abstract：:Drug designing targeting protein-protein interactions is challenging. Because structural elucidation and computational analysis have revealed the importance of hot spot residues in stabilizing these interactions, there have been on-going efforts to develop drugs which bind the hot spots and out-compete the native prot...

journal_title：Current pharmaceutical design

authors： Ma B,Nussinov R

更新日期：2014-01-01 00:00:00

abstract：:Sex-dependent differences are frequently observed in the biological and behavioural effects of substances of abuse, including cannabis. We recently demonstrated a modulating effect of sex and oestrous cycle on cannabinoid-taking and seeking behaviours. Here, we investigated the influence of sex and oestrogen in the re...

journal_title：Current pharmaceutical design

authors： Castelli MP,Fadda P,Casu A,Spano MS,Casti A,Fratta W,Fattore L

更新日期：2014-01-01 00:00:00

abstract：:Telomerase is a specialized enzymatic complex responsible for the synthesis of telomeric repeats 5'-TTAGGG-3' localized at the ends of eukaryotic chromosomes. This mechanism prevents shortening of telomeres after each cell division. The enzyme is detected in about 85% of human tumors, but it is not expressed in normal...

journal_title：Current pharmaceutical design

authors： Romaniuk A,Kopczynski P,Ksiazek K,Rubis B

更新日期：2014-01-01 00:00:00

abstract：:The influence of mitochondrial dysfunction on pathological states involving inflammatory and/or oxidative stress in tissues that do not show frank cellular apoptosis or necrosis has been rather difficult to unravel, and the literature is replete with contradictory information. Although such discrepancies have many pot...

journal_title：Current pharmaceutical design

authors： Suliman HB,Piantadosi CA

更新日期：2014-01-01 00:00:00

abstract：:We set up two models of gastric bleeding in rats using low-dose aspirin (ASA) and the antiplatelet drug clopidogrel, a P2Y₁₂ receptor antagonist, and examined the effect of antiulcer drugs on gastric bleeding and ulcerogenic responses under such conditions. Under urethane anesthesia, two catheters were inserted into t...

journal_title：Current pharmaceutical design

authors： Takeuchi K,Izuhara C,Takayama S,Momode T,Kojo M,Hara D,Amagase K

更新日期：2014-01-01 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

authors： Casoli T,Balietti M,Giorgetti B,Solazzi M,Scarpino O,Fattoretti P

更新日期：2013-01-01 00:00:00

abstract：:The cystic fibrosis transmembrane conductance regulator (CFTR) protein is a cAMP-regulated Cl- channel whose major function is to facilitate epithelial fluid secretion. Loss-of-function mutations in CFTR cause the genetic disease cystic fibrosis. CFTR is required for transepithelial fluid transport in certain secretor...

journal_title：Current pharmaceutical design

authors： Verkman AS,Synder D,Tradtrantip L,Thiagarajah JR,Anderson MO

更新日期：2013-01-01 00:00:00

abstract：:Low density lipoproteins (LDL) and high density lipoproteins (HDL) are independent risk factors for coronary heart disease (CHD); decreasing LDL-cholesterol (LDL-C) levels with statin therapy represents the primary goal in the management of cardiovascular disease. However, despite the efficacy of statins in reducing c...

journal_title：Current pharmaceutical design

authors： Pirillo A,Norata GD,Catapano AL

更新日期：2013-01-01 00:00:00

abstract：:Abnormal regulation of the ubiquitin-proteasome system (UPS) has been known to be involved in the pathogenesis of a variety of human diseases. A number of studies have focused on the identification of small modifiers for the UPS. Even though the proteasome inhibitor Bortezomib (Velcade®) has been approved for the ther...

journal_title：Current pharmaceutical design

authors： Lim KH,Baek KH

更新日期：2013-01-01 00:00:00

abstract：:Rapid increase in the emergence and spread of microbes resistant to conventionally used antibiotics has become a major threat to global health care. Antimicrobial peptides (AMPs) are considered as a potential source of novel antibiotics because of their numerous advantages such as broad-spectrum activity, lower tenden...

journal_title：Current pharmaceutical design

authors： Lohan S,Bisht GS

更新日期：2013-01-01 00:00:00

abstract：:DARPins (designed ankyrin repeat proteins), new kinds of binding proteins, have the potential to overcome the defects of monoclonal antibodies, and hence may become the alternatives to antibodies and generate a novel therapeutic approach. DARPins can be selected to bind any given target proteins with high affinity and...

journal_title：Current pharmaceutical design

authors： Wu X,Shi Y,Ren P,Wang D,Li G

更新日期：2013-01-01 00:00:00

abstract：:Cytokines are known to play a key role in regulation of gastric functions. Interferon-alpha (IFN-α) has been published to impair gastric motility. Aims of this study were to clarify effect of IFN-α on gastric acid secretion (GAS) and determine role of nitric oxide (NO) in the process. Both subcutaneous (1000, 10000, 1...

journal_title：Current pharmaceutical design

authors： Czimmer J,Király Á,Szabó IL,Mózsik G,Sütő G

更新日期：2013-01-01 00:00:00

abstract：:The signal transducer and activator of transcription 3 (STAT3) transduces stress signals from the plasma membrane to the nucleus but has recently also been identified in mitochondria. Inhibition of cardiomyocyte mitochondrial STAT3 with the STAT3-specific inhibitor Stattic decreases ADP-stimulated respiration and enha...

journal_title：Current pharmaceutical design

authors： Boengler K,Ungefug E,Heusch G,Schulz R

更新日期：2013-01-01 00:00:00

abstract：:No-reflow, i.e., the lack of distal myocardial perfusion to fully recover following recanalization of an acutely occluded coronary artery, is not only a mere consequence of ischemic injury, as substantial microvascular alterations may also develop subsequently, after initial restoration of perfusion. Since part of per...

journal_title：Current pharmaceutical design

authors： Tritto I,Zuchi C,Vitale S,Ambrosio G

更新日期：2013-01-01 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

authors： Yoffe S,Leshuk T,Everett P,Gu F

更新日期：2013-01-01 00:00:00

abstract：:In this review we discuss the role of protonation states in receptor-ligand interactions, providing experimental evidences and computational predictions that complex formation may involve titratable groups with unusual pKa's and that protonation states frequently change from unbound to bound states. These protonation ...

journal_title：Current pharmaceutical design

authors： Petukh M,Stefl S,Alexov E

更新日期：2013-01-01 00:00:00

abstract：:Free energy simulations are a powerful tool to study molecular recognition. The most rigorous variants can provide in depth understanding for a particular system, but are not suited for high throughput application to large libraries of compounds. Related, but less expensive methods are increasingly popular, including ...

journal_title：Current pharmaceutical design

authors： Simonson T

更新日期：2013-01-01 00:00:00

abstract：OBJECTIVES:This paper reviews literary evidence on antithrombotic therapies currently employed in TAVR to assess validity and efficacy; duration and modality are also considered. In the absence of firm guidelines and reliable trial results, we analyze current knowledge of interaction between PPI and antithrombotic drug...

journal_title：Current pharmaceutical design

authors： Fusari M

更新日期：2013-01-01 00:00:00

abstract：:Nonalcoholic fatty liver disease (NAFLD) affects about 20%-30% of the general population, and its clinical relevance arises from the fact that 20%-30% of these subjects develop non-alcoholic steatohepatitis (NASH), a condition at risk of cirrhosis progression. In addition NAFLD, and in particular NASH patients, are al...

journal_title：Current pharmaceutical design

authors： Petta S,Handberg A,Craxì A

更新日期：2013-01-01 00:00:00

abstract：:Deubiquitinating enzymes (DUBs) remove ubiquitin and ubiquitin-like modifications from proteins and they have been known to contribute to processes relevant in microbial infection, such as immune responses pathways. Numerous viral and bacterial DUBs have been identified, and activities of several host DUBs are known t...

journal_title：Current pharmaceutical design

authors： Nanduri B,Suvarnapunya AE,Venkatesan M,Edelmann MJ

更新日期：2013-01-01 00:00:00

abstract：:During the last two decades, the studies on ubiquitination in regulating transcription factor NF-κB activation have elucidated the expanding role of ubiquitination in modulating cellular events by non-proteolytic mechanisms, as well as by proteasomal degradation. The significance of ubiquitination has also been recogn...

journal_title：Current pharmaceutical design

authors： Wu ZH,Shi Y

更新日期：2013-01-01 00:00:00

abstract：:Recent advances in the fabrication, characterization and application of micro- and nano-particles that possess a non-uniform internal structure are reviewed. The particle structures include core-shell particles, particles with multiple cores or a multi-layered structure, porous particles with both regular and random p...

journal_title：Current pharmaceutical design

authors： Čejková J,Štêpánek F

更新日期：2013-01-01 00:00:00

abstract：:The clinically most relevant medications for lipid management are the statins, which constitute in the majority of the cases the basis of any lipid-modulating therapy. However, other agents are often needed to either reduce low-density cholesterol to target levels and/or to treat residual serum lipoprotein abnormaliti...

journal_title：Current pharmaceutical design

authors： Gouni-Berthold I,Berthold HK

更新日期：2013-01-01 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

authors： Hofbauer A,Stoger E

更新日期：2013-01-01 00:00:00

abstract：:Single-agent therapy with molecularly targeted agents has shown limited success in tumor growth control, mainly because escape or resistance mechanisms are activated once a signalling molecule is inhibited. Rational combinations of target-specific agents could counteract this response providing a useful strategy in ca...

journal_title：Current pharmaceutical design

authors： Porcelli L,Quatrale AE,Mantuano P,Silvestris N,Rolland JF,Biancolillo L,Paradiso A,Azzariti A

更新日期：2013-01-01 00:00:00

abstract：:In the last two decades the development of efficient plant-based expression strategies and new concepts for the purification of recombinant proteins prompted the application of plant-derived vaccines for veterinary purposes. The expression of recombinant proteins in plants possesses advantages over conventional eukary...

journal_title：Current pharmaceutical design

authors： Phan HT,Floss DM,Conrad U

更新日期：2013-01-01 00:00:00

abstract：:Stimulant use disorders are an unrelenting public health concern worldwide. Agonist replacement therapy is among the most effective strategies for managing substance use disorders including nicotine and opioid dependence. The present paper reviewed clinical data from human laboratory self-administration studies and cl...

journal_title：Current pharmaceutical design

authors： Stoops WW,Rush CR

更新日期：2013-01-01 00:00:00

abstract：:Nesfatin-1, derived from the precursor NEFA/nucleobindin2 (NUCB2), was initially identified as a feeding-suppressing neuropeptide, acting at central (mainly, hypothalamic) levels in a leptin-independent manner. However, recent experimental evidence strongly suggests that, rather than being a simple anorectic hypothala...

journal_title：Current pharmaceutical design

authors： García-Galiano D,Tena-Sempere M

更新日期：2013-01-01 00:00:00

abstract：:Hypertension and insomnia are very common and often coexist. There is evidence to suggest that the increasing prevalence of arterial hypertension in the past decade might be related both to an increased prevalence of insomnia and to the decline of sleep duration due to modern lifestyle. The aim of this paper is to rec...

journal_title：Current pharmaceutical design

authors： Palagini L,Bruno RM,Gemignani A,Baglioni C,Ghiadoni L,Riemann D

更新日期：2013-01-01 00:00:00

abstract：:Heat shock proteins (HSPs) are involved in a number of cellular processes, including cell cycle, growth, and survival, apoptosis, stress responses, angiogenesis, and oncogenesis. Among the characterized HSPs, the molecular chaperone HSP90 has emerged as an exciting molecular target for cancer therapy since its discove...

journal_title：Current pharmaceutical design

authors： Kondoh Y,Osada H

更新日期：2013-01-01 00:00:00

abstract：:Nanogels are nanosized hydrogel particles formed by physical or chemical cross-linked polymer networks. The advantageous properties of nanogels related to the ability of retaining considerable amount of water, the biocompatibility of the polymers used, the ability to encapsulate and protect a large quantity of payload...

journal_title：Current pharmaceutical design

authors： Maya S,Sarmento B,Nair A,Rejinold NS,Nair SV,Jayakumar R

更新日期：2013-01-01 00:00:00

abstract：:Iron oxide (Fe₃O₄) nanoparticles (IONPs) have received much attention for their utility in biomedical applications such as magnetic resonance imaging, drug delivery and hyperthermia. Recent studies reported that IONPs induced cytotoxicity in mammalian cells. However, little is known about the genotoxicity of IONPs fol...

journal_title：Current pharmaceutical design

authors： Ahamed M,Alhadlaq HA,Alam J,Khan MA,Ali D,Alarafi S

更新日期：2013-01-01 00:00:00

abstract：:Serotonin (5-HT) is one of the main transmitters in the nervous system. Serotonergic neurons in the raphe nuclei in the brainstem innervate most parts of the central nervous system including motoneurons in the spinal cord and brainstem. This review will focus on the modulatory role that 5-HT exerts on motoneurons and ...

journal_title：Current pharmaceutical design

authors： Perrier JF,Rasmussen HB,Christensen RK,Petersen AV

更新日期：2013-01-01 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

authors： Arvanian V

更新日期：2013-01-01 00:00:00

abstract：:Since the discovery of human immunodeficiency virus (HIV) as a causative agent of acquired immune deficiency syndrome (AIDS) various strategies were employed to counter its devastating actions. One such concept relies on the prevention of HIV entry into host's "competent" cells by means of compounds known as entry inh...

journal_title：Current pharmaceutical design

authors： Micewicz ED,Ruchala P

更新日期：2013-01-01 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

authors： Andersson S,Mints M,Weiderpass E,Johansson B

更新日期：2013-01-01 00:00:00

abstract：:Periodontal diseases are common inflammatory conditions of the supporting apparatus of the teeth which lead to early tooth loss. This review discusses the evidence for a role of reactive oxygen species in inducing periodontal tissue damage and focuses on recent evidence showing increased local and systemic alterations...

journal_title：Current pharmaceutical design

authors： Nibali L,Donos N

更新日期：2013-01-01 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

authors： Schmid CA,Craig VJ,Müller A,Flori M

更新日期：2013-01-01 00:00:00

abstract：:The octapeptide angiotensin II (Ang II) plays a homeostatic role in the regulation of blood pressure and water and electrolyte balance, and also contributes to the progression of cardiovascular remodeling. Ang II activates Ang II type 1 (AT1) receptor and type 2 (AT2) receptor, both of which belong to the seven-transm...

journal_title：Current pharmaceutical design

authors： Akazawa H,Yano M,Yabumoto C,Kudo-Sakamoto Y,Komuro I

更新日期：2013-01-01 00:00:00

abstract：:In the classical renin angiotensin system (RAS), angiotensin II Ang IIplays many important roles in cardiovascular disease and in kidney, brain, and other organs via the Ang II type 1 receptor (AT1). The RAS consists of many angiotensin peptides, including Ang (1-7), Ang (1-9), Ang (2-8), and Ang IV. Ang (1-7), produc...

journal_title：Current pharmaceutical design

authors： Ohishi M,Yamamoto K,Rakugi H

更新日期：2013-01-01 00:00:00