Novel ligands: fine tuning the transcriptional activity of the glucocorticoid receptor.

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：BACKGROUND:Central serous chorioretinopathy (CSC) is the fourth most frequent retinal disorder in terms of prevalence. It typically occurs in young subjects and affects men more often than women. CSC is characterized by serous retinal detachment (SRD) involving mainly the macular area. The clinical course is usually se...

journal_title：Current pharmaceutical design

authors： Iacono P,Toto L,Costanzo E,Varano M,Parravano MC

更新日期：2018-01-01 00:00:00

abstract：:The typical way of judging about either the efficacy of a new treatment or, on the contrary, the damage of a pollutant agent is through a test of hypothesis having its ineffectiveness as null hypothesis. This is the typical operational field of Kolmogorov's statistical framework where wastes of data (for instance non ...

journal_title：Current pharmaceutical design

authors： Apolloni B,Bassis S,Gaito S,Malchiodi D

更新日期：2007-01-01 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：: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：:Cyclooxygenase-1 (COX-1) derived eicosanoids promote gastroprotective mucosal defenses and induce platelet aggregation. By sparing COX-1, COX-2 specific inhibitors provide effective anti-inflammatory and analgesic activity while substantially reducing the risk of peptic ulcer disease and GI bleeding compared to dual C...

journal_title：Current pharmaceutical design

authors： Scheiman JM

更新日期：2003-01-01 00:00:00

abstract：:Quinone based bioreductive drugs have, potentially, a very versatile use in cancer chemotherapy. They can be activated by DT-diaphorase and hence can be used to target tumour types rich in this (O2)-independent reductase enzyme. Small molecular modifications can substantially reduce specificity for DT-diaphorase and u...

journal_title：Current pharmaceutical design

authors： McNally VA,Patterson AV,Williams KJ,Cowen RL,Stratford IJ,Jaffar M

更新日期：2002-01-01 00:00:00

abstract：:Cumulative scientific evidence gathered over the past ten years has confirmed the role of platelet GP IIb/IIIa inhibitors in reducing ischemic complications of patients undergoing percutaneous coronary intervention (PCI). Recently, mortality data available on more than 20,000 patients enrolled in randomized clinical t...

journal_title：Current pharmaceutical design

authors： Dery JP,Harrington RA,Tcheng JE

更新日期：2004-01-01 00:00:00

abstract：:Backgound: Current drug therapy for the management of arterial hypertension and heart failure has provided substantial benefits but has also some limitations. LCZ696, a dual inhibitor of angiotensin receptor blockers and neprilysin, and finerenone, a non-steroidal mineralocorticoid receptor antagonist, are two recentl...

journal_title：Current pharmaceutical design

authors： Faselis C,Boutari C,Doumas M,Imprialos K,Stavropoulos K,Kokkinos P

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:Sodium-glucose cotransporter 2 inhibitors (SGLT2i) are a novel category of oral antidiabetic drugs that inhibit renal glucose reabsorption and increase renal glucose excretion, thus lowering plasma glucose levels. This unique mechanism of SGLT2i action is insulin independent, thus improving glycemic control ...

journal_title：Current pharmaceutical design

authors： Katsiki N,Mikhailidis DP,Theodorakis MJ

更新日期：2017-01-01 00:00:00

abstract：:Philosophers have been trying to solve the mind-body problem for hundreds of years. Consciousness is the core of this problem: How do subjective conscious sensations, perceptions, feelings, and thoughts arise out of objective physical brain activities? How is this subjective conscious world in causal interaction with ...

journal_title：Current pharmaceutical design

authors： Långsjo JW,Revonsuo A,Scheinin H

更新日期：2014-01-01 00:00:00

abstract：:Chemotherapy is one of the most frequently employed and reliable treatment options for the management of a variety of cancers. Taxanes (paclitaxel, docetaxel and cabazitaxel) are frequently prescribed to treat breast cancer, hormone refractory prostate cancer, non-small cell lung cancer and ovarian cancer. Most of the...

journal_title：Current pharmaceutical design

authors： Kumar P,Raza K,Kaushik L,Malik R,Arora S,Katare OP

更新日期：2016-01-01 00:00:00

abstract：:The tumor cell growth inhibitory activities (log 1/GI(50)) of 166 anticancer agents studied at the National Cancer Institute (NCI) in vitro anticancer screening program have allowed us to analyze the relative importance of physicochemical parameters in influencing the inhibitory activities. Increased molecular weight,...

journal_title：Current pharmaceutical design

authors： Ren SS,Lien EJ

更新日期：2004-01-01 00:00:00

abstract：:Gene therapy, currently, represents one of the new therapies that have emerged for the treatment of different diseases. Between the different approaches that can be chosen concerning this therapy, gene delivery with non-viral systems has focused the attention during the past decades, because of the reduced toxicity co...

journal_title：Current pharmaceutical design

authors： Urbiola K,Blanco-Fernandez L,de Ilarduya CT

更新日期：2015-01-01 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

authors： Zhao J,Zhu H,Wang S,Ma X,Liu X,Wang C,Zhao H,Fan S,Jin X,Zhao B,Zhao T,Jia L,Wang K,Zou Y,Hu K,Sun A,Ge J

更新日期：2013-01-01 00:00:00

abstract：:The hypothesis that the interaction of agouti-related protein (AGRP) and the melanocortin-4 receptor (MC4R) modulates feeding behavior in humans has stimulated the synthesis of conformationally constrained peptides, peptoids and small molecules in efforts to identify novel compounds that can potentially be used in the...

journal_title：Current pharmaceutical design

authors： Wang X,Richards NG

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND:Antiepileptic treatment strategy plays an important role in the management of intracranial vascular malformations. The intracranial vascular malformations can be divided into cavernous hemangiomas, arteriovenous malformations, developmental venous anomalies and capillary telangiectasias. Seizures and hemorrh...

journal_title：Current pharmaceutical design

authors： Giakoumettis D,Margetis K,Stranjalis G,Haliasos N,Papaioannou TG,Themistocleous MS

更新日期：2017-01-01 00:00:00

abstract：:Acute kidney injury (AKI) is relatively common in patients undergoing transcatheter aortic valve implantation (TAVI) and has been associated with increased mortality and worse outcomes. The administration of iodinated contrast media in an elderly population with increased rates of chronic kidney injury and heart failu...

journal_title：Current pharmaceutical design

authors： Kampaktsis PN,Feldman DN,Charitakis K

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Non-alcoholic fatty liver disease (NAFLD) is a global epidemic involving 20-40% of the general population. NAFLD is rapidly becoming the leading cause of hepatocellular carcinoma (HCC) worldwide. Knowledge about NAFLD-HCC peculiar features is needed to understand this emerging disease better. OBJECTIVE:To r...

journal_title：Current pharmaceutical design

authors： Tovoli F,Ferri S,Piscaglia F

更新日期：2020-01-01 00:00:00

abstract：:The term endozepines designates a family of astroglia-secreted proteins including the diazepambinding inhibitor (DBI) and its processing products, which have been originally isolated and characterized as endogenous ligands of benzodiazepine receptors. It is now clearly established that the octadecaneuropeptide ODN (DB...

journal_title：Current pharmaceutical design

authors： Masmoudi-Kouki O,Hamdi Y,Ghouili I,Bahdoudi S,Kaddour H,Leprince J,Castel H,Vaudry H,Amri M,Vaudry D,Tonon MC

更新日期：2018-01-01 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：:Estrogens are known as important modulators of development, growth and maintenance of primary sexual physiology. The medical field has also grown increasingly appreciative of the effects of estrogens on non-traditional target tissues such as bone, cardiovascular tissue and the CNS. Postmenopausal women have been the b...

journal_title：Current pharmaceutical design

authors： Miller CP

更新日期：2002-01-01 00:00:00

abstract：:Transforming growth factor-β family members, which include TGF-βs, activins and bone morphogenetic proteins (BMPs), play important roles in development and maintaining tissue homeostasis. The extracellular TGF-β family members signal across the plasmamembrane by activating type I and type II serine/threonine kinase re...

journal_title：Current pharmaceutical design

authors： de Gorter DJ,Jankipersadsing V,Ten Dijke P

更新日期：2012-01-01 00:00:00

abstract：:In the early 1980s, an "atypical" beta-adrenergic receptor was discovered and subsequently called the beta (3)-adrenoceptor (beta(3)-AR). Agonists of the beta(3)-AR were observed to simultaneously increase lipolysis, fat oxidation, energy expenditure and insulin action leading to the belief that this receptor might se...

journal_title：Current pharmaceutical design

authors： de Souza CJ,Burkey BF

更新日期：2001-09-01 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

authors： Guslandi M

更新日期：2014-01-01 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：:Histone deacetylases (HDACs) are important enzymes that effect post-translational modifications of proteins by altering the acetylation state of lysine residues. HDACs control epigenetic changes that trigger cell transformation and proliferation of transformed cells associated with many diseases. These enzymes are val...

journal_title：Current pharmaceutical design

authors： Andrews KT,Tran TN,Fairlie DP

更新日期：2012-01-01 00:00:00

abstract：:Tumor metastasis is an important prognostic factor regarding long-term survival rate of cancer patients. At present, no imaging modality or technique is ideal for diagnosis of metastases. Molecular imaging has provided a fantastic tool for tumor metastases imaging. Based on the current medical imaging tools such as ma...

journal_title：Current pharmaceutical design

authors： Qiao R,Zhu R,Gao M

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:In the field of forensic toxicology, the quality of analytical methods is of great importance to ensure the reliability of results and to avoid unjustified legal consequences. A key to high quality analytical methods is a thorough method development. METHODS:The presented article will provide an overview on...

journal_title：Current pharmaceutical design

authors： Peters FT,Wissenbach DK,Busardo FP,Marchei E,Pichini S

更新日期：2017-01-01 00:00:00

abstract：:Transpeptidation reactions result in the formation of new peptide bonds and this can occur between two separate peptides or within the one peptide. These reactions are catalyzed by enzymes and when the N- and C-terminus of the one peptide are joined it results in the formation of cyclic proteins. Cyclization via head-...

journal_title：Current pharmaceutical design

authors： Conlan BF,Anderson MA

更新日期：2011-12-01 00:00:00