Abstract:
:Cellular signaling is regulated by several biochemical reactions, whose dynamics depends on changes in the fluxes of specific ligands through the containment barriers that are the biological membranes. The regulation of this complex dynamic equilibrium is mainly due to the activity of border proteins, that must be able to interact simultaneously with the lipid bilayer and the extracellular milieu. Endocannabinoid receptors, that include type-1 and type-2 cannabinoid receptors, the transient vanilloid potential receptors and the peroxisome proliferator-activated receptors, represent one of the most intriguing examples of "border" proteins. They have also been identified as important drug discovery targets with potential therapeutic applications, from antiemesis, appetite enhancement, analgesia, glaucoma treatment, and immune suppression. However, as yet the molecular details of endocannabinoid receptor regulation remain elusive. In this review we summarize the most relevant aspects of the structural/functional characterization of these receptors, with a focus on the active role played by biological membranes (in particular lipid rafts) in the modulation of their accessibility and mode of ligand binding. Based on available evidence, we propose that endocannabinoid receptors can be regulated by the rate of interlayer exchange and lateral diffusion of endocannabinoid/cholesterol complexes within lipid bilayers, thus suggesting innovative approaches for the therapeutic exploitation of the membrane component of endocannabinoid signaling.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Dainese E,Oddi S,Maccarrone Mdoi
10.2174/092986710790980087subject
Has Abstractpub_date
2010-01-01 00:00:00pages
1487-99issue
14eissn
0929-8673issn
1875-533Xpii
BSP/CMC/E-Pub/ 097journal_volume
17pub_type
杂志文章,评审abstract::G protein-coupled receptors (GPCRs) comprise a large protein family of transmembrane receptors involved in many physiological processes. They are engaged in various transduction processes of extracellular signals into intracellular responses. Due to their involvement in numerous diseases they represent an important ph...
journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Current medicinal chemistry
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更新日期:2002-03-01 00:00:00
abstract::Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decad...
journal_title:Current medicinal chemistry
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abstract::Acyclic nucleoside analogues bearing phosphonomethoxy residues in the side chain (ANP) attract much attention due to a very beneficial combination of biological properties. Intensive work of organic chemists during the last two decades resulted in a large panel of new compounds that were evaluated as potential antivir...
journal_title:Current medicinal chemistry
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abstract::Vitamins are dietary components which are necessary for life. They play a major role in health and their deficiency may be linked to symptoms of psychiatric disorders. B vitamins are required for proper functioning of the methylation cycle, monoamine oxidase production, DNA synthesis and the repair and maintenance of ...
journal_title:Current medicinal chemistry
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abstract::The mitotic cell cycle is a tightly regulated process that ensures the correct division of one cell into two daughter cells. Progress along the different phases of the cell cycle is positively regulated by the sequential activation of a family of serine-threonine kinases called CDKs (Cyclin Dependent Kinases). Their a...
journal_title:Current medicinal chemistry
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更新日期:2005-01-01 00:00:00
abstract::To date, many scientific attempts have been directed towards the development of experimental models for the identification of neuronal mechanisms evoking cardiovascular and hemodynamic dysfunctions. The spontaneously hypertensive rat (SHR), a genetic model of essential hypertension, has become a valuable rodent for th...
journal_title:Current medicinal chemistry
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abstract::Apoptotic cell death has been reported in human oocytes and preimplantation embryos under in vivo and in vitro conditions. BCL-2 family proteins comprise both anti- and pro-apoptotic members, which are likely to play a key role in controlling oocyte and early embryo survival. However, very limited data are available o...
journal_title:Current medicinal chemistry
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更新日期:2014-01-01 00:00:00
abstract::Osteoporosis is a pathological loss of bone mass due to an imbalance in bone remodeling where osteoclast-mediated bone resorption exceeds osteoblast-mediated bone formation resulting in skeletal fragility and fractures. Anti-resorptive agents such as bisphosphonates and SERMs, and anabolic drugs that stimulate bone fo...
journal_title:Current medicinal chemistry
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更新日期:2020-03-30 00:00:00
abstract::The lung is a unique organ in terms of its direct exposure to high levels of oxygen and reactive compounds. Several parenchymal lung diseases (e.g. emphysema associated with smoking and a number of fibrotic lung disorders) have been proposed to be due to the exposure of the lung to exogenous irritants leading to local...
journal_title:Current medicinal chemistry
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更新日期:2007-01-01 00:00:00
abstract::Microcin J25 (MccJ25) is a plasmid-encoded peptide of 21 L-amino acids (G1-G-A-G-H5-V-P-E-Y-F10-V-G-I-G-T15-P-I-S-F-Y20-G), excreted to the medium by an Escherichia coli strain. MccJ25 is active on Gram-negative bacteria related to the producer strain, including some pathogenic strains. The four-plasmid genes mcjABCD,...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709787458461
更新日期:2009-01-01 00:00:00
abstract::Nanomedicine is certainly one of the scientific and technological challenges of the coming years. In particular, biodegradable nanoparticles formulated from poly (D,L-lactide-co-glycolide) (PLGA) have been extensively investigated for sustained and targeted delivery of different agents, including recombinant proteins,...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311320170006
更新日期:2013-01-01 00:00:00
abstract::The concept of click chemistry represented by the formation of the 1,2,3-triazole core has found wide application in drug discovery, particularly in the early discovery phases and the lead optimization process. 1,2,3-Triazoles ha ve attracted considerable attention in recent years because of their wide range of biolog...
journal_title:Current medicinal chemistry
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更新日期:2015-01-01 00:00:00
abstract::In the course of studying human mucin MUC1, the attitude towards this molecule has been changing time and again. Initially, the list of presumable functions of MUC1 was restricted to protecting and lubricating epithelium. To date, it is assumed to play an important role in cell signaling as well as in all stages of on...
journal_title:Current medicinal chemistry
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更新日期:2019-01-01 00:00:00
abstract::Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharma...
journal_title:Current medicinal chemistry
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更新日期:2016-01-01 00:00:00
abstract::Raltegravir, the only drug targeting the integration step in HIV-1 life cycle, makes β-ketoenol integrase (IN) strand transfer inhibitor (STI) gain a definitive place in the treatment of HIV-1 infection. However, the emergence of viral strains resistant to β-ketoenol STI demands a continued effort toward the discovery...
journal_title:Current medicinal chemistry
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更新日期:2012-01-01 00:00:00
abstract::Genito-urinary malignancies (prostate, bladder, renal and testicular cancers) rank high among human tumors with an incidence that varies with age and organ involvement. Prostate cancer is the most commonly detected male cancer followed by bladder and kidney cancers, less frequent in women. Testicular cancer, although ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2011-01-01 00:00:00
abstract::Protein-ligand docking is currently an important tool in drug discovery efforts and an active area of research that has been the subject of important developments over the last decade. These are well portrayed in the rising number of available protein-ligand docking software programs, increasing level of sophisticatio...
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pub_type: 历史文章,杂志文章,评审
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更新日期:2013-01-01 00:00:00
abstract:BACKGROUND:Monocyte chemoattractant protein-1 (MCP-1) is a member of the CC chemokine family that plays a key role in the inflammatory process. It has been broadly studied in the aspect of its role in obesity and diabetes related diseases. MCP-1 causes the infiltration of macrophages into obese adipose tissue via bindi...
journal_title:Current medicinal chemistry
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更新日期:2017-01-01 00:00:00
abstract::Receptor-binding peptides have attracted an enormous interest in targeting molecules for the development of tumour specific radiopharmaceutical compounds. The overexpression of many receptors on human tumour makes such peptide-ligands attractive agents for diagnostic imaging and therapy of cancers. The use of solid-ph...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/092986710791859388
更新日期:2010-01-01 00:00:00
abstract::Homocysteine is a thiol aminoacid synthesized during the metabolism of methionine. Increased plasma levels of homocysteine can be the result of mutations in the enzymes responsible for homocysteine metabolism, particularly cystathionine-beta synthase (CBS) and 5,10-methylenetetrahydrofolate reductase (MTHFR). Addition...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707779941140
更新日期:2007-01-01 00:00:00
abstract::Leukoaraiosis (LA), one of the most frequent causes of cognitive disturbances, is presumed to involve vascular demyelinization and cerebral small-vessel diseases. Although it has been suggested that the development of LA is associated with cerebral circulatory disturbances, the pathomechanism of this circulatory probl...
journal_title:Current medicinal chemistry
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更新日期:2007-01-01 00:00:00
abstract:BACKGROUND:Resveratrol, a natural polyphenol product, is used in plant defense from fungal and microbial aggression. It is found naturally, especially in plants such as grapes, peanuts, and berries. It has the highest concentrations in blueberries, mulberries, blackberries, and the skin of red grapes. Resveratrol has v...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327999200918100746
更新日期:2020-09-17 00:00:00
abstract::The resin of Pistacia lentiscus (L.) var. chia (Duham), an evergreen shrub belonging to the family Anacardiaceae and uniquely cultivated in southern Chios, is known as mastic. It has been used for more than 2500 years in traditional Greek medicine for treating several diseases such as gastralgia and peptic ulcers, whi...
journal_title:Current medicinal chemistry
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doi:10.2174/092986712800229014
更新日期:2012-01-01 00:00:00
abstract::Angiotensin converting enzyme (ACE) 2 is a homologue of ACE that catalyzes the conversion of Angiotensin (Ang) II into Ang1-7, which induces vasodilation, anti-fibrotic, anti-proliferative and anti-inflammatory effects. Given that ACE2 counterbalances the effects of Ang II, it has been proposed as a biomarker in kidne...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00
abstract::The cellular response to DNA damage is critical for determining whether carcinogenesis, cell death or other deleterious biological effects will ensue. Numerous cellular enzymatic mechanisms can directly repair damaged DNA, or allow tolerance of DNA lesions, and thus reduce potential harmful effects. These processes in...
journal_title:Current medicinal chemistry
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更新日期:2008-01-01 00:00:00
abstract::The discovery and development of novel drugs has been influenced over the last several decades by new techniques in medicinal chemistry. Combinatorial and parallel synthesis chemistry techniques have opened up immense opportunities in drug discovery and development efforts. These techniques, which include solid phase ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043364469
更新日期:2004-10-01 00:00:00
abstract::Various human tumors preferentially metastasize by lymphatic route and lymphovascular invasion predicts lymph node metastasis. In this review article, we will summarize recent literature data concerning lymphangiogenesis, focusing on tumor lymphangiogenesis. In detail, we try to answer some important questions related...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710790514471
更新日期:2010-01-01 00:00:00