Abstract:
:Aquaporins (AQPs) are expressed in physiologically essential tissues and organs in which edema and fluid imbalances are of major concern. Potential roles in brain water homeostasis and edema, angiogenesis, cell migration, development, neuropathological diseases, and cancer suggest that this family of membrane proteins is an attractive set of novel drug targets. A problem in pursuing therapeutic and basic research strategies for dissecting contributions of AQPs to cell and tissue functions is that little is known regarding the pharmacology of AQP channels; currently defined agents such as tetraethylammonium and phloretin as blockers for aquaporins suffer from a lack of specificity and potency. Subtypes of AQPs modulated by signaling pathways could enable discrete localized control of fluid homeostasis, volume and morphology in cells and intracellular organelles, and might be found to participate in many different aspects of physiology, such as the control of paracellular permeability, process extension, growth, migration, and other responses involving changes in cell shape or surface to volume ratios. Recognizing that AQP1 is a water channel and, under permissive conditions, also a cGMP-gated cation channel, evidence in various tissues for a coupling of the cGMP signaling cascade to a physiological outcome that might involve AQP1 dual ion-and-water channel functions is of interest. Groundbreaking advances in defining aquaporin gating mechanisms suggest conformational changes are important elements in regulation and gating across classes of aquaporins. With a rapidly expanding knowledge of aquaporin structure and functional regulation, new avenues for manipulation of aquaporin channels are likely to be discovered. In parallel, a discovery for novel compounds with specificity and potency for aquaporins is a compelling goal. The need for pharmacological agents to dissect the roles of aquaporins in physiological and pathological processes is a clear call for further research in the field.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Yool AJdoi
10.2174/138161207782341349subject
Has Abstractpub_date
2007-01-01 00:00:00pages
3212-21issue
31eissn
1381-6128issn
1873-4286journal_volume
13pub_type
杂志文章,评审abstract::The increasing prevalence of persistent biofilm infections, such as wound infections, chronic lung infections or medical device- related infections, which usually tolerate conventional antibiotic treatment, calls for the development of new therapeutic strategies. To date, antimicrobial peptides (AMPs) are considered a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140905124312
更新日期:2015-01-01 00:00:00
abstract::microRNAs (miRNAs) comprise a recently discovered class of non-coding RNAs with regulatory functions in post-transcriptional gene expression control. Many miRNAs are located in genomic regions that are frequently deleted in cancer, or are subject to epigenetic and transcriptional deregulation in cancer cells. The miRN...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161213804805649
更新日期:2013-01-01 00:00:00
abstract::Patients with diabetes mellitus (DM) type 2 have a high prevalence of coronary artery disease (CAD), as diabetes is implicated in the formation of atherosclerotic plaque. Hyperglycemia, elevated free fatty acid, increased amount of circulating end-glucosylated serum products and insulin resistance are the main mechani...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209788453185
更新日期:2009-01-01 00:00:00
abstract::The diatomic molecule of oxygen contains two uncoupled electrons and can therefore undergo reduction, yielding several different oxygen metabolites, which are collectively called Reactive Oxygen Species or ROS. They are invariably produced in aerobic environments through a variety of mechanisms, which include electron...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043384664
更新日期:2004-01-01 00:00:00
abstract::Syncytin-1 is a protein coded by a human endogenous retrovirus (HERV) gene of the HERV-W family (HERVWE1). Syncytin- 1 mediates formation of syncytiotrophoblasts through fusion of cytotrophoblasts, a hallmark of terminal differentiation of placental trophoblast linage. Syncytin-1 also possesses nonfusogenic functions ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/13816128113199990541
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:Although medications should only be prescribed in pregnancy if benefits to the mother outweigh the risk to the fetus, drug use in pregnancy especially prescribed and over-the-counter analgesics, is very common. OBJECTIVE:The objective of this review is to present an update on known changes in analgesic disp...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170825123754
更新日期:2017-01-01 00:00:00
abstract::Diabetic retinopathy remains the most common microvascular complication suffered by diabetic patients and is the leading cause of registerable blindness in the working population of developed countries. The clinicopathological lesions of diabetic retinopathy have been well characterised and although a multitude of pat...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043383124
更新日期:2004-01-01 00:00:00
abstract:BACKGROUND:Absorption windows in particular segments of the small intestine can contribute to the development of orally administered drug formulations and can limit the bioavailability of released compounds. OBJECTIVE:The aim of this study was to evaluate use of wireless capsule enteroscopy regarding the disintegratio...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612822666161201145247
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND:Non-alcoholic fatty liver disease (NAFLD) is one of the most common causes of chronic liver disease worldwide directly related to the progressive increase in overweight and obesity. The accumulation of lipids in patients with NAFLD contributes to the development of insulin resistance, inflammatory response a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200417165801
更新日期:2020-04-17 00:00:00
abstract:BACKGROUND:Virtual Screening methodologies have emerged as efficient alternatives for the discovery of new drug candidates. At the same time, ensemble methods are nowadays frequently used to overcome the limitations of employing a single model in ligand-based drug design. However, many applications of ensemble methods ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160302103542
更新日期:2016-01-01 00:00:00
abstract::Topiramate is one of the currently most promising compounds in the field of addiction medicine. This paper discusses its potential utility related to a phase model of addiction development, focusing on the assumption that addiction is a continuous process involving different neurobiological pathways, depending on the ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161211796150864
更新日期:2011-01-01 00:00:00
abstract::This review will focus on the construction, refinement, and validation of G Protein-coupled receptor models for the purpose of structure-based virtual screening. Practical tips and tricks derived from concrete modeling and virtual screening exercises to overcome the problems and pitfalls associated with the different ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789824786
更新日期:2009-01-01 00:00:00
abstract::Inhibition of fatty acid oxidation is well recognized as a potentially effective mechanism for controlling glycemia in non-insulin-dependent diabetes mellitus (NIDDM). However, a direct targeting of inhibition of the intramitochondrial beta-oxidation pathway or an indirect modulation of fatty acid oxidation by inhibit...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:
更新日期:1998-02-01 00:00:00
abstract::The three opioid receptors, mu, delta and kappa all mediate analgesia, and knockout mice with opioid receptor deletion have proven unique tools to investigate in vivo opioid pharmacology. Since a few years, a number of new mouse lines have been engineered, with several distinct mutations of the mu receptor, to assess ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161281942140105163727
更新日期:2013-01-01 00:00:00
abstract::Advances in particle engineering techniques, such as spray drying, freeze drying and supercritical fluid precipitation, have greatly enhanced the ability to control the structure, morphology, and solid state phase of inhalable sized particles (1 - 5 µm) for formulation in pressurized metered dose inhalers (pMDI). To o...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150820110153
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Bio-soft material, a class of derivatives of the natural or synthetic material, is getting more and more prevalent in biomedical researches and applications due to the advantages such as in-vivo biodegradation, good water solubility and designable targeting ability. With the presence of bio-sof...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180515154848
更新日期:2018-01-01 00:00:00
abstract::Oral epithelium is a stratified squamous epithelium that functions as the barrier between the outside environment and the host. In the oral cavity, epithelial tissues are constantly exposed to a variety of bacteria, but most individuals maintain healthy homeostasis. Epithelial cells contribute to the innate host respo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161207782110435
更新日期:2007-01-01 00:00:00
abstract::Medicinal inorganic chemistry plays an important role in exploring the properties of metal ions for the designing of new drugs. The field has been stimulated by the success of cis-platin, the world best selling anticancer drug and platinum complexes with reduced toxicity, oral activity and activity against resistant t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160906143249
更新日期:2016-01-01 00:00:00
abstract::Naoxintong (NXT), a Chinese Materia Medica standardized product, extracted from 16 various kinds of Chinese traditional herbal medicines including Salvia miltiorrhiza, Angelica sinennsis, Astragali Radix, is clinically effective in treating atherosclerosisrelated diseases. Here, we tested the hypothesis that the anti-...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612811319330008
更新日期:2013-01-01 00:00:00
abstract::The deregulated proteolysis is associated with various diseases in humans. Proteases are commonly regarded as the therapeutic targets. Almost one-third of all proteolytic enzymes in humans are serine proteases. This work provides a brief characteristic of the proteinaceous natural inhibitors, mostly of serine protease...
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::The skin remains an attractive area for drug delivery. The skin, however, often limits the ingress of drugs, because of its very low permeability. Much research, focusing on employing a variety of physical and chemical methods, aimed at reversibly altering skin permeability in favour of compounds, has been reported. O...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150428125812
更新日期:2015-01-01 00:00:00
abstract::Diabetic patients are considered as high risk for development of atherosclerotic disease. Cholesterol treatment is of paramount importance in order to optimise cardiovascular outcomes in this subset of patients. Although statins are regarded as the mainstay of treatment, these may not be tolerated or as efficacious as...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200617170252
更新日期:2020-06-17 00:00:00
abstract::Arrhythmias in left ventricular hypertrabeculation/noncompaction (LVHT) comprise sustained or non-sustained ventricular tachycardia (VT) (n=135), atrial fibrillation (AF) (n=96) AV block (n=55) and QT prolongation (n=47). The prevalence differs between children and adults. In children most frequent are WPW-syndrome (n...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210793176518
更新日期:2010-01-01 00:00:00
abstract::In recent years, the simple paradigm of adipose tissue as merely a fat store is rapidly evolving into a complex paradigm of this tissue as multipotential secretory organ, partitioned into a few large depots, including visceral and subcutaneous location, and many small depots, associated with a variety of organs in the...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033455152
更新日期:2003-01-01 00:00:00
abstract::Depression is one of the leading causes of disability in the world. Current pharmaceutical treatment for depression remains unsatisfactory due to its limited therapeutic efficacy and undesirable side effects. There is increasing interest in looking for alternative strategies from diet for the treatment of depressive d...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180803113106
更新日期:2018-01-01 00:00:00
abstract::Multidrug resistance (MDR) is a phenomenon through which tumor cells develop resistance against the cytotoxic effects of various structurally and mechanistically unrelated chemotherapeutic agents. The most consistent feature in MDR is overexpression and/or overactivity of ATP-dependent drug efflux transporters. Other ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666151124234417
更新日期:2016-01-01 00:00:00
abstract::We have gained considerable insight and understanding about the etiology, embryogenesis of the myocardium, genetic background, diagnosis and outcome of left ventricular non-compaction (LVNC) over the last 2 decades. LVNC has a distinct morphological appearance with a thickened, two-layered myocardium consisting of an ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161282104141204143212
更新日期:2015-01-01 00:00:00
abstract::Electropulsation (electroporation) is a physical method for delivery of various molecules into the cells in vitro and in vivo. It is an expanding field due to its applicability in cancer therapy, where combined application of electric pulses and chemotherapeutic drugs is used for treatment of cutaneous and subcutaneou...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206778559740
更新日期:2006-01-01 00:00:00
abstract::Mast cells are important in the development of allergic and anaphylactic reactions, but also in acquired and innate immunity. There is also increasing evidence that mast cells participate in inflammatory diseases, where they can be activated by non-allergic triggers, such as neuropeptides and cytokines, often having s...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212800165997
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Most proteoglycans are heterogeneous molecules composed of a protein core with glycosaminoglycans (GAGs) attached. GAGs are highly negatively charged molecules that readily bind to enzymes, growth factors, cytokines etc. and as such have many functions. The role played by proteoglycans in diabetes has only r...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170125154915
更新日期:2017-01-01 00:00:00