Advances in the discovery of novel antibacterial agents during the year 2002.

abstract：:The purinergic receptor P2X7 is highly expressed in immune peripheral and central cells suggesting its important role in numerous diseases characterized by inflammatory processes like cancer, or neurodegenerative pathologies in relation with modulation of the immune system. Thereby, antagonization of this receptor may...

journal_title：Current medicinal chemistry

authors： Baudelet D,Lipka E,Millet R,Ghinet A

更新日期：2015-01-01 00:00:00

abstract：:Type 2 diabetes mellitus (DM) is a public health burden and its co-existence with hypertension is long established in the context of the metabolic syndrome. Both DM and hypertension are major risk factors, for end-stage renal disease, cardiovascular events and mortality. Strict blood pressure (BP) control in diabetics...

journal_title：Current medicinal chemistry

authors： Loutradis C,Papadopoulou E,Angeloudi E,Karagiannis A,Sarafidis P

更新日期：2020-01-01 00:00:00

abstract：:Inflammation plays a critical role in the atherosclerotic process in various vascular beds, starting from endothelial dysfunction and counting all stages of plaque development. The significant contribution of inflammation in the initiation and progression of atherosclerosis has been documented over many years but its ...

journal_title：Current medicinal chemistry

authors： Vavuranakis M,Kariori M,Vrachatis D,Siasos G,Kalogeras K,Bei E,Moldovan C,Lavda M,Aznaouridis K,Oikonomou E,Tousoulis D

更新日期：2015-01-01 00:00:00

abstract：:Platinum complex-based chemotherapy is one of the major treatment options of many malignancies. Although severe side effects occur, and only a limited spectrum of tumors can be cured, Pt compounds are used in every second therapy scheme. Thus, many different drug design strategies have been employed for improving the ...

journal_title：Current medicinal chemistry

authors： Hartinger CG,Nazarov AA,Ashraf SM,Dyson PJ,Keppler BK

更新日期：2008-01-01 00:00:00

abstract：:Mammalian terminal deoxyribonucleotidyl transferase (TDT) catalyzes the non-template-directed polymerization of deoxyribonucleoside triphosphates and has a key role in V(D)J recombination during lymphocyte and repertoire development. Over 90% of leukemic cells in acute lymphocytic leukemia and approximately 30% of leu...

journal_title：Current medicinal chemistry

authors： Di Santo R,Maga G

更新日期：2006-01-01 00:00:00

abstract：:Reversible phosphorylation is a key mechanism for regulating the biological activity of many human proteins that affect a diverse array of cellular processes, including protein-protein interactions, gene transcription, cell-cycle progression and apoptosis. Once viewed as simple house keeping enzymes, recent studies ha...

journal_title：Current medicinal chemistry

authors： Honkanen RE,Golden T

更新日期：2002-11-01 00:00:00

abstract：:The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA synthetases (AaRS). Aminoacyl-tRNA synthetases are the...

journal_title：Current medicinal chemistry

authors： Lv PC,Zhu HL

更新日期：2012-01-01 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：:Human immunodeficiency virus (HIV) infection commonly results in a myriad of comorbid conditions secondary to immune deficiency. Infection also affects broad organ system function. Although current antiretroviral therapy (ART) reduces disease morbidity and mortality through effective control of peripheral viral load, ...

journal_title：Current medicinal chemistry

authors： Edagwa BJ,Zhou T,McMillan JM,Liu XM,Gendelman HE

更新日期：2014-01-01 00:00:00

abstract：:Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in Diabetes Mellitus (DM) and contributes to the develo...

journal_title：Current medicinal chemistry

authors： Tentolouris A,Eleftheriadou I,Tzeravini E,Tsilingiris D,Paschou SA,Siasos G,Tentolouris N

更新日期：2020-01-01 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：: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：:The discovery of anandamide as an endogenous ligand for the cannabinoid receptors has led to a resurgence of interest in the fatty acid amides. However, N-palmitoylethanolamine (PEA), a shorter and fully saturated analogue of anandamide, has been known since the fifties. This endogenous compound is a member of the N-a...

journal_title：Current medicinal chemistry

authors： Lambert DM,Vandevoorde S,Jonsson KO,Fowler CJ

更新日期：2002-03-01 00:00:00

abstract：:Demyelination occurs in several central nervous system (CNS) disorders, including multiple sclerosis, viral infection and spinal cord injury and can result in severe functional impairment. Therefore there is great interest in developing therapies promoting repair in CNS demyelinating diseases and trauma. Cell replacem...

journal_title：Current medicinal chemistry

authors： Lavdas AA,Papastefanaki F,Thomaidou D,Matsas R

更新日期：2008-01-01 00:00:00

abstract：:HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounde...

journal_title：Current medicinal chemistry

authors： Chen X,Zhan P,Li D,De Clercq E,Liu X

更新日期：2011-01-01 00:00:00

abstract：:Paediatric Acquired ImmunoDeficiency Syndrome (AIDS) is a life-threatening and infectious disease in which the Human Immunodeficiency Virus (HIV) is mainly transmitted through Mother-To- Child Transmission (MTCT) during pregnancy, labour and delivery, or breastfeeding. This review provides an overview of the distinct ...

journal_title：Current medicinal chemistry

authors： Melo R,Lemos A,Preto AJ,Bueschbell B,Matos-Filipe P,Barreto C,Almeida JG,Silva RDM,Correia JDG,Moreira IS

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:Whilst knowledge of basic biology, diagnosis and prognosis of glioblastoma (GB - WHO grade IV) are steadily improving, advancements of therapy are discouragingly slow, with the only significant novelty during last ten years represented by introduction of temozolomide in chemotherapy. In order to analyze the current st...

journal_title：Current medicinal chemistry

authors： Frosina G

更新日期：2015-01-01 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：:Cancer is the world's second leading cause of death after heart diseases, and involves abnormal cell growth at a primary site and the potential to spread to other parts of the body. Tumors are highly heterogeneous and consist of subgroups of cells with distinct characteristics. Of these, the cancer stem cells (CSC) ni...

journal_title：Current medicinal chemistry

authors： Vizetto-Duarte C,Branco PC,Custódio L

更新日期：2020-03-20 00:00:00

abstract：:Chagas disease is an infectious tropical disease included within the group of neglected tropical diseases. Though historically endemic to Latin America, it has lately spread to high-income countries due to human migration. At present, there are only two available drugs, nifurtimox and benznidazole, approved for this t...

journal_title：Current medicinal chemistry

authors： Bellera CL,Alberca LN,Sbaraglini ML,Talevi A

更新日期：2020-01-01 00:00:00

abstract：:The biological relevance of sulfur containing carbohydrates is gaining substantial attention. Thus the new developments, especially in the synthetic and medicinal chemistry of thio-sugars are critically important for carbohydrate drug design. New studies of biological processes including biosynthetic reactions and enz...

journal_title：Current medicinal chemistry

authors： Witczak ZJ

更新日期：1999-02-01 00:00:00

abstract：:Preterm labour is a major cause of perinatal mortality and morbidity. However, during the past 40 years of clinical studies and despite the use of multiple therapeutic agents, the rate of preterm birth has not drastically declined. In 1991, it was estimated that in the US approximately 116,000 women admitted with acut...

journal_title：Current medicinal chemistry

authors： Schwarz MK,Page P

更新日期：2003-08-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

abstract：:The role of cell adhesion molecules (CAMs), such as intercellular cell adhesion molecule-1 (ICAM-1), vascular endothelial cell adhesion molecule-1 (VCAM-1), E-selectin, and P-selectin, has been studied extensively in the process of inflammation. These molecules are responsible for recruiting leukocytes onto the vascul...

journal_title：Current medicinal chemistry

authors： Kobayashi H,Boelte KC,Lin PC

更新日期：2007-01-01 00:00:00

abstract：:Specific noncovalent interactions that are indicative of attractive, directional intermolecular forces have always been of key interest to medicinal chemists in their search for the "glue" that holds drugs and their targets together. With the rapid increase in the number of solved biomolecular structures as well as th...

journal_title：Current medicinal chemistry

authors： Zhou P,Huang J,Tian F

更新日期：2012-01-01 00:00:00

abstract：:Inflammation is an initial response of the body to a harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions ...

journal_title：Current medicinal chemistry

authors： Soubhye J,Aldib I,Delporte C,Prévost M,Dufrasne F,Antwerpen PV

更新日期：2016-01-01 00:00:00

abstract：:Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...

journal_title：Current medicinal chemistry

authors： Bedin C,Crotti S,Tasciotti E,Agostini M

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:With global increase in elderly population, modern societies must find strategies to reduce the consequences of aging process; thereby decreasing the incidence of age-related neurodegenerative diseases. Oxidative stress and recently inflammation, have been pointed out as the leading causes of brain aging. Th...

journal_title：Current medicinal chemistry

authors： Sarubbo F,Moranta D,Asensio VJ,Miralles A,Esteban S

更新日期：2017-01-01 00:00:00

abstract：:In situ hybridization (ISH) is a type of hybridization that uses a labeled complementary DNA or RNA strand to localize a specific DNA or RNA sequence on a chromosome or section of tissue (in-situ) fixed on a slide. Flourescence in-situ hybridization (FISH) technique facilitates the localization of genes to different c...

journal_title：Current medicinal chemistry

authors： Jehan Z,Uddin S,Al-Kuraya KS

更新日期：2012-01-01 00:00:00