Surface plasmon resonance--more than a screening technology: insights in the binding mode of σ70:core RNAP inhibitors.

abstract：:The protein kinase superfamily is one of the most important families of enzymes in molecular biology. Protein kinases typically catalyze the transfer of the γ-phosphate from ATP to a protein substrate (a highly ubiquitous cellular reaction), thereby controlling key areas of cell regulation. Deregulation of protein kin...

journal_title：Future medicinal chemistry

authors： Elphick LM,Lee SE,Anderson AA,Child ES,Bonnac L,Gouverneur V,Mann DJ

更新日期：2009-10-01 00:00:00

abstract：:It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage suffers from a lack of scientists trained in the art and science of early drug discovery chemistry. Many recent publications report the discovery of compounds by screening that are most likely artifacts or promiscuous bioacti...

journal_title：Future medicinal chemistry

authors： Dahlin JL,Walters MA

更新日期：2014-07-01 00:00:00

abstract：:Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor ty...

journal_title：Future medicinal chemistry

authors： Chiba K,Adachi K

更新日期：2012-04-01 00:00:00

abstract：:Endogenous nucleotides have widespread actions in the cardiovascular system, but it is only recently that the P2X and P2Y receptor subtypes, at which they act, have been identified and subtype-selective agonists and antagonists developed. These advances have greatly increased our understanding of the physiological and...

journal_title：Future medicinal chemistry

authors： Kennedy C,Chootip K,Mitchell C,Syed NI,Tengah A

更新日期：2013-03-01 00:00:00

abstract：:The emergence of multidrug-resistant Mycobacterium tuberculosis strains has made many of the currently available anti-tuberculosis (TB) drugs ineffective. Accordingly, there is a pressing need to identify new drug targets. Filamentous temperature-sensitive protein Z (FtsZ), a bacterial tubulin homologue, is an essenti...

journal_title：Future medicinal chemistry

authors： Kumar K,Awasthi D,Berger WT,Tonge PJ,Slayden RA,Ojima I

更新日期：2010-08-01 00:00:00

abstract：:Platinum-based anticancer agents have been widely used in the clinic to successfully treat many different types of cancer. However, the therapeutic efficacy of platinum drugs is limited by serious side effects and the occurrence of inherent or acquired resistance of tumor cells. Nanoparticulate drug-delivery systems h...

journal_title：Future medicinal chemistry

authors： Bryde S,de Kroon AI

更新日期：2009-11-01 00:00:00

abstract：:HIV/AIDS remains a formidable disease with millions of individuals inflicted worldwide. Although treatment regimens have improved considerably, drug resistance brought on by viral mutation continues to erode their effectiveness. Intense research efforts are currently underway in search of new and improved therapies. T...

journal_title：Future medicinal chemistry

authors： Ghosh AK,Anderson DD

更新日期：2011-07-01 00:00:00

abstract：BACKGROUND:The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane and is responsible of a severe form of cystic fibrosis. Trafficking can be improved by small organic molecules called 'correctors'. MATERIALS & METHODS:By different synthetic ways, we prepared 4-chloroanisole ...

journal_title：Future medicinal chemistry

authors： Nieddu E,Pollarolo B,Mazzei MT,Anzaldi M,Schenone S,Pedemonte N,Pesce E,Galietta LJ,Mazzei M

更新日期：2014-01-01 00:00:00

abstract：:Clinical development in brain diseases has one of the lowest success rates in the pharmaceutical industry, and many promising rationally designed single-target R&D projects fail in expensive Phase III trials. By contrast, successful older CNS drugs do have a rich pharmacology. This article will provide arguments sugge...

journal_title：Future medicinal chemistry

authors： Geerts H,Kennis L

更新日期：2014-01-01 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：:The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential applicati...

journal_title：Future medicinal chemistry

authors： Hui M,Jian Z,Peiyuan Z,Zhenwei W,Huibin Z

更新日期：2018-04-01 00:00:00

abstract：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：:Pseudomonas aeruginosa is a leading cause of hospital-acquired infections and is resistant to most antibiotics. With therapeutic options against P. aeruginosa dwindling, and the lack of new antibiotics in advanced developmental stages, strategies for preserving the effectiveness of current antibiotics are urgently req...

journal_title：Future medicinal chemistry

authors： Lamers RP,Burrows LL

更新日期：2016-06-01 00:00:00

abstract：:Aim:   Histone deacetylases (HDACs) are one of the validated targets for cancer treatments. In our previous work, we designed a series of bis-substituted aromatic amide HDAC inhibitors (HDACis), among which compounds 7 and 8 showed promising anticancer effects. However, the low solubilities prevented their subsequent ...

journal_title：Future medicinal chemistry

authors： Yang F,Han L,Zhao N,Yang Y,Ge D,Zhang H,Chen Y

更新日期：2020-04-01 00:00:00

abstract：:Schistosomes, like many eukaryotic pathogens, typically display morphologically distinct stages during their life cycles. Epigenetic mechanisms underlie the pathogens' morphological transformations, and the targeting of epigenetics-driven cellular programs therefore represents an Achilles' heel of parasites. To speed ...

journal_title：Future medicinal chemistry

authors： Marek M,Oliveira G,Pierce RJ,Jung M,Sippl W,Romier C

更新日期：2015-01-01 00:00:00

abstract：:Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

journal_title：Future medicinal chemistry

authors： Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

更新日期：2015-01-01 00:00:00

abstract：:The current state of antimalarial drug resistance emphasizes the need for new therapies with novel modes of action that will add a significant benefit compared with current standards. In this regard, high throughput phenotypic whole-cell screening aids the discovery of novel antiplasmodial scaffolds that are inherentl...

journal_title：Future medicinal chemistry

authors： Paquet T,Gordon R,Waterson D,Witty MJ,Chibale K

更新日期：2012-12-01 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：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：AIM:Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-a...

journal_title：Future medicinal chemistry

authors： Singh A,Viljoen A,Kremer L,Kumar V

更新日期：2017-10-01 00:00:00

abstract：:Anthraquinones exhibit a unique anticancer activity. Since their discovery, medicinal chemists have made several structural modifications, resulting in the design and synthesis of a large number of novel anthraquinone compounds with different biological activities. In general, anthraquinone compounds have been conside...

journal_title：Future medicinal chemistry

authors： Tian W,Wang C,Li D,Hou H

更新日期：2020-04-01 00:00:00

abstract：:PA-824 is an experimental anti-tubercular agent that has a novel mechanism of action. It is effective against both active and persistent forms of the disease and has recently shown early bactericidal activity in a Phase II clinical trial. This review summarizes recent studies on the mode of action of PA-824 and outlin...

journal_title：Future medicinal chemistry

authors： Denny WA,Palmer BD

更新日期：2010-08-01 00:00:00

abstract：:Graphical abstract [Formula: see text]. ...

journal_title：Future medicinal chemistry

authors： Choudhary S,Silakari O

更新日期：2020-02-01 00:00:00

abstract：BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...

journal_title：Future medicinal chemistry

authors： Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch A

更新日期：2013-04-01 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：:FGFs and their receptors (FGFRs) are critical for many biologic processes, including angiogenesis, wound healing and tissue regeneration. Aberrations in FGFR signaling are common in cancer, making FGFRs a promising target in antitumor studies. To date, many FGFR inhibitors are being detected in clinical studies, and r...

journal_title：Future medicinal chemistry

authors： Xue WJ,Li MT,Chen L,Sun LP,Li YY

更新日期：2018-09-01 00:00:00

abstract：:Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...

journal_title：Future medicinal chemistry

authors： Chung PY,Bian ZX,Pun HY,Chan D,Chan AS,Chui CH,Tang JC,Lam KH

更新日期：2015-01-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and its receptors, LPA1-6, are integral parts of signaling pathways involved in cellular proliferation, migration and survival. These signaling pathways are of therapeutic interest for the treatment of multiple types of cancer and to reduce cancer metastasis and side effects. Validated ther...

journal_title：Future medicinal chemistry

authors： Parrill AL

更新日期：2014-05-01 00:00:00

abstract：AIM:Cisplatin resistance in ovarian cancer remains a complex problem as tumors frequently develop resistance against drugs, a mechanism sometimes mediated by ATP-Binding Cassette transporters. Our goal was to find compounds restricting their inhibition capacity to the cisplatin efflux mediated by ABCC2 pump, among prev...

journal_title：Future medicinal chemistry

authors： Comsa E,Nguyen KA,Loghin F,Boumendjel A,Peuchmaur M,Andrieu T,Falson P

更新日期：2018-06-01 00:00:00

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