Dopamine transporter ligands: recent developments and therapeutic potential.

abstract：:The ryanodine receptor (RyR) is the major calcium (Ca(2+)) release channel in the sarcoplasmic reticulum (SR) of skeletal and cardiac muscle and is required for excitation-contraction (EC) coupling. The 565 kDa RyR protein forms a tetrameric channel that is part of a macromolecular signaling complex that also includes...

journal_title：Current topics in medicinal chemistry

authors： Lehnart SE,Huang F,Marx SO,Marks AR

更新日期：2003-01-01 00:00:00

abstract：AIMS:Computational modelling may help us to detect the more important factors governing this process in order to optimize it. BACKGROUND:The generation of hazardous organic waste in teaching and research laboratories poses a big problem that universities have to manage. METHODS:In this work, we report on the experime...

journal_title：Current topics in medicinal chemistry

authors： Montes-Bageneta I,Akesolo U,López S,Merino M,Anakabe E,Arrasate S

更新日期：2020-01-01 00:00:00

abstract：:This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) require...

journal_title：Current topics in medicinal chemistry

authors： Pelton PD,Patel M,Demarest KT

更新日期：2005-01-01 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：:Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, n...

journal_title：Current topics in medicinal chemistry

authors： Bolognesi ML

更新日期：2011-11-01 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：:In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...

journal_title：Current topics in medicinal chemistry

authors： González-Díaz H,Arrasate S,Gómez-SanJuan A,Sotomayor N,Lete E,Besada-Porto L,Ruso JM

更新日期：2013-01-01 00:00:00

abstract：:Ropivacaine, the S-(-)-enantiomer of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinecarboxamide is a new long-acting local anesthetic. This review demonstrates that it is effective in brachial plexus anesthesia. It is at least as efficient as bupivacaine in terms of quality, duration of analgesia, anesthesia, and motor b...

journal_title：Current topics in medicinal chemistry

authors： Singelyn FJ

更新日期：2001-08-01 00:00:00

abstract：:Lipoic acid (LA) is an antioxidant able to produce its effects in aqueous or lipophilic environments. Lipoate is the conjugate base of lipoic acid, and the most prevalent form of LA under physiological conditions. It presents a highly negative reduction potential, increases the expression of antioxidant enzymes and pa...

journal_title：Current topics in medicinal chemistry

authors： Moura FA,de Andrade KQ,dos Santos JC,Goulart MO

更新日期：2015-01-01 00:00:00

abstract：:Aromatic polyketides represent important members of the family of polyketides, which have displayed a wide assortment of bioactive properties, such as antibacterial, antitumor, and antiviral activities. Bacterial aromatic polyketides are mainly synthesized by type II polyketide synthases (PKSs). Whereas malonyl-CoA is...

journal_title：Current topics in medicinal chemistry

authors： Zhan J

更新日期：2009-01-01 00:00:00

abstract：:Rhodiola as one of traditional medicines has been used for clinical treatments due to its strong antioxidant properties. Phytochemical analysis revealed the presence of flavonoids, phenylpropanoids, phenylethanol/benzyl alcohol derivatives, cyanogenic glycosides and terpenoids. The bioactive compounds had been demonst...

journal_title：Current topics in medicinal chemistry

authors： Li Y,Wu J,Shi R,Li N,Xu Z,Sun M

更新日期：2017-01-01 00:00:00

abstract：:Fluorine-18 ((18)F, beta(+); 96.7%, T(1/2)=109.8 min) is of considerable importance for developing positron emission tomography (PET) ligands for imaging receptor, enzyme, gene expression etc. in brain, tumor, myocardium and other regions or organs due to its optimal decay characteristics. To synthesize (18)F-labeled ...

journal_title：Current topics in medicinal chemistry

authors： Zhang MR,Suzuki K

更新日期：2007-01-01 00:00:00

abstract：:Non-selective NSAIDs enhance the risk of serious ulcer complications (bleeding, perforation, obstruction), hospitalization and death about 3-10-fold. The gastrointestinal side effects of NSAIDs have a considerable economical burden, since they are responsible for 5-10 billion dollars in hospitalization charges and los...

journal_title：Current topics in medicinal chemistry

authors： Lehmann FS,Beglinger C

更新日期：2005-01-01 00:00:00

abstract：:Neglected diseases comprise a number of infectious diseases historically endemic to low- and middle-income countries, though recently they have spread to high-income countries due to human migrations. In the past, pharmaceutical companies have shown hesitant to invest in these health conditions, due to the limited ret...

journal_title：Current topics in medicinal chemistry

authors： Bellera CL,Sbaraglini ML,Talevi A

更新日期：2018-01-01 00:00:00

abstract：:In situ structural characterization of organic compounds attached to solid supports can be achieved by high-resolution magic angle spinning NMR (HRMAS NMR), a technique that provides solution-like spectra for resin-bound molecules. This review outlines the principles of the technique, the influence of the solid suppor...

journal_title：Current topics in medicinal chemistry

authors： Espinosa JF

更新日期：2011-01-01 00:00:00

abstract：:Compared with the increasing and widespread bacterial resistance to clinical medicines and the urgent need for cures of intractable diseases, there is a dramatic decline in the numbers of drugs reaching the market or clinical trials. Accordingly, it has become imperative to discover more rational and efficient strateg...

journal_title：Current topics in medicinal chemistry

authors： Wang T,Wu MB,Zhang RH,Chen ZJ,Hua C,Lin JP,Yang LR

更新日期：2016-01-01 00:00:00

abstract：:After the identification of the anti-inflammatory properties of VA5-13l (2-benzyl-1- methyl-5-nitroindazolinone) in previous investigations, some of its analogous compounds were designed, synthesized and evaluated in two anti-inflammatory methods: LPS-enhanced leukocyte migration assay in zebrafish; and 12-O-tetradeca...

journal_title：Current topics in medicinal chemistry

authors： Siverio-Mota D,Andujar I,Marrero-Ponce Y,Giner RM,Diaz-Mendoza C,Paba GM,Vicet-Muro L,Cordero-Maldonado ML,de Witte PAM,Crawford AD,Veitia MS,Perez-Jimenez F,Aran VJ

更新日期：2018-02-09 00:00:00

abstract：:Results of various projects on Mexican Indian ethnobotany and some of the subsequent pharmacological and phytochemical studies are summarised focusing both on chemical-pharmacological as well as anthropological (ethnopharmacological) aspects of our research. We have identified taste and smell properties of medicinal (...

journal_title：Current topics in medicinal chemistry

authors： Heinrich M

更新日期：2003-01-01 00:00:00

abstract：:Cathepsin S has been of increasing interest as a target of medicinal chemistry efforts given its role in modulating antigen-presentation by major histocompatibility class II (MHC II) molecules as well as its involvement in extracellular proteolytic activities. Inhibition of the cathepsin S enzyme reduces degradation o...

journal_title：Current topics in medicinal chemistry

authors： Wiener JJ,Sun S,Thurmond RL

更新日期：2010-01-01 00:00:00

abstract：:Since the advent of high-throughput DNA sequencing technologies, the ever-increasing rate at which genomes have been published has generated new challenges notably at the level of genome annotation. Even if gene predictors and annotation softwares are more and more efficient, the ultimate validation is still in the ob...

journal_title：Current topics in medicinal chemistry

authors： Hernandez C,Waridel P,Quadroni M

更新日期：2014-01-01 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：:Latest microarray-based technologies, including small molecule-, peptide-, protein- and cell-based arrays, and their applications in the field of proteomics are reviewed. ...

journal_title：Current topics in medicinal chemistry

authors： Chen GY,Uttamchandani M,Lue RY,Lesaicherrea ML,Yao SQ

更新日期：2003-01-01 00:00:00

abstract：:Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...

journal_title：Current topics in medicinal chemistry

authors： Meiera C,Renzea J,Ducho C,Balzarini J

更新日期：2002-10-01 00:00:00

abstract：:The knowledge about to which biomolecules a small molecule binds is highly valuable in the drug development process. Although analytical methods to dissect ligand-binding proteome have made substantial progress in the past decades, it is generally too costly, if not infeasible, to know where a small molecule binds at ...

journal_title：Current topics in medicinal chemistry

authors： Lin JH

更新日期：2012-01-01 00:00:00

abstract：:The scaffold protein Axin plays important roles in multiple signaling pathways through mediating the formation of different signaling complexes. Axin is best known for its role as a negative regulator in Wnt/β-catenin pathway. Aberrant activation of the key components in Wnt/β-catenin pathway including Axin has been l...

journal_title：Current topics in medicinal chemistry

authors： Song X,Cai W,Li L

更新日期：2016-01-01 00:00:00

abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...

journal_title：Current topics in medicinal chemistry

authors： Thai KM,Ngo TD,Tran TD,Le MT

更新日期：2013-01-01 00:00:00

abstract：:Traditionally the role of sexual steroid hormones was focused primarily on reproductive organs: the breast, female reproductive tract (uterus, mammary gland, and ovary), and male reproductive tract (testes, epididymis and prostate), however our current understanding of tissue-specific effects of sex steroids has eluci...

journal_title：Current topics in medicinal chemistry

authors： Morimoto S,Jiménez-Trejo F,Cerbón M

更新日期：2011-01-01 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：:Transition metal complexes with terpyridine ligands have attracted a widespread interest with respect to biomedical applications: [(tpy)PtCl]Cl and [(tpy)RuCl(3)] are potent anti-tumor agents with activities comparable to those of cisplatin and carboplatin. The Ru(II) complexes feature a high potential as reactive pro...

journal_title：Current topics in medicinal chemistry

authors： Winter A,Gottschaldt M,Newkome GR,Schubert US

更新日期：2012-01-01 00:00:00

abstract：:Pulmonary drug delivery represents the best way of treating lung diseases, since it allows direct delivery of the drug to the site of action, with few systemic effects. Meanwhile, the lungs may be used as a portal of entry to the body, allowing systemic delivery of drugs via the airway surfaces into the bloodstream. I...

journal_title：Current topics in medicinal chemistry

authors： d'Angelo I,Conte C,Miro A,Quaglia F,Ungaro F

更新日期：2015-01-01 00:00:00