High-throughput selection system for assessing the activity of epoxide hydrolases.

abstract：:Cell-based screening using phenotypic assays is a useful means of identifying bioactive chemicals for use as tools to elucidate complex cellular processes. However, the chemicals must display sufficient selectivity and their targets have to be identified. We describe how cell-based screening assays can be designed to ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Schriemer DC,Kemmer D,Roberge M

更新日期：2008-09-01 00:00:00

abstract：:P-glycoprotein (P-gp) is well known to cause multidrug resistance (MDR) in cancer cells. This MDR leads to cancer recurrence which is a major obstacle in cancer treatment. High P-gp expression has been observed in the population of cancer stem cells (CSCs) having self-renewal potential. Early detection and inhibition ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tripathi A,Misra K

更新日期：2016-01-01 00:00:00

abstract：AIMS AND OBJECTIVE:The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tratrat C

更新日期：2020-01-01 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：:A simple and fast method with high reliability is necessary for the identification of mutations, polymorphisms and sequence variants (MPSV) within many genes and many samples, e.g. for clarifying the genetic background of individuals with multifactorial diseases. Here we review our experience with the polymerase chain...

journal_title：Combinatorial chemistry & high throughput screening

authors： Miterski B,Krüger R,Wintermeyer P,Epplen JT

更新日期：2000-06-01 00:00:00

abstract：AIM AND OBJECTIVE:MMP-13 belongs to a large family of proteases called matrix metalloproteinases (MMPs) that degrades type II collagen, the main structural protein of articular cartilage. The main pathologic role of MMP-13 over expression is to contribute to the development of osteoarthritis. METHODS:To find new inhib...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ramezani M,Shamsara J

更新日期：2017-01-01 00:00:00

abstract：:NMR has proven to be a valuable tool for identifying small molecule drug leads that serve as starting points for lead optimization programs. In addition, NMR screening can also be applied during lead optimization in order to improve the pharmacokinetic properties of a compound. In this paper we review the NMR methods ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Huth JR,Sun C

更新日期：2002-12-01 00:00:00

abstract：:Amino acids were immobilised by attaching them via a carbamate linker to Wang resin. These intermediates were converted to 1-(1,3-benzoxazol-2-yl)alkanamines over three steps, followed by coupling with 4-alkyl-6-chloro-1,3,5-triazine-2-amines to furnish the desired N-[1-(1,3-benzoxazol-2-yl)alkyl]-6-alkyl-1,3,5-triazi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Dietrich H,Giencke W,Klein R

更新日期：2005-11-01 00:00:00

abstract：:Sequential injection analysis (SIA) has been employed as the platform for the development of a high throughput automated assay for glutathione (GSH) in nutrition supplements. The proposed assay is based on the on-line formation of a UV-absorbing thioacrylate derivative (lambda(max) = 285 nm) upon reaction of thiol wit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zacharis CK,Tzanavaras PD

更新日期：2010-07-01 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：:Plasmodium falciparum is the most lethal form of the genus Plasmodium which causes malaria, a 'disease of antiquity'. Globally it affects the health and socio-economic development of a large population especially in Sub-Saharan Africa and Southeast Asia. The Plasmodium falciparum dihydrofolate reductase-thymidylate sy...

journal_title：Combinatorial chemistry & high throughput screening

authors： Borkakoty B,Sarma K,Parida P,Prakash A,Mohapatra PK,Mahanta J

更新日期：2014-01-01 00:00:00

abstract：AIM AND OBJECTIVE:Caffeic acid (CA) is a cinnamic acid derivative, found in many vegetable products, with powerful antioxidant activity, the ability to increase collagen production and capacity to prevent premature aging of the skin. The classic emulsions of CA are widely used by the consumer to provide a pleasant, ref...

journal_title：Combinatorial chemistry & high throughput screening

authors： Spagnol CM,Di Filippo LD,Isaac VLB,Correa MA,Salgado HRN

更新日期：2017-01-01 00:00:00

abstract：:In recent years, combinatorial libraries have become a major tool for drug discovery and drug development. Along the way, one potential use of combinatorial chemistry libraries almost been neglected: the basic study of intermolecular interactions. Especially "one-bead-one-structure" libraries can be a powerful means f...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nestler HP,Liu R

更新日期：1998-10-01 00:00:00

abstract：:In the life cycle of hepatitis C virus (HCV), NS3/NS4A protease has been proved to play a vital role in the replication of the HCV virus. Narlaprevir and its derivatives, the inhibitors of NS3/NS4A, would be potentially developed as important anti-HCV drugs in the future. In this study, quantitative structure-activity...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhu J,Li Y,Yu H,Zhang L,Mao X,Hou T

更新日期：2012-07-01 00:00:00

abstract：:Herein, we describe a simple, four-step process for the preparation of 1,2,3-triazino[1,6- a]quinazolin-13-ones. This method involves ring-opening, quinazoline-forming condensation, reduction, diazotization accompanied by rapid intramolecular cyclization in the last step afforded the desired products with structurally...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sayahi MH,Baghersaei S,Goli F,Moghimi S,Mahdavi M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2016-01-01 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：:Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammator...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wood SJ,Miller KA,David SA

更新日期：2004-05-01 00:00:00

abstract：:In the present work, we report characterization studies of antigen(Ag)-antibody (Ab) interaction based on the multi-walled carbon nanotube array-modified gold electrode for label-free electrochemical immunosensor. -COOH functionalization of MWCNT was suggested by FTIR spectroscopy. Images from atomic force microscopy ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zahmatkeshan M,Ilkhani H,Paknejad M,Adel M,Sarkar S,Saber R

更新日期：2015-01-01 00:00:00

abstract：:Formazan-based colorimetric cytotoxicity assays, such as the MTT assay, are typically used to assess cell viability with only metabolically active cells reducing tetrazolium salts into the formazans, which is then quantified by absorbance. Fluorescence offers several advantages compared to colorimetric assays and woul...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ladyman MK,Walton JG,Lilienkampf A,Bradley M

更新日期：2016-01-01 00:00:00

abstract：AIM AND OBJECTIVE:Actinomycetes produce structurally unique secondary metabolites with pharmaceutically essential bioactivities. Salinispora, an obligate marine actinomycete, produces structurally varied and unique secondary metabolites. There is plenty of scope for development of drugs from the novel compounds isolate...

journal_title：Combinatorial chemistry & high throughput screening

authors： Dineshkumar K,Vasudevan A,Hopper W

更新日期：2017-01-01 00:00:00

abstract：:African trypanosomes are the causative agent of sleeping sickness. The therapeutics used to control and treat the disease are very ineffective and thus, the development of improved drugs is urgently needed. Recently, new strategies for the design of novel trypanocidals have been put forward. Among them are techniques ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Adler A,Forster N,Homann M,Göringer HU

更新日期：2008-01-01 00:00:00

abstract：:Centaurea solstitialis L. ssp. solstitialis (CSS) has been used as medicine for various diseases. In this work, root, stem and flower parts of the plant were separately extracted with methanol to execute bioassay-guided isolation. Antiproliferative activities of each extracts on C6 cells (Rat Brain tumor cells) and He...

journal_title：Combinatorial chemistry & high throughput screening

authors： Erenler R,Sen O,Yaglioglu AS,Demirtas I

更新日期：2016-01-01 00:00:00

abstract：:Screening of phage display libraries allows rapid identification of peptides binding to a target. However, functional analysis of the phage sequences and their reproduction as soluble and stable peptides are often the most time-consuming part in the screening. We have used here intein-based peptide biosynthesis to pro...

journal_title：Combinatorial chemistry & high throughput screening

authors： Björklund M,Valtanen H,Savilahti H,Koivunen E

更新日期：2003-02-01 00:00:00

abstract：:Protein Kinase C βII (PKCβII) overexpression has been linked to various diabetic microvascular complications viz. retinopathy, neuropathy, and cardiomyopathy. Novel and potent small molecules with preferential selective inhibitory property of PKCβII will be helpful in treatment as well as understanding insight of PKCβ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Grewal BK,Sobhia ME

更新日期：2014-01-01 00:00:00

abstract：AIM AND OBJECTIVE:Specific inhibitors of monoamine oxidase (MAO)-B are considered useful therapeutic agents in targeting neurological disorders like Alzheimer's and Parkinson's diseases. Due to the academic challenge of designing new hMAO-B inhibitors and the possibility of discovering compounds with improved propertie...

journal_title：Combinatorial chemistry & high throughput screening

authors： Mathew B,Mathew GE,Petzer JP,Petzer A

更新日期：2017-01-01 00:00:00

abstract：:Human activities have introduced tens of thousands of chemicals into water systems around the world which has significantly impacted water quality and aquatic ecosystems. The aim of this study was to develop an in silico QSAR model, capable of predicting the aquatic toxicity of pesticides in terms of a lethal dose (LD...

journal_title：Combinatorial chemistry & high throughput screening

authors： Agatonovic-Kustrin S,Morton DW,Razic S

更新日期：2014-01-01 00:00:00

abstract：:A comparative structure-affinity study of anthraquinone dyes adsorption on cellulose fibre is presented in this paper. We used receptor-dependent 4D-QSAR methods based on grid and neural (SOM) methodology coupled with IVEPLS procedure. The applied RD 4D-QSAR approach focuses mainly on the ability of mapping dye proper...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bak A,Wyszomirski M,Magdziarz T,Smolinski A,Polanski J

更新日期：2014-01-01 00:00:00

abstract：:Combinatorial phage peptide libraries have been used to identify the ligands for specific target molecules. These libraries are also useful for identification of the specific substrates of various proteases. A substrate phage library has a random peptide sequence at the N-terminus of the phage coat protein and an addi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ohkubo S,Miyadera K,Sugimoto Y,Matsuo K,Wierzba K,Yamada Y

更新日期：2001-11-01 00:00:00

abstract：BACKGROUND:Panax notoginseng, a Chinese herbal medicine, has been widely used to treat vascular diseases. Diabetic retinopathy (DR) is one of the complications of diabetic microangiopathy. According to recent studies, the application of Panax notoginseng extract and related Chinese patent medicine preparations can sign...

journal_title：Combinatorial chemistry & high throughput screening

authors： Piao C,Sun Z,Jin,Wang H,Wu X,Zhang N,Lian F,Tong X

更新日期：2020-01-01 00:00:00

abstract：:Organic reactions performed in the absence of solvent in domestic ovens without appropriate temperature control are generally considered as not reproducible, particularly when different instruments are used. For this reason, reproducibility has historically been one of the major issues associated with Microwave-Assist...

journal_title：Combinatorial chemistry & high throughput screening

authors： Díaz-Ortiz A,de la Hoz A,Alcázar J,Carrillo JR,Herrero MA,Fontana A,Muñoz Jde M,Prieto P,de Cózar A

更新日期：2011-02-01 00:00:00