Natural products and ion channel pharmacology.

abstract：:Although activity has been reported in vivo, free nucleic acid-based drugs are rapidly degraded and cleared following systemic administration. To address these challenges and improve the potency and bioavailability of genetic drugs, significant efforts have been made to develop effective delivery systems of which lipi...

journal_title：Future medicinal chemistry

authors： Lin PJ,Tam YK

更新日期：2015-01-01 00:00:00

abstract：:Due to the impermeable structure and barrier function of the blood-brain barrier (BBB), the delivery of therapeutic molecules into the CNS is extremely limited. Nanodelivery systems are regarded as the most effective and versatile carriers for the CNS, as they can transport cargo molecules across the BBB via various m...

journal_title：Future medicinal chemistry

authors： Kim KT,Lee HS,Lee JJ,Park EK,Lee BS,Lee JY,Bae JS

更新日期：2018-11-01 00:00:00

abstract：:Dextran has become a hot research topic in drug vehicle material because of its biodegradable, nonspecific cell adhesion, resistance to protein adsorption, low price and ease of structural modification. The fate and changes of dextran in vivo are not fully understood. It is helpful to guide the design and modification...

journal_title：Future medicinal chemistry

authors： Huang S,Huang G

更新日期：2019-07-01 00:00:00

abstract：AIM:The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS:Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhib...

journal_title：Future medicinal chemistry

authors： El-Bakhshawangy NM,El-Nassan HB,Kassab AE,Taher AT

更新日期：2018-06-01 00:00:00

abstract：:Trichomonas vaginalis and Entamoeba histolytica are clinically important protozoa that affect humans. T. vaginalis produces sexually transmitted infections and E. histolytica is the causative agent of amebic dysentery. Metronidazole, a compound first used to treat T. vaginalis in 1959, is still the main drug used worl...

journal_title：Future medicinal chemistry

authors： Moya IA,Su Z,Honek JF

更新日期：2009-07-01 00:00:00

abstract：:Every organism is in contact with numerous small molecules (<1000 Da). Chemicals may cause or trigger adverse health effects, including diseases of the immune system. They may also be exploited as drugs. In this review, we look at the interaction between small molecules and the immune system. We discuss the hapten and...

journal_title：Future medicinal chemistry

authors： Kadow S,Jux B,Chmill S,Esser C

更新日期：2009-12-01 00:00:00

abstract：:Nucleoside analogs are extremely useful for the development of therapeutic agents to control viral diseases and cancer. Among the numerous modifications on the nucleoside skeleton, replacement of the oxygen of the furanose ring by a CH2 group resulted in increased flexibility and higher resistance to phosphorylases an...

journal_title：Future medicinal chemistry

authors： Bessières M,Chevrier F,Roy V,Agrofoglio LA

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Due to the complex etiology of neurodegenerative diseases, there is growing interest in multitarget drugs. In this study we synthesized and evaluated a new series of compounds, with benzo[f]coumarin structure, as potential inhibitors of MAO-A, MAO-B, AChE and BuChE. RESULTS:In vitro studies show that most o...

journal_title：Future medicinal chemistry

authors： Matos MJ,Janeiro P,González Franco RM,Vilar S,Tatonetti NP,Santana L,Uriarte E,Borges F,Fontenla JA,Viña D

更新日期：2014-03-01 00:00:00

abstract：:Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...

journal_title：Future medicinal chemistry

authors： Chan CC

更新日期：2012-11-01 00:00:00

abstract：:In total, 47,500,000 people worldwide are affected by dementia and this number is estimated to double by 2030 and triple within 2050 resulting in a huge burden on public health. Alzheimer's disease (AD), a progressive neurodegenerative disorder, is the most common cause of dementia, accounting for 60-70% of all the ca...

journal_title：Future medicinal chemistry

authors： Stotani S,Giordanetto F,Medda F

更新日期：2016-04-01 00:00:00

abstract：:MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...

journal_title：Future medicinal chemistry

authors： Hequet E,Henoumont C,Muller RN,Laurent S

更新日期：2019-05-01 00:00:00

abstract：BACKGROUND:Cucurbit[n]urils (CB[n]; n = 5, 6, 7, 8 or 10) are a family of macrocycles made from the acid-catalyzed condensation of glycoluril and formaldehyde. RESULTS:The synthesis of CB[n] using microwave radiation has been examined and the effect of acid type, reaction time and temperature on the distribution of pr...

journal_title：Future medicinal chemistry

authors： Wheate NJ,Patel N,Sutcliffe OB

更新日期：2010-02-01 00:00:00

abstract：:At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing a...

journal_title：Future medicinal chemistry

authors： Huang G,Huang H

更新日期：2017-10-01 00:00:00

abstract：:Sialic acid is associated with glycoproteins and gangliosides of eukaryotic cells. It regulates various molecular interactions, being implicated in inflammation and cancer, where its expression is regulated by sialyltransferases and sialidases. Angiogenesis, the formation of new capillaries, takes place during inflamm...

journal_title：Future medicinal chemistry

authors： Chiodelli P,Urbinati C,Paiardi G,Monti E,Rusnati M

更新日期：2018-12-01 00:00:00

abstract：:Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positiv...

journal_title：Future medicinal chemistry

authors： Manetti D,Bellucci C,Chiaramonte N,Dei S,Teodori E,Romanelli MN

更新日期：2018-02-01 00:00:00

abstract：:Despite the wealth of information available for the reverse transcriptase (RT)-associated ribonuclease H (RNaseH) domain of lentiviruses, gammaretroviruses and long terminal repeat containing retrotransposons, exploiting this information in the form of an RNaseH inhibitor with high specificity and low cellular toxicit...

journal_title：Future medicinal chemistry

authors： Corona A,Masaoka T,Tocco G,Tramontano E,Le Grice SF

更新日期：2013-12-01 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Since their initial isolation from the marine alga Delisea pulchra, bromofuranones have been investigated as potential inhibitors of quorum sensing (QS) in various bacterial strains. QS is an important mechanism by which bacteria co-ordinate their molecular response to the environment. QS is intrinsically linked to ba...

journal_title：Future medicinal chemistry

authors： Lyons T,Gahan CG,O'Sullivan TP

更新日期：2020-11-01 00:00:00

abstract：:Systematic investigation of the lipidome will reveal new opportunities for disease diagnosis and intervention. However, lipidomic research has been hampered by the lack of molecular tools to track specific lipids of interest. Accumulating reports indicate lipid recognition can be achieved with properly constructed sho...

journal_title：Future medicinal chemistry

authors： Gao J,Zheng H

更新日期：2013-05-01 00:00:00

abstract：AIM:Hypertension is associated with development of cardiovascular disease and has become a significant health problem worldwide. Naturally-derived antihypertensive peptides have emerged as promising alternatives to synthetic drugs. MATERIALS & METHODS:This study introduces predictor of antihypertensive activity of pep...

journal_title：Future medicinal chemistry

authors： Win TS,Schaduangrat N,Prachayasittikul V,Nantasenamat C,Shoombuatong W

更新日期：2018-08-01 00:00:00

abstract：:The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...

journal_title：Future medicinal chemistry

authors： Sun G,Zhao L,Zhong R,Peng Y

更新日期：2018-08-01 00:00:00

abstract：:Aim: To determine the computer-predicted anticancer activity of mupirocin and to compare its activities with those determined for another polyene antibiotic, batumin. Materials & methods: Molecular docking, cytotoxicity assays, cell microscopy and cell cycle progression were studied in cancer and nontumorigenic cell l...

journal_title：Future medicinal chemistry

authors： Reva ON,Rademan S,Visagie MH,Lebelo MT,Gwangwa MV,Klochko VV,Joubert AM,Lall N

更新日期：2019-04-01 00:00:00

abstract：:Mitochondria play a key role in ATP generation, redox homeostasis and regulation of apoptosis. Due to the essential role of mitochondria in metabolism and cell survival, targeting mitochondria in cancer cells is considered as an attractive therapeutic strategy. However, metabolic flexibility in cancer cells may enable...

journal_title：Future medicinal chemistry

authors： Cui Q,Wen S,Huang P

更新日期：2017-06-01 00:00:00

abstract：:An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2016-01-01 00:00:00

abstract：AIM:The pharmacotherapy of inflammatory bowel disease is difficult and currently available treatments bring mostly poor and unsatisfactory results. RESULTS:The purpose of this work was the synthesis of opiorphin, sialorphin, spinorphin and a series of their analogs and the in vitro characterization of their effect on ...

journal_title：Future medicinal chemistry

authors： Kamysz E,Sałaga M,Sobocińska M,Giełdoń A,Fichna J

更新日期：2016-12-01 00:00:00

abstract：:Kinetic and thermodynamic ligand-protein binding parameters are gaining growing importance as key information to consider in drug discovery. The determination of the molecular structures, using particularly x-ray and NMR techniques, is crucial for understanding how a ligand recognizes its target in the final binding c...

journal_title：Future medicinal chemistry

authors： Deganutti G,Moro S

更新日期：2017-04-01 00:00:00

abstract：BACKGROUND:The understanding of biomolecular interactions ultimately depends on knowledge about the structural and dynamic details of the interacting system. Rational structure-based drug design implements computational methodology in this rationale. DISCUSSION:Together with increasing throughput of structural biology...

journal_title：Future medicinal chemistry

authors： Skjevik AA,Teigen K,Martinez A

更新日期：2009-04-01 00:00:00

abstract：AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...

journal_title：Future medicinal chemistry

authors： Al-Salahi R,Anouar EH,Marzouk M,Taie HA,Abuelizz HA

更新日期：2018-02-01 00:00:00

abstract：:The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena. However, these advances have not led to improvements in drug-discovery success. Drug programs must find new ways to identify superior compounds. Advances in label-free assay technologies may provide advanta...

journal_title：Future medicinal chemistry

authors： Lunn CA

更新日期：2010-11-01 00:00:00