Abstract:
BACKGROUND:Cholesterol efflux as a key event in reverse cholesterol transport (RCT) is considered now as both diagnostic tool and a promising target for the treatment of atherosclerosis. Radioactive in vitro cholesterol efflux assay (CEA) is the gold standard for determination of efflux at cellular level. Fluorescent tracers and stable isotope-labeled cholesterol gradually come into use as convenient tools for non-radioactive CEAs. RESULTS:We review the use of various tracer-based and tracer-free methods for CEAs and for measuring RCT with focus on macrophage-specific cholesterol efflux. CEA utilizing stable isotope-labeled cholesterol is equally reliable with radioactive assay and especially well suited for the determination of both cholesterol efflux and net cholesterol flux. Fluorescent tracers cannot fully mimic cholesterol; however, they are successfully applied in CEA in specific well-defined conditions. Fluorescent CEAs can be high throughput and can provide unique information on efflux from fast cholesterol pools or with single cell resolution. Enzymatic and chromatographic CEAs are net cholesterol flux assays, and they can be applied as efflux assays when used with specific acceptors only. In vivo tests are suited for studies of cholesterol efflux and RCT at the level of the organism. They include injection of tracer-loaded macrophages, a method suitable at present for animal models only, and recently invented modification of whole body tracer kinetics with multicompartment modeling that is capable to determine cholesterol efflux from macrophages. CONCLUSION:Despite the decisive role of in vitro assays in our understanding of cholesterol efflux mechanism, the in vivo assays are highly desired to study cholesterol efflux in atherosclerotic lesions and RCT in whole body.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Litvinov DY,Savushkin EV,Garaeva EA,Dergunov ADdoi
10.2174/0929867323666160809093009subject
Has Abstractpub_date
2016-01-01 00:00:00pages
3883-3908issue
34eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-77640journal_volume
23pub_type
杂志文章,评审abstract::The discovery of anandamide as an endogenous ligand for the cannabinoid receptors has led to a resurgence of interest in the fatty acid amides. However, N-palmitoylethanolamine (PEA), a shorter and fully saturated analogue of anandamide, has been known since the fifties. This endogenous compound is a member of the N-a...
journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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更新日期:2001-07-01 00:00:00
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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更新日期:2017-11-17 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2010-01-01 00:00:00
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更新日期:2020-01-01 00:00:00
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更新日期:2015-01-01 00:00:00
abstract::Reversible phosphorylation is a key mechanism for regulating the biological activity of many human proteins that affect a diverse array of cellular processes, including protein-protein interactions, gene transcription, cell-cycle progression and apoptosis. Once viewed as simple house keeping enzymes, recent studies ha...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2002-11-01 00:00:00
abstract::Osteogenic peptides are, or have potential to be, therapies for the treatment of osteoporosis, fracture repair, and repair of loosened bone implants. Human parathyroid hormone has been approved for the treatment of post-menopausal osteoporosis. Constrained analogs of PTH and the parathyroid-hormone related peptide (PT...
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更新日期:2004-11-01 00:00:00
abstract::The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA synthetases (AaRS). Aminoacyl-tRNA synthetases are the...
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abstract:: ...
journal_title:Current medicinal chemistry
pub_type: 社论
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abstract::The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...
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更新日期:2007-01-01 00:00:00
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journal_title:Current medicinal chemistry
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更新日期:2004-05-01 00:00:00
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