Abstract:
:Nuclear magnetic resonance spectroscopy has been exploited to study the metabolic characteristics (phenotype) of genetic disorders by taking advantage of some unique characteristics of the technique. The first application, metabolic profiling for diagnosis and therapeutic monitoring in vitro, demonstrates the exceptional diversity of metabolites detected by NMR, and has resulted in new interest in significant metabolites largely ignored previously because other techniques do not detect them, e.g. betaine and creatine. Moreover, previously 'unknown' genetic disorders have been detected and characterised The same NMR technique can be effectively exploited for metabolic profiling of mutation models in yeast and mice, leading to a prominent role in the development of large scale metabolomic profiling to link genomic information with phenotype. The second application, magnetic resonance spectroscopy (MRS), exploits the unique possibility of studying human metabolism in vivo, which permits intracellular rather than extracellular metabolic profiling. When it is possible to detect the precise diagnostic metabolites in vivo, investigators have been able to link clinical status with cellular biochemistry, sometimes questioning the clinical value of extracellular (plasma) metabolite measurements. Thus, claims have been made that brain phenylalanine concentrations match more closely the clinical status of patients with phenylketonuria. These studies in vivo have also led to new diagnoses e.g. the disorders of creatine synthesis and transport, highlighting a new category of brain syndromes. Future applications of NMR are cautiously considered as they are critically dependent on continued improvement in resolution and sensitivity in turn generated by developments in magnet design and higher fields.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Iles RAdoi
10.2174/092986708783330719subject
Has Abstractpub_date
2008-01-01 00:00:00pages
15-36issue
1eissn
0929-8673issn
1875-533Xjournal_volume
15pub_type
杂志文章,评审abstract::Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade. FXa catalyses the conversion of prothrombin to thrombin via the prothrombinase complex. Its singular role in thrombin generation, coupled with its potentiating effects on c...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707782023659
更新日期:2007-01-01 00:00:00
abstract::The deposition of β-amyloid (Aβ) plaques in the parenchymal and cortical brain is accepted as the main pathological hallmark of Alzheimer's disease (AD). According to the amyloid cascade hypothesis, the Aβ deposition in the brain appears to be a good diagnostic biomarker for AD and may also be a good predictive biomar...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/09298673113209990216
更新日期:2014-01-01 00:00:00
abstract::Diabetes mellitus (DM) is a significant healthcare concern worldwide that affects more than 165 million individuals leading to cardiovascular disease, nephropathy, retinopathy, and widespread disease of both the peripheral and central nervous systems. The incidence of undiagnosed diabetes, impaired glucose tolerance, ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707781058968
更新日期:2007-01-01 00:00:00
abstract::Ca(2+) is a highly versatile intracellular second messenger in the central nervous system, and regulates many complicated cellular processes, including excitation, plasticity and apoptosis. Influx of Ca(2+) from the extracellular fluid is required for sustained elevation of the cytosolic Ca(2+) concentration and full ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712803341430
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:The possibilities of treatment for oncological diseases are growing enormously in the last decades. Unfortunately, these developments have led to the onset of resistances with regards to the new treatments. This is particularly true if we face with the therapeutic field of Tyrosine Kinase Inhibitors (TKIs). ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180607092451
更新日期:2019-01-01 00:00:00
abstract::Selenium is an essential trace element. It is, however toxic at concentration little above which is required for health. Selenium is incorporated into proteins as selenocysteine, the 21(st) amino acid. Selenoproteins are found in bacteria, archaea and eukaryotes. Biochemical and physicochemical properties of selenium ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043365053
更新日期:2004-06-01 00:00:00
abstract:BACKGROUND:Histone deacetylases (HDAC) are an important class of enzymes that play a pivotal role in epigenetic regulation of gene expression that modifies the terminal of core histones leading to remodelling of chromatin topology and thereby controlling gene expression. HDAC inhibitors (HDACi) counter this action and ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180530094120
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Fatty liver, or steatosis, is a condition of excess accumulation of lipids, mainly under form of triglycerides (TG), in the liver, and it is the hallmark of non-alcoholic fatty liver disease (NAFLD). NAFLD is the most common liver disorder world-wide and it has frequently been associated with obesity, hyperl...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170518101334
更新日期:2019-01-01 00:00:00
abstract::In situ hybridization (ISH) is a type of hybridization that uses a labeled complementary DNA or RNA strand to localize a specific DNA or RNA sequence on a chromosome or section of tissue (in-situ) fixed on a slide. Flourescence in-situ hybridization (FISH) technique facilitates the localization of genes to different c...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801661031
更新日期:2012-01-01 00:00:00
abstract::Analytical chemists have increasingly turned their attention to drug discovery and drug analysis and to solve fundamental questions of biological significance in physiology and genetics. New technologies have been developed, and a variety of instruments have been redesigned for biomedical applications. The development...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867310504050501
更新日期:2005-01-01 00:00:00
abstract::The chemokine receptor, CXCR4, is a GPCR that transduces signals of its endogenous ligand, CXCL12 (stromal cell-derived factor-1, SDF-1). The CXCL12-CXCR4 system plays an important role in the migration of progenitors during embryologic development of the cardiovascular, hemopoietic, central nervous systems, etc. This...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707779313499
更新日期:2007-01-01 00:00:00
abstract:OBJECTIVES:Post-exercise cardiac troponin T (cTnT) release has been widely reported in adult athletes but limited data is available for adolescents. The aim of this study was to determine the incidence and magnitude of cTnT appearance in a large group of adolescent runners, and to determine any association between cTnT...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/092986711796642625
更新日期:2011-01-01 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::Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new c...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711793979779
更新日期:2011-01-01 00:00:00
abstract::Although resin-based chemistry offers many practical advantages over conventional solution phase for the synthesis of combinatorial libraries, effective monitoring of reactions conducted on the support remains a challenge. A number of techniques have been developed to enable the analysis of solid phase organic synthes...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867023368737
更新日期:2002-12-01 00:00:00
abstract::Traditional opioids, mainly alkaloids, have been used in the clinical management of pain for a number of years but are often associated with numerous side-effects including sedation, dizziness, physical dependence, tolerance, addiction, nausea, vomiting, constipation and respiratory depression which prevent their effe...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867323666160219115226
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Glioma is a heterogeneous, highly complicated central nervous system (CNS) tumor with uncertain mechanism of initiation and progression, resulting in an unfavorable outcome. An extended network of cytokines is recognized as a major regulator of glioma pathogenesis, either promoting or inhibiting glioma progr...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666171129125712
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Despite the historical employment of boron-containing compounds (BCCs) with medicinal purposes, the reported cases of BCC toxicity in humans during the twentieth century were driving us towards an "boron-withdrawal" period. Fortunately, the use of boric acid for specific purposes remains, and the discovery o...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867326666190327154954
更新日期:2019-03-27 00:00:00
abstract:BACKGROUND:Excessive norepinephrine (NE) release in the ischemic heart elicits severe and often lethal arrhythmias. Resident cardiac mast cells synthesize and store active renin, which is released upon degranulation, causing the activation of a local cardiac renin-angiotensin system (RAS) responsible for NE release and...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180214115127
更新日期:2018-01-01 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
pub_type: 杂志文章,评审
doi:10.2174/092986708783497328
更新日期:2008-01-01 00:00:00
abstract::This review presents a general overview of the subtype-selective dopamine receptor radioligands for in vivo imaging of dopamine receptor expression by positron emission tomography (PET). Besides the (11)C- and (18)F-labeled radioligands which are already in clinical use, a summary of subtype-selective radioligands whi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712802002518
更新日期:2012-01-01 00:00:00
abstract::Chemoprevention is based on the use of non-toxic, pharmacologically active agents to prevent tumor progression. In this regard, natural dietary agents have been described by the most recent literature as promising tools for controlling onset and progression of malignancies. Extensive research has been so far performed...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867325666180629153141
更新日期:2020-01-01 00:00:00
abstract::Paediatric Acquired ImmunoDeficiency Syndrome (AIDS) is a life-threatening and infectious disease in which the Human Immunodeficiency Virus (HIV) is mainly transmitted through Mother-To- Child Transmission (MTCT) during pregnancy, labour and delivery, or breastfeeding. This review provides an overview of the distinct ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180904123549
更新日期:2020-01-01 00:00:00
abstract::Fabry disease (FD) is an X-linked glycosphingolipid storage disorder caused by deficient activity of the lysosomal enzyme alpha-galactosidase A. This leads to a progressive accumulation of globotriaosylceramide (Gb3) in the lysosomes of different cells and tissues, causing principally ventricular hypertrophy, renal fa...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986710791111297
更新日期:2010-01-01 00:00:00
abstract::Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708784638861
更新日期:2008-01-01 00:00:00
abstract::Fibroblast growth factor receptor-4 (FGFR4) is a tyrosine kinase with a range of important physiological functions. However, it is also frequently mutated in various cancers and is now generating significant interest as a potential therapeutic target. Unfortunately, biochemical characterization of its role in disease,...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867311320100001
更新日期:2013-01-01 00:00:00
abstract::Cholecystokinin (CCK) is an important neuro-intestinal peptide hormone produced by the enteroendocrine I-cells in the upper part of small intestine. Protein- and fat-enriched food plays an important role in triggering CCK secretion from the intestine. Carbohydrates stimulate only small amounts of CCK release. The CCK-...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170619104801
更新日期:2019-01-01 00:00:00
abstract::Potent enzyme inhibitors have long been recognized as powerful tools for assessing the physiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities in vivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere with other members of th...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867023371120
更新日期:2002-02-01 00:00:00
abstract::Heparins are used in "therapeutic doses" for systemic anticoagulation to treat patients who have confirmed venous thromboembolism, or in "prophylactic doses "for the prevention of venous thromboembolism: they are generally lower doses and are employed once a day. Structure-function relationships are strongly influence...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709788803105
更新日期:2009-01-01 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...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712801323199
更新日期:2012-01-01 00:00:00