The chemistry of transition metals in relation to their potential role in neurodegenerative processes.

abstract：:Many efforts are currently being made to connect small molecules to target proteins by extracting pharmacological data from bibliographic sources and storing them in annotated chemical libraries. Here, small molecules are further connected to biological pathways, with particular focus to pathways involving members of ...

journal_title：Current topics in medicinal chemistry

authors： Hettne K,Cases M,Boyer S,Mestres J

更新日期：2007-01-01 00:00:00

abstract：:Millions of deaths each year are attributed to malaria worldwide. Transmitted through the bite of an Anopheles mosquito, infection and subsequent death from the Plasmodium species, most notably P. falciparum, can readily spread through a susceptible population. A malaria vaccine does not exist and resistance to virtua...

journal_title：Current topics in medicinal chemistry

authors： Zhang VM,Chavchich M,Waters NC

更新日期：2012-01-01 00:00:00

abstract：:Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addr...

journal_title：Current topics in medicinal chemistry

authors： Wegscheid-Gerlach C,Gerber HD,Diederich WE

更新日期：2010-01-01 00:00:00

abstract：:An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administ...

journal_title：Current topics in medicinal chemistry

authors： Sharpe PC,Richardson DR,Kalinowski DS,Bernhardt PV

更新日期：2011-01-01 00:00:00

abstract：:Parkinson's disease is a motor dysfunction that has been widely studied but many of the reports on commercial drugs for the treatment of this disease have afforded some undesirable side effects that generate an extensive and unviable treatment by economic costs and due to the bioavailability of the assayed compounds. ...

journal_title：Current topics in medicinal chemistry

authors： Fazel Nabavi S,Uriarte E,Rastrelli L,Modak B,Sobarzo-Sánchez E

更新日期：2016-01-01 00:00:00

abstract：:A modified version of the CORAL software (http://www.insilico.eu/coral) allows building up the classification model for the case of the Yes/No data on the anti-sarcoma activity of organic compounds. Three random splits into the sub-training, calibration, and test sets of the data for 3017 compounds were examined. The ...

journal_title：Current topics in medicinal chemistry

authors： Toropov AA,Toropova AP,Benfenati E,Gini G,Leszczynska D,Leszczynski J

更新日期：2012-01-01 00:00:00

abstract：:Protein-ligand binding is among the most fundamental phenomena underlying all molecular biology, and a greater ability to more accurately and robustly predict the binding free energy of a small molecule ligand for its cognate protein is expected to have vast consequences for improving the efficiency of pharmaceutical ...

journal_title：Current topics in medicinal chemistry

authors： Abel R,Wang L,Mobley DL,Friesner RA

更新日期：2017-01-01 00:00:00

abstract：:The majority of functionally important biological processes are regulated by allosteric communication within individual proteins and across protein complexes. The proteins controlling these communication networks respond to changes in the cellular environment by switching between different conformational states. Targe...

journal_title：Current topics in medicinal chemistry

authors： Persico M,Di Dato A,Orteca N,Fattorusso C,Novellino E,Andreoli M,Ferlini C

更新日期：2015-01-01 00:00:00

abstract：:The recognition that malfunction of the microtubule (MT) associated protein tau is likely to play a defining role in the onset and/or progression of a number of neurodegenerative diseases, including Alzheimer's disease, has resulted in the initiation of drug discovery programs that target this protein. Tau is an endog...

journal_title：Current topics in medicinal chemistry

authors： Ballatore C,Brunden KR,Trojanowski JQ,Lee VM,Smith AB 3rd,Huryn DM

更新日期：2011-01-01 00:00:00

abstract：:Ascidians (tunicates; sea squirts) are marine animals which provide a source of diverse, bioactive natural products, and a model for toxicity screenings. Compounds isolated from ascidians comprise an approved anti-tumor drug and many others are potent drug leads. Furthermore, the use of invertebrate embryos for toxico...

journal_title：Current topics in medicinal chemistry

authors： Dumollard R,Gazo I,Gomes IDL,Besnardeau L,McDougall A

更新日期：2017-01-01 00:00:00

abstract：:Escherichia coli purine nucleoside phosphorylase (PNP) catalyzes the cleavage of 9-(2-deoxy-beta-D-ribofuranosyl)-6-methylpurine (MeP-dR), while human PNP does not. MeP-dR is well tolerated while the cleavage product, 6-methylpurine (MeP), is highly cytotoxic. This clinical profile suggests an anticancer gene therapy ...

journal_title：Current topics in medicinal chemistry

authors： Zhang Y,Parker WB,Sorscher EJ,Ealick SE

更新日期：2005-01-01 00:00:00

abstract：:PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...

journal_title：Current topics in medicinal chemistry

authors： Nanda BL,Nataraju A,Rajesh R,Rangappa KS,Shekar MA,Vishwanath BS

更新日期：2007-01-01 00:00:00

abstract：:Two general aspects which need to be considered for the successful application of dendrimers for biomedical purposes are their availability at an acceptable cost and their suitability as regards their pharmacodynamic and pharmacokinetic properties. These two aspects are covered in this review. In the first part, synth...

journal_title：Current topics in medicinal chemistry

authors： Villalonga-Barber C,Micha-Screttas M,Steele BR,Georgopoulos A,Demetzos C

更新日期：2008-01-01 00:00:00

abstract：:Target-Related Affinity Profiling (TRAP) is a computational drug discovery technology that is based on 'affinity fingerprints', which are molecular descriptors derived from the protein binding preferences of small molecules. The underlying concepts of TRAP are reviewed. Affinity fingerprints are compared to molecular ...

journal_title：Current topics in medicinal chemistry

authors： Beroza P,Damodaran K,Lum RT

更新日期：2005-01-01 00:00:00

abstract：:Pyrola (Pyrolaceae), also known as Luxiancao/in China, was recorded in Sheng Nong's Herbal Classic listed in top grade. Pyrola herbs were used as medicinal plants for a long history with wide-ranging activities such as nourishing kidney-yang, strengthening muscles and bones, activating blood, stopping bleeding, dispel...

journal_title：Current topics in medicinal chemistry

authors： Yang X,She J,Liu J,Yang T,An G,Chen Q,Fan C,Li S,Liu Q,Qian C,Liu Y,Zhou Y,Zhao J

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS:A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofil...

journal_title：Current topics in medicinal chemistry

authors： Singla RK,Dubey AK

更新日期：2019-01-01 00:00:00

abstract：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 00:00:00

abstract：:The serotonin receptor subtype 5 HT(1A) was one of the first serotonin receptor subtypes pharmacologically characterized. Over the last twenty years the 5 HT(1A) receptor has been the object of intense research efforts as witnessed by the 5 HT(1A) acting drugs marketed as anxiolytics. In recent years, several new chem...

journal_title：Current topics in medicinal chemistry

authors： Lacivita E,Leopoldo M,Berardi F,Perrone R

更新日期：2008-01-01 00:00:00

abstract：:The replication cycle of human immunodeficiency virus (HIV) is divided into an early and a late phase. Most of the steps of the cycle have been targeted in antiviral therapy, although the drugs currently available for clinical use are only effective against two replication enzymes of the virus, either against the reve...

journal_title：Current topics in medicinal chemistry

authors： Tözsér J

更新日期：2003-01-01 00:00:00

abstract：:Iron chelators may be of value as therapeutic agents in the treatment of cancer. They may act by depleting iron, a necessary nutrient, and limiting tumor growth. Alternatively or additionally, they may form redox-active metal complexes that cause oxidative stress via production of reactive oxygen species, damaging cri...

journal_title：Current topics in medicinal chemistry

authors： Buss JL,Greene BT,Turner J,Torti FM,Torti SV

更新日期：2004-01-01 00:00:00

abstract：:A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Lang W,Masucci JA

更新日期：2012-01-01 00:00:00

abstract：:Nanotechnology is revolutionizing the development of different branches of science. The investigation of nanomaterials in the battle against cancer is not an exception. The main goal of this contribution is to bring an overview about the types of organic and inorganic nanomaterials that are under investigation for its...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Dominguez CN,Gallardo-Blanco HL,Rodriguez-Rodriguez AA,Vela-Gonzalez AV,Sanchez-Dominguez M

更新日期：2014-03-01 00:00:00

abstract：:Several non-cardiovascular drugs have been withdrawn from the market due to their inhibition of hERG K+ channels that can potentially lead to severe heart arrhythmia and death. As hERG safety testing is a mandatory FDArequired procedure, there is a considerable interest for developing predictive computational tools to...

journal_title：Current topics in medicinal chemistry

authors： Braga RC,Alves VM,Silva MF,Muratov E,Fourches D,Tropsha A,Andrade CH

更新日期：2014-01-01 00:00:00

abstract：:The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

journal_title：Current topics in medicinal chemistry

authors： Aiello F,Valacchi G

更新日期：2014-01-01 00:00:00

abstract：:HIV-1 integrase (IN) plays an important role in the life cycle of HIV and is responsible for integration of the virus into the human genome. We present computational approaches used to design novel HIV-1 IN inhibitors. We created an IN inhibitor database by collecting experimental data from the literature. We develope...

journal_title：Current topics in medicinal chemistry

authors： Guasch L,Zakharov AV,Tarasova OA,Poroikov VV,Liao C,Nicklaus MC

更新日期：2016-01-01 00:00:00

abstract：:Estrogens control a wide number of aspects of human physiology and play a key role in multiple diseases, including cancer. Estrogens act by binding to and activating the cognate receptor (ER), however numerous studies have revealed that the G protein-coupled receptor named GPR30/GPER mediates also estrogen signals. As...

journal_title：Current topics in medicinal chemistry

authors： Sinicropi MS,Lappano R,Caruso A,Santolla MF,Pisano A,Rosano C,Capasso A,Panno A,Lancelot JC,Rault S,Saturnino C,Maggiolini M

更新日期：2015-01-01 00:00:00

abstract：:The use of vaccines has led to tremendous decreases in disease burdens across the world. Many challenges remain in expanding vaccine coverage to new pathogens, however, a struggle further hampered by a lack of understanding into many of the fundamental processes through which vaccines elicit robust immunity. In this r...

journal_title：Current topics in medicinal chemistry

authors： Platt A,Wetzler L

更新日期：2013-01-01 00:00:00

abstract：:Thermolysin (TLN) and other thermolysin-like zinc metalloproteinases (TLPs),are important virulence factors for pathogenesis of bacterial infections by suppressing the innate immune system of the host. Therapeutic inhibition ofTLPs is believed to be a novel strategy inthe development of a new generation antibiotics.In...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Dedachi K,Matsui T,Kurita N,Borgatti M,Gambari R,Sylte I

更新日期：2012-01-01 00:00:00

abstract：:Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which...

journal_title：Current topics in medicinal chemistry

authors： Layton ME,Kelly MJ 3rd,Rodzinak KJ

更新日期：2006-01-01 00:00:00

abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

journal_title：Current topics in medicinal chemistry

authors： Casazza V,Rossi F,Rizzi M

更新日期：2011-01-01 00:00:00