beta-ol, out of a cell or organelle. [GOC:BHF, GOC:dph, GOC:tb] |
| phospholipid transport | biological process | The directed movement of phospholipids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Phospholipids are any lipids containing phosphoric acid as a mono- or diester. [GOC:ai] |
| cholesterol transport | biological process | The directed movement of cholesterol, cholest-5-en-3-beta-ol, into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:mah, ISBN:0198506732] |
| positive regulation of cholesterol transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of cholesterol into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:mah] |
| triglyceride transport | biological process | The directed movement of triglyceride into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Triglycerides are important components of plant oils, animal fats and animal plasma lipoproteins. [GOC:BHF, GOC:rl] |
| very-low-density lipoprotein particle remodeling | biological process | The acquisition, loss or modification of a protein or lipid within a very-low-density lipoprotein particle, including the hydrolysis of triglyceride by hepatic lipase or lipoprotein lipase and the subsequent loss of free fatty acid. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| low-density lipoprotein particle remodeling | biological process | The acquisition, loss or modification of a protein or lipid within a low-density lipoprotein particle, including the hydrolysis of triglyceride by hepatic lipase, with the subsequent loss of free fatty acid, and the transfer of cholesterol esters from LDL to a triglyceride-rich lipoprotein particle by cholesteryl ester transfer protein (CETP), with the simultaneous transfer of triglyceride to LDL. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| high-density lipoprotein particle remodeling | biological process | The acquisition, loss or modification of a protein or lipid within a high-density lipoprotein particle, including the hydrolysis of triglyceride by hepatic lipase, with the subsequent loss of free fatty acid, and the transfer of cholesterol esters from LDL to a triglyceride-rich lipoprotein particle by cholesteryl ester transfer protein (CETP), with the simultaneous transfer of triglyceride to LDL. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| cholesterol homeostasis | biological process | Any process involved in the maintenance of an internal steady state of cholesterol within an organism or cell. [GOC:go_curators] |
| reverse cholesterol transport | biological process | The directed movement of peripheral cell cholesterol, cholest-5-en-3-beta-ol, towards the liver for catabolism. [GOC:ecd, PMID:7751809] |
| phosphatidylcholine metabolic process | biological process | The chemical reactions and pathways involving phosphatidylcholines, any of a class of glycerophospholipids in which the phosphatidyl group is esterified to the hydroxyl group of choline. They are important constituents of cell membranes. [ISBN:0198506732] |
| lipid homeostasis | biological process | Any process involved in the maintenance of an internal steady state of lipid within an organism or cell. [GOC:BHF, GOC:rl] |
| phospholipid homeostasis | biological process | Any process involved in the maintenance of an internal steady state of phospholipid within an organism or cell. [GOC:BHF, GOC:rl] |
| triglyceride homeostasis | biological process | Any process involved in the maintenance of an internal steady state of triglyceride within an organism or cell. [GOC:BHF, GOC:mah] |
| positive regulation of phospholipid transport | biological process | Any process that activates or increases the frequency, rate or extent of phospholipid transport. [GOC:obol] |