Novel inhibitors of AKT: assessment of a different approach targeting the pleckstrin homology domain.

abstract：:Calcium is essential for many metabolic process, including nerve function, muscle contraction, and blood clotting. The metabolic pathways that contribute to maintain serum calcium levels are bone remodeling processes, intestinal absorption and secretion, and renal handling, but hypercalcemia occurs when at least 2 of ...

journal_title：Current medicinal chemistry

authors： Lumachi F,Motta R,Cecchin D,Ave S,Camozzi V,Basso SM,Luisetto G

更新日期：2011-01-01 00:00:00

abstract：:For more than 20 years there has been increasing interest in the development of novel therapies to raise levels of high-density lipoprotein cholesterol (HDL-C). However, well publicized failures of recent clinical trials of agents that raise HDL-C levels have stimulated considerable controversy with regard to the pote...

journal_title：Current medicinal chemistry

authors： Duong M,Nicholls SJ

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Considerable evidence demonstrates the importance of dithiocarbamates especially disulfiram as anticancer drugs. However there are no systematic reviews outlining how their metal-binding ability is related to their anticancer activity. This review aims to summarize chemical features and metal-binding activit...

journal_title：Current medicinal chemistry

authors： Viola-Rhenals M,Patel KR,Jaimes-Santamaria L,Wu G,Liu J,Dou QP

更新日期：2018-02-12 00:00:00

abstract：:The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to prov...

journal_title：Current medicinal chemistry

authors： Matute MS,Matute R,Merino P

更新日期：2016-01-01 00:00:00

abstract：:Natural products are regarded as vital key source of lead compounds for drug discovery due to their structural diversity and broad array of biological activities. Phenylpropanoid sucrose esters are naturally occurring compounds isolated from various plants and are structurally characterized by a sucrose core connected...

journal_title：Current medicinal chemistry

authors： Panda P,Appalashetti M,Judeh ZM

更新日期：2011-01-01 00:00:00

abstract：:Rutin (quercetin-3-O-rutinoside) is a multifunctional natural flavonoid glycoside with profound effects on the various cellular functions under pathological conditions. Due to the ability of rutin and/or its metabolites to cross the blood brain barrier, it has also been shown to modify the cognitive and various behavi...

journal_title：Current medicinal chemistry

authors： Habtemariam S

更新日期：2016-01-01 00:00:00

abstract：:Dendritic cells (DCs) are the most powerful antigen-presenting cells which link the innate and adaptive immune responses. Depending on the context DCs initiate the immune responses or contribute to immune tolerance. Any disturbance in their phenotypes and functions may initiate inflammatory or autoimmune diseases. Hen...

journal_title：Current medicinal chemistry

authors： Rahimi K,Hassanzadeh K,Khanbabaei H,Haftcheshmeh SM,Ahmadi A,Izadpanah E,Mohammadi A,Sahebkar A

更新日期：2020-05-14 00:00:00

abstract：BACKGROUND:Research on Chromogranin A (CGA) and its derived fragments convincingly demonstrated the multifunctional activity of the 21 amino acid peptide named Catestatin (CST: human CGA352-372, bovine CGA344-364, rat CGA367-387). This review aims to provide a synopsis of the current information concerning the biologic...

journal_title：Current medicinal chemistry

authors： Pasqua T,Angelone T,Spena A,Cerra MC

更新日期：2017-01-01 00:00:00

abstract：:Drug repositioning is a strategy to identify new uses for approved or investigational drugs that are used off-label outside the scope of the original medical indication. In this review we report the most relevant studies about drug repositioning in hematology, reporting the signalling pathways and molecular targets of...

journal_title：Current medicinal chemistry

authors： Allegra A,Imbesi C,Bitto A,Ettari R

更新日期：2020-08-16 00:00:00

abstract：:The transport mechanisms of ascorbic acid (AA) are described. The metabolism of AA and its function as an antioxidant are covered in some detail. Subsequently, indications for postoperative substitution are discussed. The supplementation of up to 300 mg of AA per day in postoperative intensive care unit patients durin...

journal_title：Current medicinal chemistry

authors： Rümelin A

更新日期：2009-01-01 00:00:00

abstract：:Although it has become acceptable that neuroretinal cells are also affected in diabetes, vascular lesions continue to be considered as the hallmarks of diabetic retinopathy. Animal models are essential for the understanding and treatment of human diabetic retinopathy, and the mouse is intensively used as a model becau...

journal_title：Current medicinal chemistry

authors： Ramos D,Carretero A,Navarro M,Mendes-Jorge L,Nacher V,Rodriguez-Baeza A,Ruberte J

更新日期：2013-01-01 00:00:00

abstract：:Over the past few years, use of the genome-wide association study (GWAS) has made it possible to identify the primary genetic mechanisms of essential hypertension. GWAS results have helped identify many loci in or near genes that generally were not expected to be associated with blood pressure or essential hypertensio...

journal_title：Current medicinal chemistry

authors： Pan S,Naruse H,Nakayama T

更新日期：2015-01-01 00:00:00

abstract：:Analytical chemists have increasingly turned their attention to drug discovery and drug analysis and to solve fundamental questions of biological significance in physiology and genetics. New technologies have been developed, and a variety of instruments have been redesigned for biomedical applications. The development...

journal_title：Current medicinal chemistry

authors： Hanai T

更新日期：2005-01-01 00:00:00

abstract：:Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharma...

journal_title：Current medicinal chemistry

authors： Álvarez R,Aramburu L,Puebla P,Caballero E,González M,Vicente A,Medarde M,Peláez R

更新日期：2016-01-01 00:00:00

abstract：:Since the outbreak of SARS (severe acute respiratory syndrome) in November 2002 in Southern China's Guangdong Province, considerable progress has been made in the development of drugs for SARS therapy. The present mini review is focused on the area of computer-aided drug discovery, i.e., the advances achieved mainly f...

journal_title：Current medicinal chemistry

authors： Chou KC,Wei DQ,Du QS,Sirois S,Zhong WZ

更新日期：2006-01-01 00:00:00

abstract：:Coumarins, also referred as benzopyran-2-ones, and their corresponding nitrogen counterpart, 1-azacoumarins also referred to as carbostyrils, are a family of nature-occurring lactones and lactams respectively. The plant extracts containing coumarin-related heterocycles, which were employed as herbal remedies in early ...

journal_title：Current medicinal chemistry

authors： Kulkarni MV,Kulkarni GM,Lin CH,Sun CM

更新日期：2006-01-01 00:00:00

abstract：:The blood-brain barrier (BBB) impedes the influx of intravascular compounds from the blood to the brain. The elements composing the BBB are endothelial cells, pericytes and the end-feet of astrocytes. Among them, the endothelial cell barrier line is the most critical for preventing toxic substances from entering the b...

journal_title：Current medicinal chemistry

authors： Ueno M

更新日期：2007-01-01 00:00:00

abstract：:Two-component signal transduction systems and their expanded variants known as phosphorelays are integral elements of the virulence and antimicrobial resistance responses of a wide range of pathogenic bacteria and fungi and also regulate essential functions. As a consequence, two-component systems and phosphorelays ar...

journal_title：Current medicinal chemistry

authors： Stephenson K,Hoch JA

更新日期：2004-03-01 00:00:00

abstract：:Atrial fibrillation represents a major clinical, social and economical matter, and its importance is expected to increase even more in the near future. The progressive ageing of population is associated with an inevitable rising in incidence and prevalence of this rhythm disorder, which limits functional capability, f...

journal_title：Current medicinal chemistry

authors： Lombardi F,Terranova P

更新日期：2006-01-01 00:00:00

abstract：:APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...

journal_title：Current medicinal chemistry

authors： Zhang X,Xu W

更新日期：2008-01-01 00:00:00

abstract：:COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...

journal_title：Current medicinal chemistry

authors： Cui J,Jia J

更新日期：2020-09-17 00:00:00

abstract：:We examined a large number of sudden infant death syndrome victims in order to point out a possible causal relationship between a previous hexavalent vaccination and the sudden infant death. We selected 110 cases submitted to in-depth histological examination of the autonomic nervous system and provided with detailed ...

journal_title：Current medicinal chemistry

authors： Matturri L,Del Corno G,Lavezzi AM

更新日期：2014-03-01 00:00:00

abstract：:Complement plays a vital role in our innate immune defense against invasive microorganisms. Excessive complement activation or insufficient control of activation on host cells, however, is associated with several chronic disorders. Essential to the activation and amplification of the Alternative Pathway (AP) of comple...

journal_title：Current medicinal chemistry

authors： Wiles JA,Galvan MD,Podos SD,Geffner M,Huang M

更新日期：2020-01-01 00:00:00

abstract：:To this point, efforts to develop therapeutic peptides for intracellular applications were guided by the perception that unmodified linear peptides are highly unstable and therefore structural modifications are required to reduce proteolytic breakdown. Largely, this concept is a consequence of the fact that most resea...

journal_title：Current medicinal chemistry

authors： Zuconelli CR,Brock R,Adjobo-Hermans MJW

更新日期：2017-01-01 00:00:00

abstract：:Photodynamic therapy (PDT) is a novel medical technique involving three key components: light, a photosensitizer molecule and molecular oxygen, which are essential to achieve the therapeutic effect. There has been great interest in the use of PDT in the treatment of many cancers and skin disorders. Upon irradiation wi...

journal_title：Current medicinal chemistry

authors： Skupin-Mrugalska P,Sobotta L,Kucinska M,Murias M,Mielcarek J,Düzgüneş N

更新日期：2014-01-01 00:00:00

abstract：:Bile formation is an osmotic process driven by the vectorial transport of actively transferred biliary components across the basolateral (sinusoidal) and apical (canalicular) hepatocyte membranes, the latter being the rate-limiting step of the overall blood-to-bile transfer. The ATP-binding cassette (ABC) superfamily ...

journal_title：Current medicinal chemistry

authors： Crocenzi FA,Mottino AD,Roma MG

更新日期：2004-02-01 00:00:00

abstract：OBJECTIVES:Post-exercise cardiac troponin T (cTnT) release has been widely reported in adult athletes but limited data is available for adolescents. The aim of this study was to determine the incidence and magnitude of cTnT appearance in a large group of adolescent runners, and to determine any association between cTnT...

journal_title：Current medicinal chemistry

authors： Nie J,George KP,Tong TK,Gaze D,Tian Y,Lin H,Shi Q

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Resveratrol, a natural polyphenol product, is used in plant defense from fungal and microbial aggression. It is found naturally, especially in plants such as grapes, peanuts, and berries. It has the highest concentrations in blueberries, mulberries, blackberries, and the skin of red grapes. Resveratrol has v...

journal_title：Current medicinal chemistry

authors： Kumar S,Chang YC,Lai KH,Hwang TL

更新日期：2020-09-17 00:00:00

abstract：:Inosine monophosphate dehydrogenase (IMPDH) catalyzes the conversion of IMP to XMP with the concomitant reduction of NAD to NADH. This reaction is the rate-limiting step in guanine nucleotide biosynthesis. IMPDH is a proven target for immunosuppressive, anticancer and antiviral chemotherapy, and may also be a target f...

journal_title：Current medicinal chemistry

authors： Hedstrom L

更新日期：1999-07-01 00:00:00

abstract：:This update covers the literature for 2002 and 2003 dealing with the main topic of the previous review entitled Heterocyclic nucleosides. Chemical synthesis and biological properties and published in Curr. Med. Chem.-AIA, 2002, 1, 389. As in the first review, the papers in this survey are grouped by the type of the he...

journal_title：Current medicinal chemistry

authors： Merino P

更新日期：2006-01-01 00:00:00