abstract：:Oncology remains an increasingly important focus of therapeutic development yet there remain many scientific and operational bottlenecks to deliver optimum treatments efficiently. Radiopharmaceuticals constitute a group of methodologies able to support the many stages of drug development. Methods such as [(18)F]-FDG-P...

journal_title：Current pharmaceutical design

authors： Murphy PS,Bergström M

更新日期：2009-01-01 00:00:00

abstract：:The maintenance and regulation of cellular NAD(P)(H) content and its influence on cell function involves many metabolic pathways, some of which remain poorly understood. Niacin deficiency in humans, which leads to low NAD status, causes sun sensitivity in skin, indicative of deficiencies in responding to UV damage. An...

journal_title：Current pharmaceutical design

authors： Benavente CA,Jacobson MK,Jacobson EL

更新日期：2009-01-01 00:00:00

abstract：:Packaging small-molecule drugs into nanoparticles improves their bio-availability, bio-compatibility and safety profiles. Multifunctional particles carrying large drug payloads for targeted transport, immune evasion and favourable drug release kinetics at the target site, require a certain minimum size usually 30-300 ...

journal_title：Current pharmaceutical design

authors： Debbage P

更新日期：2009-01-01 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

authors： Nichols WW,Epstein BJ

更新日期：2009-01-01 00:00:00

abstract：:The American Academy of Pediatrics has proposed guidelines for treating term/near term infants with hyperbilirubinemia based primarily on maintaining the total serum bilirubin concentration (TSB) below a "critical" level of 25 mg/dL (426 micromol/L). We estimated the sensitivity and specificity of this critical TSB us...

journal_title：Current pharmaceutical design

authors： Wennberg RP,Ahlfors CE,Aravkin AY

更新日期：2009-01-01 00:00:00

abstract：:Reactive oxygen species (ROS), as well as reactive nitrogen species (RNS) play either harmful or beneficial role in biological systems. Beneficial effects of ROS include physiological roles in cellular responses against infectious agents and in several cellular signalling pathways. Harmful effects are due to high conc...

journal_title：Current pharmaceutical design

authors： Balsano C,Alisi A

更新日期：2009-01-01 00:00:00

abstract：:Type 2 diabetes is associated with substantially increased cardiovascular mortality. The need to reduce the progression of atherosclerosis alongside lowering blood glucose levels is now well established. Ideally, pharmaceutical treatment should address both of these needs. This review summarises current evidence of th...

journal_title：Current pharmaceutical design

authors： Papanas N,Maltezos E

更新日期：2009-01-01 00:00:00

abstract：:Over the last years a number of reports have described elevated numbers of regulatory T (Treg) cells inside of tumors, in close proximity of the tumor, draining lymph nodes and also in peripheral blood of patients with solid tumors and hematologic malignancies. There is increasing evidence that Treg cells can migrate ...

journal_title：Current pharmaceutical design

authors： Beyer M,Schultze JL

更新日期：2009-01-01 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

authors： Tousoulis D,Kampoli AM,Papageorgiou N,Papaoikonomou S,Antoniades C,Stefanadis C

更新日期：2009-01-01 00:00:00

abstract：:This article reviews evidence that hyperpolarization-activated, cation nonselective (HCN) channels, the molecular basis of the Ih current, potentially represent valid targets for novel analgesic agents. Ih is a prominent current in many peripheral sensory nerves, with highest current density typically found in large d...

journal_title：Current pharmaceutical design

authors： Wickenden AD,Maher MP,Chaplan SR

更新日期：2009-01-01 00:00:00

abstract：:LIM (Lin-11, Isl-1, Mec-3), RING (Really interesting new gene), PHD (Plant homology domain) and MYND (myeloid, Nervy, DEAF-1) domains are all zinc-binding domains that ligate two zinc ions. Unlike the better known classical zinc fingers, these domains do not bind DNA, but instead mediate interactions with other protei...

journal_title：Current pharmaceutical design

authors： Matthews JM,Bhati M,Lehtomaki E,Mansfield RE,Cubeddu L,Mackay JP

更新日期：2009-01-01 00:00:00

abstract：:Cancer therapies through ionizing radiation or chemotherapeutic treatment may result in DNA double strand breaks (DSBs) in cell. DNA-PK has emerged as an attractive target for drug discovery efforts toward DSBs repair and in V(D)J recombination. Hence, the search for potent and selective DNA-PK inhibitors has received...

journal_title：Current pharmaceutical design

authors： Cao R,Zeng H,Zhang H

更新日期：2009-01-01 00:00:00

abstract：:Crohn's disease and ulcerative colitis are the two principal forms of inflammatory bowel disease (IBD). The root causes of these chronic and acute immunological disorders are unclear, but intestinal microorganisms are known to play a key role in the initiation and maintenance of disease. However, at present, there is ...

journal_title：Current pharmaceutical design

authors： Macfarlane GT,Blackett KL,Nakayama T,Steed H,Macfarlane S

更新日期：2009-01-01 00:00:00

abstract：:Agomelatine markedly differs from other classes of antidepressant drugs: its primary molecular targets in vivo are the melatonin MT(1) and MT(2) receptors, where it acts as a potent agonist, and the 5-HT(2C) receptors, where it exerts clear-cut antagonist properties. Agomelatine across a wide range of clinical trials ...

journal_title：Current pharmaceutical design

authors： Bourin M,Prica C

更新日期：2009-01-01 00:00:00

abstract：:Kv7.x channels are a family of six transmembrane domain, single pore-loop, voltage-gated K(+) channels. Five members of the family have been identified to date, including the cardiac channel Kv7.1 (formerly known as KvLQT1) and four neuronal Kv7.x channels, Kv7.2-5. Heteromeric channels containing Kv7.3 and either Kv7...

journal_title：Current pharmaceutical design

authors： Wickenden AD,McNaughton-Smith G

更新日期：2009-01-01 00:00:00

abstract：:There is growing evidence for the involvement of glutamatergic abnormalities in schizophrenia. Uncompetitive NMDA receptor (NMDAR) antagonists induce effects closely resembling both the positive and negative symptoms of schizophrenia; candidate risk genes for schizophrenia converge on the NMDAR expressing synapse; and...

journal_title：Current pharmaceutical design

authors： Stone JM

更新日期：2009-01-01 00:00:00

abstract：:Immunotoxins (ITs) are protein-based drugs combining a target-specific binding domain (usually derived from an antibody) and a cytotoxic domain to kill target cells. They are among the most promising new therapeutic tools to fight cancer, and several clinical trials have been completed with encouraging results. Althou...

journal_title：Current pharmaceutical design

authors： Hetzel C,Bachran C,Tur MK,Fuchs H,Stöcker M

更新日期：2009-01-01 00:00:00

abstract：:Human embryonic stem cells (hESCs) and induced pluripotent stem cells (hiPSCs) can self-renew indefinitely, while maintaining the capacity to differentiate into useful somatic cell types, including cardiomyocytes. As such, these stem cell types represent an essentially inexhaustible source of committed human cardiomyo...

journal_title：Current pharmaceutical design

authors： Shiba Y,Hauch KD,Laflamme MA

更新日期：2009-01-01 00:00:00

abstract：:Protein stability of hypoxia-inducible factor (HIF)alpha subunits is regulated by the oxygen-sensing prolyl-4-hydroxylase domain (PHD) enzymes. Under oxygen-limited conditions, HIFalpha subunits are stabilized and form active HIF transcription factors that induce a large number of genes involved in adaptation to hypox...

journal_title：Current pharmaceutical design

authors： Wenger RH,Camenisch G,Stiehl DP,Katschinski DM

更新日期：2009-01-01 00:00:00

abstract：:Aspirin is the cornerstone of treatment in patients with coronary artery disease. However, several studies investigating the in vitro response of platelets to the administration of aspirin showed this response to be variable, with some patients exhibiting non-responsiveness or resistance. Aspirin resistance may be cat...

journal_title：Current pharmaceutical design

authors： Papathanasiou A,Goudevenos J,Tselepis AD

更新日期：2009-01-01 00:00:00

abstract：:Regulatory T lymphocytes (Tregs) are specialized for immune suppression and are important regulators of the immune response in various settings. Tregs actively suppress enteroantigen-reactive cells and contribute to the maintenance of intestinal immune homeostasis. Distinct Treg subsets coexist in the intestinal mucos...

journal_title：Current pharmaceutical design

authors： Mizrahi M,Ilan Y

更新日期：2009-01-01 00:00:00

abstract：:Extracellular matrix (ECM) is composed of large collagen fibrils. Glycoproteins, such as fibronectin, can bind to collagen or form their own networks. Collagen fibrils are also decorated by proteoglycans, proteins that have large glycosaminoglycan sidechains. In addition, extracellular space often contains hyaluronan,...

journal_title：Current pharmaceutical design

authors： Heino J,Käpylä J

更新日期：2009-01-01 00:00:00

abstract：:The prevalence of type 2 diabetes is rising at an alarming rate worldwide. Coronary artery disease (CAD) is the leading cause of morbidity and mortality in the diabetic population. Future CAD risk should be routinely assessed in patients with diabetes as specific subgroups might benefit from information derived from c...

journal_title：Current pharmaceutical design

authors： Karastergiou K,Kaski JC

更新日期：2008-01-01 00:00:00

abstract：:An integrative synthesis of concepts and an explosion of experimental and epidemiological findings allow new insights as to how the interactions of genetic, environmental, dietary, cultural (social, psychological, economic) factors can influence the aging and diseases of aging processes. Although the net effect of the...

journal_title：Current pharmaceutical design

authors： Trosko JE

更新日期：2008-01-01 00:00:00

abstract：:Neuromuscular blocking agents are the leading drugs responsible for immediate hypersensitivity reactions during anaesthesia. Most hypersensitivity reactions represent IgE-mediated allergic reactions. Their incidence is estimated to be between 1 in 3,000 to 1 in 110,000 general anaesthetics. However striking variations...

journal_title：Current pharmaceutical design

authors： Mertes PM,Aimone-Gastin I,Guéant-Rodriguez RM,Mouton-Faivre C,Audibert G,O'Brien J,Frendt D,Brezeanu M,Bouaziz H,Guéant JL

更新日期：2008-01-01 00:00:00

abstract：:The current gold standard for imaging infection is radiolabeled white blood cells. For reasons of safety, simplicity and cost, it would be desirable to have a receptor-specific ligand that could be used for imaging infection and that would allow a differential diagnosis between sterile and septic inflammatory processe...

journal_title：Current pharmaceutical design

authors： Chianelli M,Boerman OC,Malviya G,Galli F,Oyen WJ,Signore A

更新日期：2008-01-01 00:00:00

abstract：:Tumour resistance to anticancer agents remains a challenge in oncological practice, because it results in exposure to toxicities, unnecessary costs and, most importantly, delay of a potentially more effective treatment. Drug uptake by tumours may be impaired by several resistance pathways. Reasons for primary resistan...

journal_title：Current pharmaceutical design

authors： van der Veldt AA,Luurtsema G,Lubberink M,Lammertsma AA,Hendrikse NH

更新日期：2008-01-01 00:00:00

abstract：:In the last two decades quantitative electroencephalogram (EEG) analysis has been widely used to investigate the neurophysiological characteristics of insomnia. These studies provided evidence in support of the hypothesis that primary insomnia is associated with hyperarousal of central nervous system and altered sleep...

journal_title：Current pharmaceutical design

authors： Marzano C,Ferrara M,Sforza E,De Gennaro L

更新日期：2008-01-01 00:00:00

abstract：:Anxiety disorders are common and disabling conditions. Current drug treatment methods have limitations including resistance, delayed efficacy and side effects. The advent of sophisticated imaging techniques and the production of highly selective receptor ligands have increased our knowledge of the biological mechanism...

journal_title：Current pharmaceutical design

authors： Christmas D,Hood S,Nutt D

更新日期：2008-01-01 00:00:00

abstract：:Cellular uptake of therapeutic oligonucleotides and subsequent intracellular trafficking to their target sites represents the major technical hurdle for the biological effectiveness of these potential drugs. Accordingly, laboratories worldwide focus on the development of suitable delivery systems. Among the different ...

journal_title：Current pharmaceutical design

authors： Laufer SD,Restle T

更新日期：2008-01-01 00:00:00

abstract：:Atherosclerosis is a multifactorial and long-lasting process in humans. Therefore, animal models where more rapid changes occur can be useful for the study of this process. Among such models are the apolipoprotein (apo) E knock out mice. Apo E deficient mice show impaired clearing of plasma lipoproteins and they devel...

journal_title：Current pharmaceutical design

authors： Kolovou G,Anagnostopoulou K,Mikhailidis DP,Cokkinos DV

更新日期：2008-01-01 00:00:00

abstract：:Heme oxygenase-1 (HO-1) catalyzes the degradation of heme to generate carbon monoxide, biliverdin and free iron. Increased HO-1 levels constitute an anatomopathological feature of many neurological diseases, such as neurodegenerative disorders and brain infections, which correlate with exacerbated oxidative stress and...

journal_title：Current pharmaceutical design

authors： Cuadrado A,Rojo AI

更新日期：2008-01-01 00:00:00

abstract：:Supraventricular tachycardias (SVTs) are observed in 0,1-0,4% of the paediatric population and represent an important clinical problem with related significant health and social issues. Most tachycardias are paroxysmal, being associated with sudden onset and termination, and only a relatively small number of them is p...

journal_title：Current pharmaceutical design

authors： Calabrò MP,Cerrito M,Luzza F,Oreto G

更新日期：2008-01-01 00:00:00

abstract：:Ablation has become an important treatment for many pediatric patients with common supraventricular tachycardias (SVTs). Many multicenter studies have documented that radiofrequency (RF) catheter ablation is a safe and effective procedure for treatment of a large variety of SVTs in children and adults with a high succ...

journal_title：Current pharmaceutical design

authors： De Santis A,Fazio G,Silvetti MS,Drago F

更新日期：2008-01-01 00:00:00

abstract：:About 50 peptides, and a similar number of peptide receptors, are known to be present in the gut and this amount is likely to rise significantly over the next few years. While there has been a massive research effort to define their functions and their anatomical distribution in the central nervous system (CNS), the u...

journal_title：Current pharmaceutical design

authors： Motilva V,Talero E,Calvo JR,Villegas I,Alarcón-de-la-Lastra C,Sánchez-Fidalgo S

更新日期：2008-01-01 00:00:00

abstract：:The integrin family of cell surface receptors were principally thought to be involved in cell adhesion. Intense study has shown that these glycoproteins also regulate a diverse range of physiological processes. Inappropriate activation of integrins has been implicated in many pathological processes. Recent studies hav...

journal_title：Current pharmaceutical design

authors： Robertson JH,Iga AM,Sales KM,Winslet MC,Seifalian AM

更新日期：2008-01-01 00:00:00

abstract：:The involvement of the central nervous system (CNS) is one of the major causes of morbidity and mortality in systemic lupus erythematosus (SLE) patients and the less understood aspect of the disease. Its recognition and treatment continue to represent a major diagnostic and therapeutic challenge. Due to the lack of co...

journal_title：Current pharmaceutical design

authors： Sanna G,Bertolaccini ML,Khamashta MA

更新日期：2008-01-01 00:00:00

abstract：:The concept of probiotics has evolved immensely since it was first proposed a century ago. There are numerous potential health benefits attributed to certain probiotic bacteria, from preventing gastrointestinal (GI) infections to stimulating the immune system. Recent evidence is now quite compelling for a role of prob...

journal_title：Current pharmaceutical design

authors： O'Sullivan DJ

更新日期：2008-01-01 00:00:00

abstract：:Adenosine A(2A)-dopamine D(2) receptor interactions play a very important role in striatal function. A(2A)-D(2) receptor interactions provide an example of the capabilities of information processing by just two different G protein-coupled receptors. Thus, there is evidence for the coexistence of two reciprocal antagon...

journal_title：Current pharmaceutical design

authors： Ferré S,Quiroz C,Woods AS,Cunha R,Popoli P,Ciruela F,Lluis C,Franco R,Azdad K,Schiffmann SN

更新日期：2008-01-01 00:00:00

abstract：:Growth and metastasis of lung cancer requires a sequence of events, which alter the ability of neoplastic cells to adhere to themselves, to normal surrounding cells, or to the extracellular matrix. Interactions between cells are primarily mediated by four types of structures in the plasma membrane: gap junctions, tigh...

journal_title：Current pharmaceutical design

authors： Syrigos KN,Katirtzoglou N,Kotteas E,Harrington K

更新日期：2008-01-01 00:00:00