Abstract：
:The acidic amino acid L-glutamate acts as both a primary excitatory neurotransmitter and a potential neurotoxin within the mammalian central nervous system. Functionally juxtaposed between these neurophysiological and pathological actions are an assorted group of integral membrane transporter proteins that rapidly and efficiently sequester glutamate into cellular and subcellular compartments. While multiple systems exist that are capable of mediating the uptake of L-glutamate, the high-affinity, sodium-dependent transporters have emerged as the most prominent players in the CNS with respect to terminating the excitatory signal, recycling the transmitter, and regulating extracellular levels of glutamate below those which could induce excitotoxic pathology. The focus of the present review is on the pharmacological specificity of these sodium-dependent transporters and, more specifically, on the competitive inhibitors that have been used to delineate the chemical requirements for binding and translocation. Analogues of glutamate that are conformationally constrained as a consequence of either the addition of substituents to the carbon backbone of glutamate or aspartate (e.g., beta-hydroxyaspartate or methylglutamate derivatives) or the incorporation of ring systems (e.g., (carboxycyclopropyl)glycines, aminocyclobutane dicarboxylates, or pyrrolidine dicarboxylates), have been especially valuable in these efforts. In this review, a particular emphasis is placed on the identification of analogues that exhibit preferential activity among the recently cloned transporter subtypes and on the differentiation of substrates from non-transportable inhibitors.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Bridges RJ,Kavanaugh MP,Chamberlin ARsubject
Has Abstractpub_date
1999-05-01 00:00:00pages
363-79issue
5eissn
1381-6128issn
1873-4286journal_volume
5pub_type
杂志文章,评审abstract：:Aim of the presented study was to investigate the role of stromal derived factor 1 (SDF-1α) in mobilizing stem cells in combination with endothelial progenitor cell (EPC) transplantation in a regenerative strategy for myocardial infarction therapy in a murine ischemia/reperfusion model. Initially bone marrow was eradi...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/13816128113199990443
更新日期：2014-01-01 00:00:00
abstract：:Currently management of food allergy is mainly based on absolute avoidance of the offending food(s) and the use of rescue medication. However, the risk of severe or life-threatening reactions due to inadvertent exposure, nutritional imbalance and social isolation raises the demand of disease-modifying treatments. The ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/13816128113199990045
更新日期：2014-01-01 00:00:00
abstract：:We estimated the frequency of detection of different human papillomavirus (HPV) types in women with atypical squamous cells of undetermined significance (ASCUS) or low-grade squamous intraepithelial lesion (LSIL) cytology in a population-based primary screening programme. 247 liquid-based cytology (LBC) samples with A...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：
更新日期：2013-01-01 00:00:00
abstract：:Hyperglycemia is a common feature of the critically ill in general and of patients with sepsis in particular. Even a moderate degree of hyperglycemia appears detrimental for the outcome of critically ill patients, since maintenance of normoglycemia (blood glucose levels journal_title：Current pharmaceutical design pub_type： 杂志文章,评审 doi：10.2174/138161208784980563 更新日期：2008-01-01 00:00:00
abstract：:Gene therapy may be capable of treating a variety of diseases, a prerequisite of which is the successful delivery of polynucleic acids (e.g., DNA, RNA) to a patient's cells. Delivery can be achieved technologically (e.g., using electroporation), using viruses (natural gene delivery vectors) or non-viral vectors (e.g.,...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666170710124137
更新日期：2017-01-01 00:00:00
abstract：:Many plant species and tissues have been investigated as production and delivery vehicles for recombinant pharmaceutical proteins. Examples include cultured cells, whole aquatic plants and transgenic plants expressing recombinant proteins in their leaves, seeds, fruits or tubers/roots. Each platform has unique propert...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612811319310005
更新日期：2013-01-01 00:00:00
abstract：:The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes o...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612825666190717104547
更新日期：2019-01-01 00:00:00
abstract：BACKGROUND:Primary aldosteronism is the most common causes of secondary hypertension. Patients suffering from this clinical syndrome have an increased cardiovascular risk and target organ damage. Mineralocorticoid receptor antagonists are the optimal pharmaceutical option for the management of such patients. OBJECTIVE...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612825666190311130138
更新日期：2018-01-01 00:00:00
abstract：:The review describes key aspects of the synthesis and biological activities of conjugates of oligonucleotides and their analogues with synthetic peptides, in particular aimed towards gene silencing applications. The common methods of synthesis of oligonucleotide-peptide conjugates (OPCs) and PNA-peptide conjugates (PP...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161205774580769
更新日期：2005-01-01 00:00:00
abstract：:Our current understanding of cancer suggests that every tumour has individual features. Approaches to cancer treatment require thorough comprehension of the mechanisms triggering genomic instability and protecting cancer cells from therapeutic treatments. Base excision repair (BER) is a frontline DNA repair system tha...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666170710123602
更新日期：2017-01-01 00:00:00
abstract：:Sarcopenia is defined as the loss of muscle mass associated with a loss of muscle function, e.g., walking speed. A number of consensus definitions exist for sarcopenia with cut-off points being ethnically specific. A rapid screen test (SARC-F) is available and does not require different ethnic cut-off points. Sarcopen...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666161123150032
更新日期：2017-11-28 00:00:00
abstract：:Pulmonary arterial hypertension (PAH) is a severe vascular complication of connective tissue diseases. In the context of systemic sclerosis (SSc), PAH is a devastating disease with a dramatic impact on prognosis and survival. Despite advances in early diagnosis and the development of new targeted treatments, SSc-relat...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161212799504704
更新日期：2012-01-01 00:00:00
abstract：BACKGROUND:Plants have been used to treat health disorders and prevent diseases since antiquity in all civilizations including the Indian and Chinse civilizations. Giloy (Tinospora cordifolia L.) is one of the most important medicinal plants in Indian folk medicine and is commonly known as the "Heart-leaved Moonseed" o...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/1381612826666200625111530
更新日期：2020-06-25 00:00:00
abstract：:MicroRNA-34a (miR-34a) promotes apoptosis via down-regulating many anti-apoptotic proteins. Aldehyde dehydrogenase 2 (ALDH2) is an anti-apoptotic enzyme whose activity decline associates with myocardial injury. We tested hypothesis that miR-34a might play a pro-apoptotic role in myocardial infarction (MI) by down-regu...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/13816128113199990325
更新日期：2013-01-01 00:00:00
abstract：:The large conduit arteries of the thorax and abdomen are elastic while those in the arms and legs are muscular. Alterations in wall properties of elastic arteries occur over time and are usually permanent in nature; acute changes can, however, occur is response to a change in transmural pressure. Chronic alterations i...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161209787354258
更新日期：2009-01-01 00:00:00
abstract：:Alzheimer's disease (AD) is a complex degenerative disorder of the brain, associated with a progressive cognitive decline. Age is the main risk factor with almost half of the population above 90 years affected by this pathology. AD and brain aging share common molecular changes, so it has been hypothesized that AD cou...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：
更新日期：2013-01-01 00:00:00
abstract：:In the third millennium preventive medicine is becoming a corner stone in our concept of health. Colorectal cancer (CRC) fits the criteria of a disease suitable for prevention interventions. It is a prevalent disease that is associated with considerable mortality and morbidity rates, with more than 1,000,000 new cases...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161207781368783
更新日期：2007-01-01 00:00:00
abstract：:Proper understanding of blood-brain barrier (BBB) regulation is crucial to reduce/prevent its disruption during injury. Since high brain complexity makes interpretation of in vivo data challenging BBB studies are frequently performed using simplified in vitro models. Although such models represent an important and fre...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161211797440159
更新日期：2011-01-01 00:00:00
abstract：:High molecular weight kininogen (HK) is a plasma protein that is cleaved by plasma kallikrein in the clinical settings of sepsis and chronic inflammatory diseases such as rheumatoid arthritis and Crohn's disease. This proteolytic event results in a nonapeptide, bradykinin (BK), and a kinin-free derivative of HK, namel...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161206777698710
更新日期：2006-01-01 00:00:00
abstract：:The survival of patients with pulmonary arterial hypertension is closely related with right ventricular function. During the progression of right ventricular remodeling, energetic metabolism shifts from oxidative mitochondrial metabolism to glycolysis. In normal physiological conditions, cardiomyocytes use major sourc...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612822666160614082712
更新日期：2016-01-01 00:00:00
abstract：:Myocarditis is a disease whose pathogenesis is not completely understood and whose prevalence is likely underestimated. Individuals afflicted with this condition may be treated with agents that relieve symptoms arising from inflammation and concurrent cellular damage. One class of drugs commonly used in the treatment ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612033455440
更新日期：2003-01-01 00:00:00
abstract：:Superparamagnetic iron oxide nanoparticles (SPIONs) comprise a fundamental technology class within the emerging field of nanomedicine, and have been extensively researched for cancer imaging and therapy. This review article will discuss the chemistry and design considerations associated with the synthesis of SPIONs an...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：
更新日期：2013-01-01 00:00:00
abstract：BACKGROUND:Osteoarthritis (OA) is a common joint disease characterized by cartilage degeneration. Long non-coding RNAs (lncRNAs) have been associated with inflammatory diseases, including OA. Here, we investigated the potential molecular role of lncRNAs in OA pathogenesis. METHODS:ATDC5 cells were treated with lipopol...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/1381612825666190801141801
更新日期：2019-01-01 00:00:00
abstract：:In patients with acute coronary syndromes (ACS), hypertension is common. The type of ACS and severity of hypertension would determine the treatment algorithm. In ST elevation myocardial infarction (MI), time to reperfusion is essential whereas in malignant hypertension the reduction of blood pressure to prevent end or...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161207781663046
更新日期：2007-01-01 00:00:00
abstract：:Synaptic transmission through descending motor pathways to lumbar motoneurons and then to leg muscles is essential for walking in humans and rats. Spinal cord injury (SCI), even when incomplete, results in diminished transmission to motoneurons and very limited recovery of motor function. Neurotrophins have emerged as...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/13816128113199990378
更新日期：2013-01-01 00:00:00
abstract：BACKGROUND:Stroke represent one of the most devastating of all neurological diseases, affecting about 15 million people per year and is an important cause of morbidity and mortality worldwide and currently the leading cause of adult disability in developed countries. Blood pressure and heart rate may undergo several mo...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666170714162455
更新日期：2017-01-01 00:00:00
abstract：:Invasive fungal infections are a major cause of morbidity and mortality in immunosuppressed patients with fatality rates ranging from 30 % to 80 % in neutropenic patients. This results at least partly in difficulties obtaining a reliable and early diagnosis, followed by the fact that clinical symptoms are unspecific a...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/13816128113199990323
更新日期：2013-01-01 00:00:00
abstract：BACKGROUND:Arterial hypertension (AH) and peripheral arterial disease (PAD) frequently coincide. While significant attention is paid to AH, PAD is often underestimated. It is known that both AH and PAD present high cardiovascular risks for ischemic events. To date, the use of the most common anti-hypertensive drugs in ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666170608083605
更新日期：2017-01-01 00:00:00
abstract：:The concept that the gut microbiota plays a major role in the development of pouchitis in ulcerative colitis patients after restorative proctocolectomy with ileal pouch-anal anastomosis, is widely accepted and supported by a widespread use of some antibiotics (metronidazole and/or ciprofloxacin, rifaximin) to treat th...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/13816128113196660724
更新日期：2014-01-01 00:00:00
abstract：:Since identifying a transmissible agent responsible for tumorigenesis in chickens, the v-Src oncogene, significant progress has been made in determining the functions of its cellular homologue. c-Src is the product of the SRC gene and has been found both over-expressed and highly activated in a number of human cancers...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612053507576
更新日期：2005-01-01 00:00:00
