Abstract:
:The expansion of fluorescent techniques for studying the ligand-receptor interaction resulted in a burst of the novel fluorescent ligands development. The discovery of the ligand, that is of high affinity to the receptor and whose localization could be easily visualized, even on the single cell level, gave the researchers a strong impulse to investigate that field of GPCR ligands. Moreover, paying attention to the "non pharmacological" advantages of these ligands, as well as the techniques to be used, fluorescent ligands are becoming treated more seriously, as the ligands themselves, and as novel, useful tools for studying GPCRs. Herein, we review results described in the literature, starting from the year 2000, in the field of the fluorescent GPCR small, non-peptide ligands according to the affinity to the selected receptors (histamine, adenosine, adrenergic, cannabinoid, muscarinie, neuropeptide Y and serotonine) as well as the fluorophores that have been used to tag the molecules.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Kuder K,Kieć-Kononowicz Kdoi
10.2174/092986708785747599subject
Has Abstractpub_date
2008-01-01 00:00:00pages
2132-43issue
21eissn
0929-8673issn
1875-533Xjournal_volume
15pub_type
杂志文章,评审abstract::The importance of organometallics can be noticed by their presence in all life organisms. The most known natural organometallic molecule is vitamin B12, a porphyrin containing a cobalt atom, useful for several enzymatic transformations. Based on the remarkable properties of this class of compounds, a new area of medic...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710791859306
更新日期:2010-01-01 00:00:00
abstract::Nitric oxide (NO) has been established as an important messenger molecule in various steps of brain physiology, from development to synaptic plasticity, learning and memory. However, NO has also been viewed as a major agent of neuropathology when, escaping controlled production it may directly or indirectly promote ox...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033456792
更新日期:2003-10-01 00:00:00
abstract::Thrombomodulin (TM) is a membrane protein mainly expressed by endothelial cells. It is part of the anticoagulant protein C system but recently several effects were discovered which occur independently of protein C activation. TM binds thrombin and promotes the cleavage of protein C and the thrombin activatable fibrino...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666131228204839
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:Pollutants are diverse chemical entities, including gases such as ozone and particulate matter PM. PM contains toxic chemicals such as polycyclic aromatic hydrocarbons (PAHs). Some PAHs can induce strong oxidative stress under UVA exposure. Pollution aggravates some skin diseases such as atopy or eczema, but...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170918123907
更新日期:2018-01-01 00:00:00
abstract::Migraine is a common disabling neurological disorder which is characterised by a recurring headache associated with a variety of sensory and autonomic symptoms. The pathophysiology of migraine remains not entirely understood, although many mechanisms involving the central and peripheral nervous system are now becoming...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180622154411
更新日期:2019-01-01 00:00:00
abstract::Magnetic resonance imaging (MRI) contrast agents are utilized adjunctively to enhance the contrast between normal and abnormal structures on MRI scans. Along with the rapid evolution of the field has come a new appreciation for the medicinal chemistry of this unique class of metallopharmaceuticals. The efficacy of MRI...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867053507379
更新日期:2005-01-01 00:00:00
abstract::Epinephrine and Norepinephrine, typically released during stress bind to nine different adrenoceptors (AR) which classically control the cardiovascular and respiratory systems. New targets were described for the many agonists and antagonists developed for these AR, as the central nervous system. During the last three ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709788186048
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Inflammation is one of the most misunderstood aspects of human health. People have been encouraged to eat foods that have a high antioxidant capacity, and in vitro tests for total antioxidant capacity emerged. They were based on measuring the destruction of oxidized test compounds in direct reactions with th...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666190517113533
更新日期:2020-01-01 00:00:00
abstract::Reactive oxygen species (ROS) are widely believed to cause or aggravate several human pathologies such as neurodegenerative diseases, cancer, stroke and many other ailments. Antioxidants are assumed to counteract the harmful effects of ROS and therefore prevent or treat oxidative stress-related diseases. In this repor...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711803414368
更新日期:2011-01-01 00:00:00
abstract::Histone deacetylase inhibitors have generated significant interest as anti-cancer agents due to their ability to cause growth arrest, terminal differentiation and/ or apoptosis in carcinoma cells. Abbott entered this area after the serendipitous discovery of the biaryl hydroxamate A-161906 in a TGF beta mimetic screen...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033456576
更新日期:2003-11-01 00:00:00
abstract::Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170529101810
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Numerous studies have reported sex and gender differences in the prevalence and treatment of cardiovascular diseases. However, sex differences in the therapy of hypertension have not been completely examined. OBJECTIVE:To estimate the gender-specific dissimilarity in outcomes among patients following antihy...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,meta分析
doi:10.2174/0929867323666161213160440
更新日期:2017-01-01 00:00:00
abstract::The utilization of graphene-based nanomaterials combined with magnetic nanoparticles offers key benefits in the modern biomedicine. In this minireview, we focus on the most recent advances in hybrids of magnetic graphene derivatives for biomedical applications. We initially analyze the several methodologies employed f...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666161216144218
更新日期:2017-01-01 00:00:00
abstract::The discovery of the high-affinity, high-specificity folate receptor in mamalian kidney cells, coupled with the ability of folate to enter cells by folate receptor-mediated endocytosis and the subsequent elucidation of the folate receptor's overexpression in specific cancer cell types; heralded the arrival of the area...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180209143715
更新日期:2018-01-01 00:00:00
abstract::Andrographolide, the main bioactive component separated from Andrographis paniculata in 1951, have been scrutinized with modern drug discovery approach for anti-inflammatory properties since 1984. Identifying new uses for existing drugs can be facilitated by evidence linking them to known or yet undiscovered drug targ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666200810135604
更新日期:2020-08-10 00:00:00
abstract::Over the years, natural products have shown success as antidiabetics in in vitro, in vivo studies and clinical trials. Because natural product-derived drugs are more affordable and effective with fewer side-effects compared to conventional therapies, pharmaceutical research is increasingly leaning towards the discover...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160813222436
更新日期:2018-01-01 00:00:00
abstract::The aminocoumarin antibiotics novobiocin, clorobiocin and coumermycin A(1) are produced by different Streptomyces strains and are potent inhibitors of DNA gyrase. The biosynthetic gene clusters of all three antibiotics have been cloned and sequenced, and the function of most genes contained therein has been elucidated...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867053363063
更新日期:2005-01-01 00:00:00
abstract::Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666171116124255
更新日期:2018-01-01 00:00:00
abstract::The discovery of cannabinoid receptors at the beginning of the 1990s, CB1 cloned in 1990 and CB2 cloned in 1993, and the availability of selective and potent cannabimimetics could only be justified by the existence of endogenous ligands that are capable of binding to them. Thus, the characterisation and cloning of the...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180226095132
更新日期:2019-01-01 00:00:00
abstract::Cellular resistance to anthracyclines is a major limitation of their clinical use in the treatment of human tumors. Resistance to doxorubicin is described as a multifactorial phenomenon involving the overexpression of defense factors and alterations in drug-target interactions. Such changes do not account for all mani...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867013373994
更新日期:2001-01-01 00:00:00
abstract::APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708786242840
更新日期:2008-01-01 00:00:00
abstract::This update covers the literature for 2002 and 2003 dealing with the main topic of the previous review entitled Heterocyclic nucleosides. Chemical synthesis and biological properties and published in Curr. Med. Chem.-AIA, 2002, 1, 389. As in the first review, the papers in this survey are grouped by the type of the he...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706776055779
更新日期:2006-01-01 00:00:00
abstract:: ...
journal_title:Current medicinal chemistry
pub_type: 社论
doi:10.2174/092986732601190314144026
更新日期:2019-01-01 00:00:00
abstract::The transport of organic and inorganic molecules, along with inorganic ions across the plasma membrane results in chemical fluxes that reflect the cellular function in healthy and diseased states. Measurement of these chemical fluxes enables the characterization of protein function and transporter stoichiometry, chara...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867326666190506111629
更新日期:2019-05-06 00:00:00
abstract::Breakdown of glucose under physiological conditions gives rise to glucose degradation products (GDPs). GDPs are also formed during heat sterilization of glucose-containing peritoneal dialysis fluids (PD-fluids). In PD-fluids GDPs have been shown in many different in vitro assays to be responsible for adverse effects s...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706778201576
更新日期:2006-01-01 00:00:00
abstract::Among naturally occurring isoflavones, soy isoflavones are an important class with various biological activities. Due to their phytoestrogenic structure, their effects on the brain are profound thus making the neurobiological effects of these compounds an active area of research. One such compound is daidzein, which h...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666161101140214
更新日期:2017-01-01 00:00:00
abstract::Xanthones (dibenzo-γ-pyrones) constitutes an important class of oxygenated heterocycles and occur as secondary metabolites in plants and microorganisms. They are known for various biological activities such as antioxidant, monoamine oxidase inhibitor, antihypertensive, hepatoprotective, antithrombotic, antifungal and ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/09298673113209990144
更新日期:2013-01-01 00:00:00
abstract::Statins are inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-limiting enzyme of cholesterol synthesis. In recent years, statins have become the major choice of treatment for hypercholesterolemia. Emerging evidence from both animal and human studies indicates that mechanisms i...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867033457205
更新日期:2003-08-01 00:00:00
abstract:BACKGROUND:Nitric oxide (NO) plays important regulatory roles in a plethora of biological functions and thus holds tremendous potential to be exploited for clinical uses. However, the chemistries in the molecular design of nano-nitric oxide delivery systems is currently lacking. OBJECTIVE:The overarching aim of this r...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170407141222
更新日期:2018-01-01 00:00:00
abstract::Type 2 diabetes mellitus (DM) is a public health burden and its co-existence with hypertension is long established in the context of the metabolic syndrome. Both DM and hypertension are major risk factors, for end-stage renal disease, cardiovascular events and mortality. Strict blood pressure (BP) control in diabetics...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666191029111713
更新日期:2020-01-01 00:00:00