Emerging analytical separation techniques with high throughput potential for pharmaceutical analysis, part I: Stationary phase and instrumental developments in LC.

abstract：:Mass spectrometric plasma analysis for biomarker discovery has become an exploratory focus in proteomic research: the challenges of analyzing plasma samples by mass spectrometry have become apparent not only since the human proteome organization (HUPO) has put much emphasis on the human plasma proteome. This work demo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tammen H,Hess R,Schulte I,Kellmann M,Appel A,Budde P,Zucht HD,Schulz-Knappe P

更新日期：2005-12-01 00:00:00

abstract：:Time-resolved fluorescence (TRF) assay formats are frequently used technologies in high-throughput screening. In this article, we have characterised the novel Plate::Vision(2) 96-microlens array reader (Carl Zeiss Jena GmbH, Germany) and compared it to the novel LEADseeker Generation IV multimodality imaging system (L...

journal_title：Combinatorial chemistry & high throughput screening

authors： Merk S,Lietz A,Kroner M,Valler M,Heilker R

更新日期：2004-02-01 00:00:00

abstract：:Microwave-assisted Suzuki-Miyaura and Stille cross-coupling reactions for the synthesis of highly electron-rich and diversely functionalized biaryl intermediates are presented. Microwave-irradiation has been demonstrated to be a very powerful tool for performing difficult transition metal-catalyzed cross-coupling reac...

journal_title：Combinatorial chemistry & high throughput screening

authors： Appukkuttan P,Dehaen W,Van der Eycken E

更新日期：2007-11-01 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：:Due to the numerous challenges in hit identification from random RNAi screening, we have examined current practices with a discovery of a variety of methodologies employed and published in many reports; majority of them, unfortunately, do not address the minimum associated criteria for hit nomination, as this could po...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bhinder B,Djaballah H

更新日期：2012-11-01 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：AIM AND OBJECTIVE:Antibiotic resistance is a serious constraint to the development of new effective antibacterials. Therefore, the discovery of the new antibacterials remains one of the main challenges in modern medicinal chemistry. This study was undertaken to identify novel molecules with antibacterial activity. MAT...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ivanenkov YA,Yamidanov RS,Osterman IA,Sergiev PV,Aladinskiy VA,Aladinskaya AV,Terentiev VA,Veselov MS,Ayginin AA,Skvortsov DA,Komarova KS,Chemeris AV,Baimiev AK,Sofronova AA,Malyshev AS,Machulkin AE,Petrov RA,Bezrukov D

更新日期：2019-08-08 00:00:00

abstract：:Virtual screening encompasses a wide range of computational approaches aimed at the high-throughput, cost-efficient exploration of chemical libraries or databases to discover new bioactive compounds or novel medical indications of known drugs. Here, we have performed a systematic comparison of the performance of a lar...

journal_title：Combinatorial chemistry & high throughput screening

authors： Di Ianni ME,Gantner ME,Ruiz ME,Castro EA,Bruno-Blanch LE,Talevi A

更新日期：2015-01-01 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：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：INTRODUCTION:Enzymatic degradation of peptidoglycan, a structural cell wall component of Gram-positive bacteria, has attracted considerable attention being a specific target for many known antibiotics. METHODS:Peptidoglycan hydrolases are involved in bacterial lysis through peptidoglycan degradation. β-N-acetylglucosa...

journal_title：Combinatorial chemistry & high throughput screening

authors： Rathee A,Panwar A,Kumari S,Chhibber S,Kumar A

更新日期：2020-11-03 00:00:00

abstract：:The aim of this review is to describe and to analyze the ingredients that are necessary in order to develop a robust and effective experimental approach for the high-throughput characterization of protein-nanostructured surface interaction. In the first part of this paper we review the nanostructured surface synthesis...

journal_title：Combinatorial chemistry & high throughput screening

authors： Scopelliti PE,Bongiorno G,Milani P

更新日期：2011-03-01 00:00:00

abstract：AIM AND OBJECTIVE:4-Hydroxyphenylpyruvate dioxygenase (HPPD), converting phydroxyphenylpyruvate (HPPA) to homogentisate (HGA), is an important target for treating type I tyrosinemia and synthesizing novel herbicides due to its significant role in tyrosine catabolism. Hence, it is imperative to design novel HPPD inhibit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Fu Y,Sun YN,Cao HF,Yi KH,Zhao LX,Li JZ,Ye F

更新日期：2017-01-01 00:00:00

abstract：:The breast cancer resistant protein (BCRP) is an important transporter and its inhibitors play an important role in cancer treatment by improving the oral bioavailability as well as blood brain barrier (BBB) permeability of anticancer drugs. In this work, a computational model was developed to predict the compounds as...

journal_title：Combinatorial chemistry & high throughput screening

authors： Belekar V,Lingineni K,Garg P

更新日期：2015-01-01 00:00:00

abstract：AIM AND OBJECTIVE:In the past decade, the drug design technologies have been improved enormously. The computer-aided drug design (CADD) has played an important role in analysis and prediction in drug development, which makes the procedure more economical and efficient. However, computation with big data, such as ZINC c...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hua GJ,Hung CL,Tang CY

更新日期：2018-01-01 00:00:00

abstract：:We have developed a high throughput assay for the measurement of protease activity in solution. This technology will accelerate research in functional proteomics and enable biologists to streamline protease substrate evaluation and optimization. The peptide sequences that serve as protease substrates in this assay are...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kozlov IA,Melnyk PC,Zhao C,Hachmann JP,Shevchenko V,Srinivasan A,Barker DL,Lebl M

更新日期：2006-07-01 00:00:00

abstract：BACKGROUND:One of the main problems that fruit health has gone through in recent years is the difficult eradication of their fungal pathogens during crops or the post-harvest stage. This concerns the whole world because it represents huge production losses, fruit export restrictions and consumer distrust. Consequently,...

journal_title：Combinatorial chemistry & high throughput screening

authors： Stegmayer MI,Fernández LN,Álvarez NH,Seimandi GM,Reutemann AG,Derita MG

更新日期：2021-01-20 00:00:00

abstract：OBJECTIVE:Lung cancer is the most prevalent cancer in the world, and lung adenocarcinoma is the most common lung cancer subtype. Identification and determination of relevant prognostic markers are the key steps to personalized cancer management. METHODS:We collected the gene expression profiles from 265 tumor tissues ...

journal_title：Combinatorial chemistry & high throughput screening

authors： He ZH,Lv W,Wang LM,Wang YQ,Hu J

更新日期：2019-01-01 00:00:00

abstract：:A new and simple high-performance liquid chromatography method was developed and validated for the simultaneous determination of retinol, retinyl palmitate, β-carotene, α-tocopherol and vitamin C in rat serum treated with Plantago Major L. and 7,12 dimethylbenz[a]anthracene. High-performance liquid chromatography anal...

journal_title：Combinatorial chemistry & high throughput screening

authors： Levent A,Oto G,Ekin S,Berber I

更新日期：2013-02-01 00:00:00

abstract：:Accurate classification of instances depends on identification and removal of redundant features. Classification of data having high dimensionality is usually performed in conjunction with an appropriate feature selection method. Feature selection enables identification of the most informative feature subset from the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Patil D,Raj R,Shingade P,Kulkarni B,Jayaraman VK

更新日期：2009-06-01 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：:Drug metabolism can have profound effects on the pharmacological and toxicological profile of therapeutic agents. In the pharmaceutical industry, many in vitro techniques are in place or under development to screen and optimize compounds for favorable metabolic properties in the drug discovery phase. These in vitro te...

journal_title：Combinatorial chemistry & high throughput screening

authors： Masimirembwa CM,Thompson R,Andersson TB

更新日期：2001-05-01 00:00:00

abstract：:The development of stents has been a major advancement over balloon angioplasty, improving vessel revascularization in obstructive coronary artery disease. The development of drug-eluting stents (DES) was the next breakthrough, designed to prevent the development of neointimal hyperplasia (restenosis) following percut...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hezi-Yamit A,Sullivan C,Wong J,David L,Chen M,Cheng P,Shumaker D,Wilcox J,Udipi K

更新日期：2009-08-01 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：: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：:Clinical application of viral vectors is often hampered by the lack of selectivity of viral particles for the targeted tissue. This drawback decreases the efficiency of gene delivery and raises safety concerns. We successfully established a novel in vitro evolution protocol to engineer adeno-associated virus vectors w...

journal_title：Combinatorial chemistry & high throughput screening

authors： Märsch S,Huber A,Hallek M,Büning H,Perabo L

更新日期：2010-11-01 00:00:00

abstract：BACKGROUND:Corona Virus Disease 2019 (COVID-19) pandemic threatens patients, societies and healthcare systems around the world. There is an emergent need to search for possible medications. OBJECTIVE:This article intends to use virtual screening and molecular docking methods to find potential inhibitors that can respo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chtita S,Belhassan A,Aouidate A,Belaidi S,Bouachrine M,Lakhlifi T

更新日期：2020-07-30 00:00:00

abstract：:For years, the physicochemical properties of drug candidates have been used to predict their in vivo pharmacokinetic behaviors. Several theories and empirical correlations have been established by various researchers with the overall goal of expediting the drug candidate selection process, with greater confidence and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chiang PC,Hu Y

更新日期：2009-03-01 00:00:00

abstract：AIM AND OBJECTIVE:To determine the mechanisms present in the etiopathogenesis of nasal polyposis. It is not clear whether amino acids contribute in a causal way to the development of the disease. Therefore, the aim of this study was to determine the plasma-free amino acid profile in patients with nasal polyposis and to...

journal_title：Combinatorial chemistry & high throughput screening

authors： Celik M,Şen A,Koyuncu İ,Gönel A

更新日期：2019-01-01 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