Fluorescent GPCR ligands as new tools in pharmacology.

abstract：:Recent advances have identified the podocyte as a key target in glomerular injury. The podocyte is a highly specialized cell which is responsible for the glomerular permselectivity for proteins in the kidney. Podocyte injury or loss leads to proteinuria. Apoptosis has been shown to contribute to renal cell loss, inclu...

journal_title：Current medicinal chemistry

authors： Moreno JA,Sanchez-Niño MD,Sanz AB,Lassila M,Holthofer H,Blanco-Colio LM,Egido J,Ruiz-Ortega M,Ortiz A

更新日期：2008-01-01 00:00:00

abstract：:Neurodegenerative disorders (NDDs) like Alzheimer's disease, Parkinson's disease and Huntington's disease are a heterogeneous group of disorders with the progressive and severe loss of neurons. There are no full proof cures for these diseases, and only medicines are available that can alleviate some of the symptoms. D...

journal_title：Current medicinal chemistry

authors： Volcho KP,Laev SS,Ashraf GM,Aliev G,Salakhutdinov NF

更新日期：2018-01-01 00:00:00

abstract：:Flavonoids are major dietary constituents of plant-based food found ubiquitously in plant kingdom where they are usually present in substantial amounts. Rutin is a flavonol-type polyphenol which consists of the flavonol quercetin and the disaccharide rutinose. Rutin has been reported to exert diverse biological effect...

journal_title：Current medicinal chemistry

authors： Budzynska B,Faggio C,Kruk-Slomka M,Samec D,Nabavi SF,Sureda A,Devi KP,Nabavi SM

更新日期：2019-01-01 00:00:00

abstract：:ATP-sensitive K(+) channels (K(ATP)channels) regulate insulin secretion by coupling intracellular metabolic changes to excitability of the plasma membrane in pancreatic beta-cells. The channels are closed when extracellular glucose levels are elevated due to enhanced feature. By contrast, cardiac-type K(ATP) channels,...

journal_title：Current medicinal chemistry

authors： Kakei M

更新日期：2003-02-01 00:00:00

abstract：:Various human tumors preferentially metastasize by lymphatic route and lymphovascular invasion predicts lymph node metastasis. In this review article, we will summarize recent literature data concerning lymphangiogenesis, focusing on tumor lymphangiogenesis. In detail, we try to answer some important questions related...

journal_title：Current medicinal chemistry

authors： Raica M,Ribatti D

更新日期：2010-01-01 00:00:00

abstract：:Snakes are fascinating creatures and have been residents of this planet well before ancient humans dwelled the earth. Venomous snakes have been a figure of fear, and cause notable mortality throughout the world. The venom constitutes families of proteins and peptides with various isoforms that make it a cocktail of di...

journal_title：Current medicinal chemistry

authors： Waheed H,Moin SF,Choudhary MI

更新日期：2017-01-01 00:00:00

abstract：:MicroRNAs (miRNAs) translationally repressing their target messenger RNAs due to their gene-regulatory functions play an important but not unexpected role in a tumour development. More surprising are the findings that levels of various miRNAs are well correlated with presence of specific tumours and formation of metas...

journal_title：Current medicinal chemistry

authors： Pekarik V,Gumulec J,Masarik M,Kizek R,Adam V

更新日期：2013-01-01 00:00:00

abstract：:The new drug class of dipeptidyl peptidase-4 (DPP4) inhibitors has been widely accepted in the daily management of type 2 diabetes since its strategic advantages with regard to body weight, risk of hypoglycaemia, and beta cell survival. We have previously evaluated the theoretical implications of DPP4 inhibition given...

journal_title：Current medicinal chemistry

authors： Matteucci E,Giampietro O

更新日期：2011-01-01 00:00:00

abstract：:Adenosine is an important autocoid, exerting its physiological effects on the human body by activation of four different G-protein-coupled-receptors (GPCRs) classified as A(1), A(2A), A(2B), and A(3). These receptors are coupled to secondary messenger systems including adenylate cyclase, inositol phosphate metabolism,...

journal_title：Current medicinal chemistry

authors： Romagnoli R,Baraldi PG,Tabrizi MA,Gessi S,Borea PA,Merighi S

更新日期：2010-01-01 00:00:00

abstract：:Among the strategies that can lead to the discovery of new drugs, the identification and use of privileged structures, molecular fragments that are able to interact with more than one target, gained particular attention, in an attempt to find new drugs in a shorter time with respect to other strategies. These structur...

journal_title：Current medicinal chemistry

authors： Costantino L,Barlocco D

更新日期：2006-01-01 00:00:00

abstract：:The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：:TB drug development pipeline represents varied structural classes of molecules. Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR. They act by inhibiting translation at the initiation phase of protein...

journal_title：Current medicinal chemistry

authors： Jadhavar PS,Vaja MD,Dhameliya TM,Chakraborti AK

更新日期：2015-01-01 00:00:00

abstract：:The importance of organometallics can be noticed by their presence in all life organisms. The most known natural organometallic molecule is vitamin B12, a porphyrin containing a cobalt atom, useful for several enzymatic transformations. Based on the remarkable properties of this class of compounds, a new area of medic...

journal_title：Current medicinal chemistry

authors： Chavain N,Biot C

更新日期：2010-01-01 00:00:00

abstract：:Advanced enteropancreatic (EP) neuroendocrine tumors (NETs) can be treated with several different therapies, including chemotherapy, biotherapy, and locoregional treatments. Over the last few decades, impressive progress has been made in the biotherapy field. Three main druggable molecular targets have been studied an...

journal_title：Current medicinal chemistry

authors： Fazio N,Scarpa A,Falconi M

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Fatty liver, or steatosis, is a condition of excess accumulation of lipids, mainly under form of triglycerides (TG), in the liver, and it is the hallmark of non-alcoholic fatty liver disease (NAFLD). NAFLD is the most common liver disorder world-wide and it has frequently been associated with obesity, hyperl...

journal_title：Current medicinal chemistry

authors： Vergani L

更新日期：2019-01-01 00:00:00

abstract：:Transient Receptor Potential Melastatin-related 7 (TRPM7) is a non-selective cation channel fused with a functional kinase domain. Physiologically, TRPM7 channel is involved in magnesium homeostasis, cell survival and gastrulation. The channel part is responsible for calcium, magnesium, and metal trace entries. Cation...

journal_title：Current medicinal chemistry

authors： Gautier M,Perrière M,Monet M,Vanlaeys A,Korichneva I,Dhennin-Duthille I,Ouadid-Ahidouch H

更新日期：2016-01-01 00:00:00

abstract：:RNA aptamers are non-coding small RNAs that bind to their cognate targets with high specificity and affinity. They are generally identified by iterative rounds of in vitro selection termed SELEX (Systemic Evolution of Ligands by Exponential Enrichment). Similar to antibodies, they can inhibit, modulate and disrupt the...

journal_title：Current medicinal chemistry

authors： Li Y,Wu H,Niu Y,Hu Y,Li Q,Cao C,Cai J

更新日期：2013-01-01 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：:β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...

journal_title：Current medicinal chemistry

authors： Rochais C,Rault S,Dallemagne P

更新日期：2010-01-01 00:00:00

abstract：:Functioning of G protein-coupled receptors (GPCRs) is tightly linked to the membrane environment, but a molecular level understanding of the modulation of GPCR by membrane lipids is not available. However, specific receptor-lipid interactions as well as unspecific effects mediated by the bulk properties of the membran...

journal_title：Current medicinal chemistry

authors： Sadiq SK,Guixa-Gonzalez R,Dainese E,Pastor M,De Fabritiis G,Selent J

更新日期：2013-01-01 00:00:00

abstract：OBJECTIVE:We found a novel marine drug, SZ-685C, that was isolated from the secondary metabolites of a mangrove endophytic fungus (No. 1403) collected from the South China Sea, which has been reported to inhibit the proliferation of certain tumor cells. However, its anticancer mechanism remains unknown. The aims of thi...

journal_title：Current medicinal chemistry

authors： Chen CH,Xiao WW,Jiang XB,Wang JW,Mao ZG,Lei N,Fan X,Song BB,Liao CX,Wang HJ,She ZG,Zhu YH

更新日期：2013-01-01 00:00:00

abstract：:The cellular response to DNA damage is critical for determining whether carcinogenesis, cell death or other deleterious biological effects will ensue. Numerous cellular enzymatic mechanisms can directly repair damaged DNA, or allow tolerance of DNA lesions, and thus reduce potential harmful effects. These processes in...

journal_title：Current medicinal chemistry

authors： Lieberman HB

更新日期：2008-01-01 00:00:00

abstract：:Mast cells are best known as central effector cells in IgE-mediated type I allergic diseases including asthma and hay fever. An increasing amount of evidence, however, has demonstrated that mast cells are sentinel cells playing a critical role in host defense against invading microbes. Mast cells are located immediate...

journal_title：Current medicinal chemistry

authors： Matsuguchi T

更新日期：2012-01-01 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

abstract：:gammadelta T lymphocytes are involved in the defence from viral and mycobacterial infections; however they are also responsible for autoimmune reactions. Herein, we discuss the characteristics of these cells, focusing on the mechanism(s) underlying extravasation and tissue localization. We show that Vdelta1 and Vdelta...

journal_title：Current medicinal chemistry

authors： Poggi A,Catellani S,Fenoglio D,Borsellino G,Battistini L,Zocchi MR

更新日期：2007-01-01 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：:A number of amine-boranes and related derivatives possess a wide range of biological activities including antineoplastic, antiviral, hypolipidemic, anti-inflammatory activities, anti-osteoporotic and dopamine receptor antagonist activities. The compounds include borane complexes of alpha-amino acids, aromatic, aliphat...

journal_title：Current medicinal chemistry

authors： Burnham BS

更新日期：2005-01-01 00:00:00

abstract：:Endothelial cells (ECs) play a pivotal role in physiological and altered tissue neovascularization. They face multiple morphological, biochemical and functional changes during the different phases of angiogenesis, under the regulation of a great number of proangiogenic and antiangiogenic signals, including soluble and...

journal_title：Current medicinal chemistry

authors： Munaron L,Fiorio Pla A

更新日期：2009-01-01 00:00:00

abstract：:Non-small cell lung cancer (NSCLC) remains a fatal disease: the majority of patients are diagnosed as having metastases or advanced inoperable tumors. The activity of chemotherapy in NSCLC patients is low with objective response rarely complete and sustained. Cisplatin-based combinations are considered as the standard...

journal_title：Current medicinal chemistry

authors： Gridelli C,De Vivo R

更新日期：2002-04-01 00:00:00

abstract：BACKGROUND:Diabetic nephropathy (DN) is an important diabetic microvascular complication, and it is becoming the leading cause of end-stage renal disease worldwide. Unfortunately, there are no effective therapies to treat established DN. Therefore, new therapeutic targets are urgently required. Accumulating studies ind...

journal_title：Current medicinal chemistry

authors： Yang S,Han Y,Liu J,Song P,Xu X,Zhao L,Hu C,Xiao L,Liu F,Zhang H,Sun L

更新日期：2017-01-01 00:00:00