Screening drugs for metabolic stability using pulsed ultrafiltration mass spectrometry.

abstract：:The emergence of drug-resistant strains among the variety of pathogens worsens the situation in today's scenario. In such a situation, a very heavy demand for developing the new antibiotics has arisen, but unfortunately, very limited success has been achieved in this arena till now. Infectious diseases usually make th...

journal_title：Combinatorial chemistry & high throughput screening

authors： Mohan M,Bhattacharya D

更新日期：2021-01-01 00:00:00

abstract：:Gelatinase B/MMP-9 fulfills crucial regulator or effector functions in disease states and may be pharmacologically targeted by specific inhibitors. The characteristics of cleavages of a natural gelatinase B substrate were simulated and amino acids with zinc-ion chelating side-groups were employed to design a library o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hu J,Dubois V,Chaltin P,Fiten P,Dillen C,Van den Steen PE,Opdenakker G

更新日期：2006-09-01 00:00:00

abstract：:While the in vitro selection of nucleic acid binding species (aptamers) requires numerous liquid-handling steps, these steps are relatively straightforward and the overall process is therefore amenable to automation. Here we demonstrate that automated selection techniques are capable of generating aptamers against a n...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cox JC,Rajendran M,Riedel T,Davidson EA,Sooter LJ,Bayer TS,Schmitz-Brown M,Ellington AD

更新日期：2002-06-01 00:00:00

abstract：:Survival of cells and maintenance of genome depend on detection and repair of damaged DNA through intricate mechanisms. Cancer treatment relies on chemotherapy or radiation therapy that kills neoplastic cells by causing immense damage to the DNA. In many cases, escalated DNA repair mechanism leads to resistance agains...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jain R,Jamal S,Goyal S,Wahi D,Singh A,Grover A

更新日期：2015-01-01 00:00:00

abstract：:Increasingly, combinatorial libraries are used to screen large numbers of complex chemically- and physically-patterned polymers against cell response. There is a strong need to extract meaningful relationships between cell function and material surface features from these experiments. A novel high-throughput cell-mate...

journal_title：Combinatorial chemistry & high throughput screening

authors： Su J,Meredith JC

更新日期：2009-07-01 00:00:00

abstract：:Growth hormone secretagogues (GHSs) are synthetic molecules that stimulate and amplify pulsatile pituitary growth hormone release, via a separate pathway distinct from GH releasing hormone/somatostatin. The activity of GHSs is not fully specific for GH secretion; some GHSs also have slight releasing activity on other ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Isidro ML,Cordido F

更新日期：2006-03-01 00:00:00

abstract：:Bacteriophage (phage) display has been exploited for the purpose of discovering new cancer specific targeting peptides. However, this approach has resulted in only a small number of tumor targeting peptides useful as in vivo imaging agents. We hypothesize that in vivo screening for tumor uptake of fluorescently tagged...

journal_title：Combinatorial chemistry & high throughput screening

authors： Newton-Northup JR,Figueroa SD,Deutscher SL

更新日期：2011-01-01 00:00:00

abstract：:The GoLoco motif is a short Galpha-binding polypeptide sequence. It is often found in proteins that regulate cell-surface receptor signaling, such as RGS12, as well as in proteins that regulate mitotic spindle orientation and force generation during cell division, such as GPSM2/LGN. Here, we describe a high throughput...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kimple AJ,Yasgar A,Hughes M,Jadhav A,Willard FS,Muller RE,Austin CP,Inglese J,Ibeanu GC,Siderovski DP,Simeonov A

更新日期：2008-06-01 00:00:00

abstract：:Trivalent lanthanide ions (Ln(3+)) doped inorganic nanocrystals (NCs) have currently attracted reviving interest and come to the forefront in nanophotonics owing to their potential applications in diverse fields such as luminescent biodetection and bioimaging. As an alternative to conventional biolabels, Ln(3+)-doped ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ju Q,Tu D,Liu Y,Zhu H,Chen X

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND:Increasing the resistance issue has become the reason for the development of new antibacterial in crucial condition. Many ways are tracked to determine the most effective antibacterial agent. Some proteins that are a key role in bacteria metabolism are targeted, including MurA in cell wall biosynthesis and g...

journal_title：Combinatorial chemistry & high throughput screening

authors： Apriyanti E,Satari MH,Kurnia D

更新日期：2021-01-01 00:00:00

abstract：:Substructural Molecular Fragments (SMF) method was applied for computer-aided design of new compounds potentially possessing high anti-HIV activities: tetrahydroimidazobenzodiazepinone (TIBO) derivatives and 1-[2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives. Using available experimental data, the SMF...

journal_title：Combinatorial chemistry & high throughput screening

authors： Varnek A,Solov'ev VP

更新日期：2005-08-01 00:00:00

abstract：:A new, efficient, and solvent-free cyclocondensation reaction of arylmethylidenepyruvic acids with 6- aminouracils is presented that uses a catalytic amount of ZnO nanoparticles (ZnO Nps) as a recyclable catalyst at 70 °C. This protocol has the advantages of high yields (91-98%), easy work-up, very short reaction time...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abdolmohammadi S

更新日期：2013-01-01 00:00:00

abstract：AIM:It has been reported that glial cells are involved in Alzheimer's disease (AD). According to our previous research, Scutellaria barbata flavonoids (SBFs) can protect the neuronal disorder and memory impairment for AD-like rats, while the effect of SBFs on the glial cells disorder in AD-like rats has been less well ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cheng JJ,Guo Q,Wu XG,Ma S,Gao Y,Ya-Zhen S

更新日期：2020-12-08 00:00:00

abstract：:Approximately 5-10% of all colorectal carcinomas arise from cancer predisposition syndromes caused by heterozygote germline mutations in post-replicative DNA mismatch repair (MMR) genes. In contrast to gastrointestinal polyposis syndromes, carcinomas in these patients do not occur on the background of increased number...

journal_title：Combinatorial chemistry & high throughput screening

authors： Merkelbach-Bruse S,Köse S,Losen I,Bosserhoff AK,Buettner R

更新日期：2000-12-01 00:00:00

abstract：:We have developed high throughput fluorescence cell imaging methods to screen chemical libraries for compounds with effects on diverse aspects of cell physiology. We describe screens for compounds that arrest cells in mitosis, that block cell migration, and that block the secretory pathway. Each of these screens yield...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yarrow JC,Feng Y,Perlman ZE,Kirchhausen T,Mitchison TJ

更新日期：2003-06-01 00:00:00

abstract：BACKGROUND:Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there's a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. AIM AND OBJECTIVE:The current research focuses on ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kırımlıoğlu GY,Özer S,Büyükköroğlu G,Yazan Y

更新日期：2020-04-27 00:00:00

abstract：AIM AND OBJECTIVE:Avicularin has been found to inhibit the proliferation of HepG-2 cells in vitro in the screening of our laboratory. We intended to explain the molecular mechanism of this effect. Therefore, the combined methods of reverse molecular docking and network pharmacology were used in order to illuminate the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Duan C,Li Y,Dong X,Xu W,Ma Y

更新日期：2019-01-01 00:00:00

abstract：:Cyclic peptides have been often utilized as metabolically stable, conformationally restricted mimics of different kinds of biologically active peptides, including peptide antibiotics, endogenous opioid peptides, integrin inhibitors, peptide hormones, anticancer peptides, and so on. And in particular, cyclic compounds ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gentilucci L,Cardillo G,Tolomelli A,Squassabia F,De Marco R,Chiriano G

更新日期：2009-12-01 00:00:00

abstract：:There exists a great amount of information on ranking methods provided in the literature, a new appealing methodology that is generally dealt in a so mathematical fashion. Ranking strategies are applied in a wide range of scientific fields, such as Decision Support, Toxicology, Environmental Research, Analytical Chemi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Duchowicz PR,Castr EA

更新日期：2008-12-01 00:00:00

abstract：:Chromatographic fingerprinting technique of traditional Chinese medicine (TCM) has proved to be a comprehensive strategy for assessing the intact quality of herbal medicine. In general, one could use the chromatographic techniques to obtain a relatively complete picture of herbal medicines, which are in common called ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liang YZ,Xie PS,Chan K

更新日期：2010-12-01 00:00:00

abstract：AIM AND OBJECTIVE:In ancient China, rice bran was used to treat diabetes and hyperlipidemia. The aim of this paper is to explore the active compounds and underlying mechanism of rice bran petroleum ether extracts (RBPE) against diabetes using network pharmacology. MATERIALS AND METHODS:Gas chromatography-mass spectrom...

journal_title：Combinatorial chemistry & high throughput screening

authors： Huang X,Zhang M,Wu H,Wang X,Xu F

更新日期：2020-08-21 00:00:00

abstract：:4-Benzothiazol-2-ylamino-4-oxo-2-butenoic acid, prepared from reaction of 2-aminobenzothiazole and maleic anhydride, are used as an acid component in Passerini three-component reaction, under solvent-free media, to produce unsaturated α-benzothiazole acyloxyamides in good yields. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sheikholeslami-Farahani F,Shahvelayati AS

更新日期：2013-11-01 00:00:00

abstract：:Phage display is a biological system which facilitates the cloning and rapid selection of peptides from large combinatorial libraries. In compa-rison to the chemical combinatorial approach, the advantages of phage display lie in its simplicity and replicability. While phage display has many diverse applications, this ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Andres CJ,Denhart DJ,Deshpande MS,Gillman KW

更新日期：1999-08-01 00:00:00

abstract：BACKGROUND:In recent years, Staphylococcus aureus have developed resistance to medicines used for the treatment of human infections. Therefore, the search for antibacterial agents of high potency against Staphylococcus aureus is of great concern. Peptide deformylase (PDF), a metalloprotease catalyzing the removal of a ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liang L,Zhou Q,Hao Z,Wang F,Zhu Y,Lin Q,Gao J

更新日期：2018-01-01 00:00:00

abstract：:High throughput screening (HTS) campaigns, where laboratory automation is used to expose biological targets to large numbers of materials from corporate compound collections, have become commonplace within the lead generation phase of pharmaceutical discovery. Advances in genomics and related fields have afforded a we...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yang X,Parker D,Whitehead L,Ryder NS,Weidmann B,Stabile-Harris M,Kizer D,McKinnon M,Smellie A,Powers D

更新日期：2006-02-01 00:00:00

abstract：:Polo-like kinase 1 (Plk1) is a decisive enzyme with its multifunctional activity in cell cycle progression especially mitosis. The over expression of Plk1 in broad spectrum of cancer types turns into a promising therapeutic target against cancer. In the present study, several ligand based pharmacophore models and atom...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chekkara R,Gorla VR,Susithra E,Tenkayala SR

更新日期：2014-01-01 00:00:00

abstract：:The National Institute of Mental Health (NIMH) Psychoactive Drug Screening Program (PDSP) is a resource that provides free screening of novel compounds to academic investigators. This program differs from other public-sector screening programs in that compounds are screened against a large panel of transmembrane recep...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jensen NH,Roth BL

更新日期：2008-07-01 00:00:00

abstract：:A three-component 3+2 cycloaddition reaction followed by Suzuki coupling reaction was carried out to synthesize a library of compounds using automation (parallel synthesizer). Scaffolds that are unexplored in literature were used for the synthesis of library. The iodo-triazoles formed by 3+2 cycloaddition reaction wer...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kavitha M,Mahipal B,Mainkar PS,Chandrasekhar S

更新日期：2013-09-01 00:00:00

abstract：:Voltage-clamp techniques are typically used to study the plasma membrane proteins, such as ion channels and transporters that control bioelectrical signals. Many of these proteins have been cloned and can now be studied as potential targets for drug development. The two approaches most commonly used for heterologous e...

journal_title：Combinatorial chemistry & high throughput screening

authors： Papke RL,Smith-Maxwell C

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:ADAMTS (A disintegrin-like metalloproteinase with thrombospondin motifs) is a group of 19 zinc-dependent metalloproteases known to function in many pathological and physiological processes, such as adhesion, cell fusion, signaling, proteolysis and ECM degradation. OBJECTIVES:The aim of this study was to dem...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tayman MA,Koyuncu İ,Köklü NÖ

更新日期：2020-01-01 00:00:00