abstract：:The number of protein 3D structures without function annotation in Protein Data Bank (PDB) has been steadily increased. Many of these proteins are relevant for Pharmaceutical Design because they may be enzymes of different classes that could become drug targets. This fact has led in turn to an increment of demand for ...

journal_title：Current pharmaceutical design

authors： Concu R,Podda G,Ubeira FM,González-Díaz H

更新日期：2010-01-01 00:00:00

abstract：:Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which catalyze CO(2) hydration to bicarbonate and protons. Five genetically distinct classes are known, which represent an excellent example of convergent evolution. Inhibition of α-CAs from vertebrates, including humans, with sulfonamides was exploited clinical...

journal_title：Current pharmaceutical design

authors： Supuran CT

更新日期：2010-01-01 00:00:00

abstract：:Arterial thromboembolism is a sudden obstruction of arterial blood flow caused by dislodgment of a blood clot from the site of its formation. Atrial fibrillation (AF) is the most common cardiac arrhythmia and a major risk factor for arterial thromboembolism in clinical practice. Most of AF-related arterial thromboembo...

journal_title：Current pharmaceutical design

authors： Potpara TS,Lip GY

更新日期：2010-01-01 00:00:00

abstract：:Androgen receptor (AR) is a steroid hormone receptor that is activated by endogenous androgens, mainly testosterone and 5alpha-dihydrotestosterone (5alpha-DHT). AR is also an important drug target, and AR antagonists (antiandrogens) have been widely used for prostate cancer therapy. Antiandrogens currently available o...

journal_title：Current pharmaceutical design

authors： Gao W

更新日期：2010-01-01 00:00:00

abstract：:The heart is a sophisticated endocrine gland synthesizing a family of peptide hormones by three different genes. These cardiac hormones are stored as 3 prohormones, i.e. atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP) and C-type natriuretic peptide (CNP) prohormones. Within the ANP prohormones are 4 ...

journal_title：Current pharmaceutical design

authors： Vesely DL

更新日期：2010-01-01 00:00:00

abstract：:Senescence is defined as an irreversible growth arrest that is characterised by a changed morphology, gene expression pattern and chromatin structure as well as an activated DNA damage response. Senescence has a dual role for tumour development-it acts as a tumour suppressor to prevent the proliferation of seriously d...

journal_title：Current pharmaceutical design

authors： Saretzki G

更新日期：2010-01-01 00:00:00

abstract：:A large body of evidence on brain development and ageing has revealed that inflammatory processes profoundly affect brain functions during life span of mammalians, including humans. Activation of innate immune mechanisms leading to pro-inflammatory cytokine up-regulation is involved in devastating and disabling human ...

journal_title：Current pharmaceutical design

authors： Bossù P,Ciaramella A,Salani F,Vanni D,Palladino I,Caltagirone C,Scapigliati G

更新日期：2010-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common neurodegenerative disorder that affects the elderly. The increase of life-expectancy is transforming AD into a major health-care problem. AD is characterized by a progressive impairment of memory and other cognitive skills leading to dementia. The major pathogenic factor ass...

journal_title：Current pharmaceutical design

authors： Agostinho P,Cunha RA,Oliveira C

更新日期：2010-01-01 00:00:00

abstract：:Immunosenescence is considered a major contributory factor to the increased frequency of morbidity and mortality among elderly. On the other hand centenarians are considered the best example of successful ageing. To gain insight into mechanisms of immunosenescence and its clinical relevance, a possible model is repres...

journal_title：Current pharmaceutical design

authors： Colonna-Romano G,Buffa S,Bulati M,Candore G,Lio D,Pellicanò M,Vasto S,Caruso C

更新日期：2010-01-01 00:00:00

abstract：:Multiple molecular, cellular, structural and functional changes occur in the brain during aging. Neural cells may respond to these changes adaptively by employing multiple mechanisms in order to maintain the integrity of nerve cell circuits and to facilitate responses to environmental demands. Otherwise, they may succ...

journal_title：Current pharmaceutical design

authors： Lanni C,Stanga S,Racchi M,Govoni S

更新日期：2010-01-01 00:00:00

abstract：:A positive relationship between stress tolerance and longevity has been observed in several model systems. That the same correlation is applicable in humans and that it may be open to experimental manipulation for extending human lifespan requires studies on association of stress genes with longevity. The involvement ...

journal_title：Current pharmaceutical design

authors： Singh R,Kølvraa S,Bross P,Christensen K,Bathum L,Gregersen N,Tan Q,Rattan SI

更新日期：2010-01-01 00:00:00

abstract：:The in vitro effects of goat's milk from different sources (Jonica, Saanen, and Priska breeds plus a commercial preparation) on healthy human peripheral blood mononuclear cells (PBMCs) were evaluated in terms of nitric oxide (NO) and cytokine release. According to the incubation time (24 h or 48 h) used all milks coul...

journal_title：Current pharmaceutical design

authors： Jirillo F,Martemucci G,D'Alessandro AG,Panaro MA,Cianciulli A,Superbo M,Jirillo E,Magrone T

更新日期：2010-01-01 00:00:00

abstract：:Stem cell therapy heralds a new chapter in cardiovascular regenerative medicine. Cardiovascular implants are often used in both surgery and interventional cardiology. Cardiovascular stents are utilized in percutaneous coronary interventions (PCI), and are classified as either bare metal stents (BMS) or drug-eluting st...

journal_title：Current pharmaceutical design

authors： Tan A,Sumpio BE,Lee S,Seifalian AM

更新日期：2010-01-01 00:00:00

abstract：:Over the last 15 years, the use of various biological therapies has largely improved the way we manage patients with Inflammatory Bowel Diseases (IBDs). Blockade of cytokine synthesis and/or activity is at the forefront of this new era with the success of inhibitors of tumor necrosis factor (TNF)-α. These therapies ar...

journal_title：Current pharmaceutical design

authors： De Nitto D,Sarra M,Cupi ML,Pallone F,Monteleone G

更新日期：2010-01-01 00:00:00

abstract：:Pancreatic cancer is hallmarked by aggressive biology and extreme lethality and very high mortality rates. The underlying molecular mechanism of its rapid development and progression is unclear, however. Recent identification and functional validation of nitric oxide (NO) production in pancreatic cancer suggest a role...

journal_title：Current pharmaceutical design

authors： Wang L,Xie K

更新日期：2010-01-01 00:00:00

abstract：:First generation drug-eluting stents (DES) have significantly improved the treatment options for patients with symptomatic coronary artery disease by decreasing rates of acute vessel closure and restenosis after percutaneous coronary revascularization procedures. However, early enthusiasm was temperd by reports of lat...

journal_title：Current pharmaceutical design

authors： Vorpahl M,Yazdani SK,Nakano M,Ladich E,Kolodgie FD,Finn AV,Virmani R

更新日期：2010-01-01 00:00:00

abstract：:Schizophrenia is a complex psychiatric disorder characterised by positive and negative symptoms, cognitive impairments, attentional problems, anxiety and depressive symptoms. The use of atypical antipsychotics has generally improved clinical outcome yet medical need remains in the treatment of this disease. The potent...

journal_title：Current pharmaceutical design

authors： McCreary AC,Jones CA

更新日期：2010-01-01 00:00:00

abstract：:Alcohol dependence is a major disease burden of adults in modern society worldwide. There is no cure for alcohol dependence. In this study, we have examined the molecular targets of ethanol-induced toxicity in humans based on a systematic review of literature data and then discussed current and potential therapeutic t...

journal_title：Current pharmaceutical design

authors： Wang LL,Yang AK,He SM,Liang J,Zhou ZW,Li Y,Zhou SF

更新日期：2010-01-01 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

authors： Stöllberger C,Finsterer J

更新日期：2010-01-01 00:00:00

abstract：:Understanding of the roles of RNAs within the cell has changed and expanded dramatically during the past few years. Based on fundamentally new insights it is now increasingly possible to employ RNAs as highly valuable tools in molecular biology and medicine. At present, the most important therapeutic strategies are ba...

journal_title：Current pharmaceutical design

authors： Poller W,Fechner H

更新日期：2010-01-01 00:00:00

abstract：:Genetic variation in the receptors and other intracellular targets that mediate the pharmacodynamic effects of drugs can affect therapeutic outcomes. However, at present greater knowledge is available concerning the extent of gene variation in drug metabolizing enzymes that determine drug pharmacokinetics and, in turn...

journal_title：Current pharmaceutical design

authors： Crettol S,Petrovic N,Murray M

更新日期：2010-01-01 00:00:00

abstract：:Bisphosphonates are widely use for pathologies such as osteoporosis, Paget's disease or bone metastasis. However, their potent antiresorptive properties open new therapeutic opportunities for other conditions associated with an increased focal or systemic bone remodelling. Moreover, apart from their antiresorptive act...

journal_title：Current pharmaceutical design

authors： Le Goff B,Berthelot JM,Maugars Y,Romas E

更新日期：2010-01-01 00:00:00

abstract：:Cancers which damage the human skeleton include multiple myeloma, where the primary tumour colonises bone directly, or breast and prostate cancer, where malignant cells travel from the primary tumour to form clonal outgrowths within the bone. Owing to the interaction of tumour cells with those normally found in the bo...

journal_title：Current pharmaceutical design

authors： Buckle CH,Neville-Webbe HL,Croucher PI,Lawson MA

更新日期：2010-01-01 00:00:00

abstract：:It is well known that heat shock proteins (HSPs) are induced by various stressors in order to confer protection against such stressors. Since stressor-induced tissue damage is involved in various diseases, especially gastrointestinal diseases, such as gastric ulcer, it has been thought that HSPs are protective against...

journal_title：Current pharmaceutical design

authors： Mizushima T

更新日期：2010-01-01 00:00:00

abstract：:In this review, the antimicrobial properties of a number of peptides are described. We first deal with helical linear peptides such as the well-known gramicidin, magainins, melittin, and other less well-known or more recently discovered peptides. Then, beta-sheet peptides (defensins isolated from insects and also from...

journal_title：Current pharmaceutical design

authors： Duclohier H

更新日期：2010-01-01 00:00:00

abstract：:By updating John Littleton's work published 15 years ago this review summarizes recent work on pharmacodynamic aspects of acamprosate and the perspective for future developments. In addition to insights into the role of glutamatergic receptor systems, craving and relapse inspired by acamprosate, clinical research poin...

journal_title：Current pharmaceutical design

authors： Kiefer F,Mann K

更新日期：2010-01-01 00:00:00

abstract：:Thiopurines are widely used in the treatment of inflammatory bowel disease (IBD). However, in clinical practice azathioprine (AZA) or 6-mercaptopurine (6-MP) are not effective in one-third of patients and up to one-fifth of patients discontinue thiopurine therapy due to adverse reactions. The observed interindividual ...

journal_title：Current pharmaceutical design

authors： Derijks LJ,Wong DR

更新日期：2010-01-01 00:00:00

abstract：:Polyunsaturated fatty acids (PUFA) are a family of lipids including some subgroups identified by the position of the last double bond in their structure. PUFA n-3 include alpha linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), while PUFA n-6 include linoleic acid (LA) and arachidonic a...

journal_title：Current pharmaceutical design

authors： Zuliani G,Galvani M,Leitersdorf E,Volpato S,Cavalieri M,Fellin R

更新日期：2009-01-01 00:00:00

abstract：:CD1 molecules are a family of non-polymorphic, class I antigen-presenting glycoproteins, which bind and present amphiphilic lipid antigens for recognition to T cells. Two groups of CD1 molecules are involved in presentation of self and foreign lipid antigens: group 1 (CD1a, CD1b and CD1c) and group 2 (CD1d). Crystal s...

journal_title：Current pharmaceutical design

authors： Schiefner A,Wilson IA

更新日期：2009-01-01 00:00:00

abstract：:Large doses of omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are used to treat several diseases including hypertriglyceridemia in humans. Modest levels of EPA and DHA may be obtained from food, particularly from fatty fish. This review presents the literature examining the differences ...

journal_title：Current pharmaceutical design

authors： Abete P,Testa G,Galizia G,Della-Morte D,Cacciatore F,Rengo F

更新日期：2009-01-01 00:00:00

abstract：:Metabolic syndrome (MetS) is a cluster of risk factors, each one individually associated with increased cardiovascular disease risk. Treatment of all components of MetS is expected to result in reduced risk. Treatment of MetS mainly includes lifestyle changes. In addition, drug therapy may be considered, especially co...

journal_title：Current pharmaceutical design

authors： Florentin M,Elisaf MS,Mikhailidis DP,Liberopoulos EN

更新日期：2009-01-01 00:00:00

abstract：:Recent progresses in the development of fluorescent technologies become a reliable device for drug discovery research. The fluorescence tools offer attractive options for an opportunity to visualize the effects of drug candidates in the cells. The fluorescent tools, such as fluorescent protein, are regularly used in a...

journal_title：Current pharmaceutical design

authors： Chakraborty C,Hsu CH,Wen ZH,Lin CS

更新日期：2009-01-01 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

authors： de Graaf C,Rognan D

更新日期：2009-01-01 00:00:00

abstract：:ADAM (a disintegrin and metalloproteinase) proteins have a predominant role in the protein ectodomain shedding of membrane-bound molecules. ADAMs have emerged as critical regulators of cell-cell signaling during development and homeostasis, and are believed to contribute to pathologies, such as cancer, where their reg...

journal_title：Current pharmaceutical design

authors： Peduto L

更新日期：2009-01-01 00:00:00

abstract：:Growth factors (GFs) are extracellular signaling polypeptides regulating cell proliferation, differentiation and survival. They exert a wide spectrum of biological activities selectively binding to and activating specific membrane receptors which then transfer the message to cell interior inducing specific biochemical...

journal_title：Current pharmaceutical design

authors： D'Andrea LD,Del Gatto A,De Rosa L,Romanelli A,Pedone C

更新日期：2009-01-01 00:00:00

abstract：:Evasion of apoptosis, the cell's intrinsic death program, is a hallmark of human cancers including neuroblastoma. Also, failure to undergo apoptosis may cause treatment resistance, since the cytotoxic activity of anticancer therapies commonly used in the clinic, e.g. chemotherapy, gamma-irradiation or immunotherapy, i...

journal_title：Current pharmaceutical design

authors： Fulda S

更新日期：2009-01-01 00:00:00

abstract：:Fibrates are widely prescribed lipid-lowering drug in the treatment of dyslipidemia. Their main clinical effects, mediated by peroxisome proliferative activated receptor (PPAR) alpha activation, are a moderate reduction in total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels, a marked reduction in ...

journal_title：Current pharmaceutical design

authors： Ansquer JC,Foucher C,Aubonnet P,Le Malicot K

更新日期：2009-01-01 00:00:00

abstract：:More and more evidences are still accumulating rapidly on the G-protein-coupled-receptors (GPCRs) dimerization/oligomerization. Such common feature of GPCRs has called extensive attention to both pharmacologists and medicinal chemists for illustration of the pharmacological functions and therapeutic utilities of such ...

journal_title：Current pharmaceutical design

authors： Liu Z,Zhang J,Zhang A

更新日期：2009-01-01 00:00:00

abstract：:Chemokines and their receptors play critical roles in leukocyte trafficking during inflammatory processes. Although the role of chemokine receptors (CKRs) in cancer biology is a relatively new field of study, a growing body of data suggest that a number of CKRs, including CXCR4, CCR4, CCR7, and CCR10, may play diverse...

journal_title：Current pharmaceutical design

authors： Wu X,Lee VC,Chevalier E,Hwang ST

更新日期：2009-01-01 00:00:00

abstract：:The pivotal therapeutic role of myocardial metabolic modulation in ischemic heart disease (IHD) is increasingly recognized. Among the others, inhibitors of free fatty acids (FFA) oxidation have been consistently shown to play an important role in the therapeutic strategy of IHD patients. Additionally, abnormalities of...

journal_title：Current pharmaceutical design

authors： Fragasso G,Salerno A,Spoladore R,Cera M,Montanaro C,Margonato A

更新日期：2009-01-01 00:00:00