In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery.

abstract：:A pulsed ultrafiltration-mass spectrometric screening assay has been developed to generate and identify electrophilic metabolites of xenobiotic compounds formed by hepatic cytochrome P450 enzymes. This assay would be suitable for the early identification of potentially toxic compounds during the initial phase of drug ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nikolic D,Fan PW,Bolton JL,van Breemen RB

更新日期：1999-06-01 00:00:00

abstract：:The molecular recognition behaviors of some representative bile salts by three 3,6'-bridged beta-cyclodextrin dimers with oligo(ethylenediamino) linkers in different lengths, i.e. 3,6'-(ethylenediamino-bridged) beta-cyclodextrin dimer (1), 3,6'-(diethylenetriamino-bridged) beta-cyclodextrin dimer (2), and 3,6'-(trieth...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu Y,Kang S,Chen Y,Cao R,Shi J

更新日期：2007-06-01 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：: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：:The recent success of the human genome project and the continued accomplishment in obtaining DNA sequences for a vast array of organisms is providing an unprecedented wealth of information. Nevertheless, an abundance of the proteome contains hypothetical proteins or proteins of unknown function, where high throughput ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Powers R

更新日期：2007-09-01 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：BACKGROUND:Traditionally, Phragmitis rhizoma has been prescribed to relive a fever, vomiting, dysuria, and constipation, and to promote secretion of fluids. In addition, recent studies have reported its efficacy as a diuretic and antiemetic. Our previous study demonstrated that the Phragmitis rhizoma aqueous extract (E...

journal_title：Combinatorial chemistry & high throughput screening

authors： Shin S,Kim NS,Kim YA,Oh HR,Bang OS

更新日期：2019-08-08 00:00:00

abstract：:This review describes the design process from conception through realisation and optimisation of a minibody'--a minimised antibody. The result was a proteinaceous molecule of novel fold and metal binding activity. We explain how combinatorial approaches, using phage display libraries, were used to randomise loop regio...

journal_title：Combinatorial chemistry & high throughput screening

authors： Vaughan CK,Sollazzo M

更新日期：2001-08-01 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：:Among the various parasitic diseases, malaria is the deadliest one. Due to the emergence of high drug resistance to the existing drug candidates there is a global need for development of new drug candidates which will be effective against resistant strains of malaria parasite. In silico molecular modeling approaches h...

journal_title：Combinatorial chemistry & high throughput screening

authors： Barmade MA,Murumkar PR,Sharma MK,Shingala KP,Giridhar RR,Yadav MR

更新日期：2015-01-01 00:00:00

abstract：:Shotgun phage display cloning is a useful tool for studying interactions between bacterial and host proteins. Libraries are constructed by cloning randomly fragmented prokaryotic DNA into phage mid-vectors. Theoretically, these libraries will consist of phages that together display all proteins encoded by the bacteria...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jacobsson K,Frykberg L

更新日期：2001-04-01 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：: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：:The electrochemical behavior of atorvastatin calcium at glassy carbon and boron-doped diamond electrodes has been studied using voltammetric techniques. The possible mechanism of oxidation was discussed with model compounds. The dependence of the peak current and potentials on pH, concentration, scan rate and nature o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Dogan-Topal B,Uslu B,Ozkan SA

更新日期：2007-08-01 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：Aims & Objective:Corona Virus Disease 2019 (COVID-19) caused by the human coronavirus 2019 (HCoV-19, also known as SARS-CoV-2) infection is currently in a global outbreak. COVID-19 has posed a huge threat to public health and economic stability worldwide. CR3022, a human monoclonal neutralizing antibody isolated from a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yu W,Wu X,Ren J,Zhang X,Wang Y,Li C,Xu W,Li J,Li G,Zheng W,Liao H,Yuan X

更新日期：2020-10-26 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：: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：BACKGROUND:Clinical outcomes after rotator cuff repair associated with diabetes mellitus(DM) are generally favorable, but no study has attempted to establish the influence of DM on outcomes after rotator cuff repair. PURPOSE:To conduct a meta-analysis of clinical studies evaluating patient outcomes between people with...

journal_title：Combinatorial chemistry & high throughput screening

authors： Lu X,Sun H,Xu Y,Cao X

更新日期：2020-10-20 00:00:00

abstract：:The Emory Chemical Biology Discovery Center (ECBDC) aims to accelerate high throughput biology and translation of biomedical research discoveries into therapeutic targets and future medicines by providing high throughput research platforms to scientific collaborators worldwide. ECBDC research is focused at the interfa...

journal_title：Combinatorial chemistry & high throughput screening

authors： Johns MA,Meyerkord-Belton CL,Du Y,Fu H

更新日期：2014-03-01 00:00:00

abstract：AIM AND OBJECTIVE:Flap endonuclease-1 (FEN1) plays a central role in DNA replication and DNA damage repair process. In mammals, FEN1 functional sites variation is related to cancer and chronic inflammation, and supports the role of FEN1 as a tumor suppressor. However, FEN1 is overexpressed in multiple types of cancer c...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu SB,Qiu XQ,Guo WQ,Li JL,Su Q,Du JH,Hu HJ,Wang XX,Song YH,Lou X,Xu XB

更新日期：2019-01-01 00:00:00

abstract：:Fingerprint representations of molecular structure and properties were among the first computational tools for similarity searching and are widely applied to this date, which is in part due to their computational efficiency and ease-of-use. Moreover, despite their simplicity, 2D molecular fingerprints have been surpri...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wang Y,Bajorath J

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND:A set of antibiotic fluoroquinolones with confirmed antimicrobial activity were analyzed with the use of two types of quantum chemical calculation methods and quantitative structure-activity relationships (QSAR). OBJECTIVE:The purpose of this study was to demonstrate the common and differentiating character...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kawczak P,Bober L,Bączek T

更新日期：2018-01-01 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：AIM AND OBJECTIVE:Lung cancer is a highly heterogeneous cancer, due to the significant differences in molecular levels, resulting in different clinical manifestations of lung cancer patients there is a big difference. Including disease characterization, drug response, the risk of recurrence, survival, etc. Method:Clin...

journal_title：Combinatorial chemistry & high throughput screening

authors： Guo B,Zheng Q

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：:African trypanosomes are extracellular blood parasites that cause sleeping sickness in humans and Nagana in cattle. The therapeutics used to control and treat these diseases are very ineffective and thus, the development of new drugs is urgently needed. We have previously suggested to use trypanosome-specific RNA apta...

journal_title：Combinatorial chemistry & high throughput screening

authors： Homann M,Lorger M,Engstler M,Zacharias M,Göringer HU

更新日期：2006-08-01 00:00:00

abstract：BACKGROUND:The Rab family proteins are involved in membrane trafficking, cell growth and differentiation. Rab38 is implicated in the biogenesis of melanosomes that help in the synthesis, storage and transport of melanin pigments. The Rab38 protein is overexpressed at the RNA level in melanoma cancer. AIM AND OBJECTIVE...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abdelmonsef AH,Dulapalli R,Dasari T,Padmarao LS,Mukkera T,Vuruputuri U

更新日期：2016-01-01 00:00:00

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：:Over the last years microarray technology has become one of the principal platform technologies for the high-throughput analysis of biological systems. Starting with the construction of first DNA microarrays in the 1990s, microarray technology has flourished in the last years and many different new formats have been d...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sobek J,Bartscherer K,Jacob A,Hoheisel JD,Angenendt P

更新日期：2006-06-01 00:00:00